Peplife 2.0 - Browse by Length

Browsing by Length

Browse Results:

Filter by Year
From
Upto

ID	PMID	YEAR	Sequence	Name	Length	N-ter MOD	C-ter MOD	Linear/Cyclic	Chirality	Chem-MOD	Origin	Nature	Incubation Time	Concentration	Half Life	Protease	Assay	Test Sample	Vivo/Vitro	Reference	Patent No.	Activity
1001	20844765	2010	RRWQWR	Lfc1	6	Free	Free	Linear	L	None	Bovine lactoferricin	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=60Î¼M for E.coli
1002	20844765	2010	RRWQWR	Lfc1	6	Free	Free	Linear	L	None	Bovine lactoferricin	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for S. aureus
1003	20844765	2010	RRWQWR	Lfc1	6	Free	Free	Linear	L	None	Bovine lactoferricin	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5 Î¼M for B. subtilis
1004	20844765	2010	RRWWRF	Com1	6	Free	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=60Î¼M for E.coli
1005	20844765	2010	RRWWRF	Com1	6	Free	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for S. aureus
1006	20844765	2010	RRWWRF	Com1	6	Free	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9 Î¼M for B. subtilis
1007	20844765	2010	RRWQWR	Lfc2	6	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=15Î¼M for E.coli
1008	20844765	2010	RRWQWR	Lfc2	6	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=15Î¼M for S. aureus
1009	20844765	2010	RRWQWR	Lfc2	6	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9Î¼M for B. subtilis
1010	20844765	2010	RRWWRF	Com2	6	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for E.coli
1011	20844765	2010	RRWWRF	Com2	6	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for S. aureus
1012	20844765	2010	RRWWRF	Com2	6	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	<30	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=0.9 Î¼M for B. subtilis
1013	20844765	2010	RRWQWR	Lfc3	6	Acetylation	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~60	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=120Î¼M for E.coli
1014	20844765	2010	RRWQWR	Lfc3	6	Acetylation	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~60	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99>120Î¼M for S. aureus
1015	20844765	2010	RRWQWR	Lfc3	6	Acetylation	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~60	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=60 Î¼M for B. subtilis
1016	20844765	2010	RRWWRF	Com3	6	Acetylation	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~60	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=120Î¼M for E.coli
1017	20844765	2010	RRWWRF	Com3	6	Acetylation	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~60	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for S. aureus
1018	20844765	2010	RRWWRF	Com3	6	Acetylation	Free	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~60	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for B. subtilis
1019	20844765	2010	RRWQWR	Lfc4	6	Acetylation	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~90	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=15Î¼M for E.coli
1020	20844765	2010	RRWQWR	Lfc4	6	Acetylation	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~90	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=60Î¼M for S. aureus
1021	20844765	2010	RRWQWR	Lfc4	6	Acetylation	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~90	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=3.8Î¼M for B. subtilis
1022	20844765	2010	RRWWRF	Com4	6	Acetylation	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~90	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for E.coli
1023	20844765	2010	RRWWRF	Com4	6	Acetylation	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~90	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for S. aureus
1024	20844765	2010	RRWWRF	Com4	6	Acetylation	Amidation	Linear	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~90	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9 Î¼M for B. subtilis
1025	20844765	2010	RRWQWR	Lfc5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for E.coli
1026	20844765	2010	RRWQWR	Lfc5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for S. aureus
1027	20844765	2010	RRWQWR	Lfc5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9Î¼M for B. subtilis
1028	20844765	2010	RRWWRF	Com5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for E.coli
1029	20844765	2010	RRWWRF	Com5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for S. aureus
1030	20844765	2010	RRWWRF	Com5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99 ‰¤ 0.45Î¼M for B. subtilis
1031	20844765	2010	CRRWQWRC	Lfc6	8	Free	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~1.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=15Î¼M for E.coli
1032	20844765	2010	CRRWQWRC	Lfc6	8	Free	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~1.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=3.8Î¼M for S. aureus
1033	20844765	2010	CRRWQWRC	Lfc6	8	Free	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	~1.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=0.9Î¼M for B. subtilis
1034	20844765	2010	CRRWWRFC	Com6	8	Free	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	6.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=3.8Î¼M for E.coli
1035	20844765	2010	CRRWWRFC	Com6	8	Free	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	6.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=0.9Î¼M for S. aureus
1036	20844765	2010	CRRWWRFC	Com6	8	Free	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	6.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=0.9Î¼M for B. subtilis
1040	20844765	2010	CRRWWRFC	Com7	8	Acetylation	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	6.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for E.coli
1041	20844765	2010	CRRWWRFC	Com7	8	Acetylation	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	6.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9Î¼M for S. aureus
1042	20844765	2010	CRRWWRFC	Com7	8	Acetylation	Amidation	Cyclic (C1-C8)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	6.5	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99 ‰¤ 0.45Î¼M for B. subtilis
1049	10495424	1999	AAGIGILTV	MART-127 €“35	9	Free	Free	Linear	L	None	Synthetic	Immunogenic peptides	Not given	1 µM	22	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 0.5 µM
1050	10495424	1999	AAGIGILTV	PEG-MART-1	9	Free	Pegylation	Linear	L	None	Synthetic	Immunogenic peptides	Not given	Not given	Stability increased	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is >35 µM
1051	10495424	1999	aAGIGILTv	D-MART-1	9	Free	Free	Linear	Mix	None	Synthetic	Immunogenic peptides	Not given	Not given	Stability increased	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	Not tested
1052	10495424	1999	AAGIGILTV	Glyco-MART-1	9	Asn(Î²-D-GlcNHAc)	Free	Linear	L	None	Synthetic	Immunogenic peptides	Not given	Not given	Stability increased	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	Not tested
1053	10495424	1999	AAGIGILTV	Cap-MART-1	9	Acetylation	Amidation	Linear	L	None	Synthetic	Immunogenic peptides	Not given	Not given	Stability increased	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 65 µM
1054	10495424	1999	AAGIGILTV	N-MART-1	9	Acetylation	Free	Linear	L	None	Synthetic	Immunogenic peptides	Not given	Not given	Stability increased	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 35 µM
1055	10495424	1999	AAGIGILTV	C-MART-1	9	Free	Amidation	Linear	L	None	Synthetic	Immunogenic peptides	Not given	Not given	Stability increased	Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte	Not mentioned	VMM5 cytotoxic T-lymphocyte line incubated in human plasma	in vitro	None	None	IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 7 µM
1078	2147696	1990	PINPRLDG	Control peptide	8	Free	Free	Linear	L	None	Synthetic peptide (scrambled amino acids of human protein S)	Anticoagulant	Not reported	Not mentioned	15	Rabbit blood proteases	Spectrofluorometry	Intravenously injected in male New Zealand white rabbits and blood samples withdrawn and plasma sample prepared	in vivo	None	None	No activity found
1088	12578830	2003	LPFFD	iAÎ²5p	5	Free	Free	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	100% inhibition of amyloid fibrillogenesis
1089	12578830	2003	LP-(NMe)-FFD	iAÎ²5p-A1	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1090	12578830	2003	LP-(NMe)-FF-(NMe)-D	iAÎ²5p-A4	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1091	12578830	2003	LP-(NMe)-F-(NMe)-FD	iAÎ²5p-A5	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1092	12578830	2003	LP-(NMe)-F-(NMe)-F-(NMe)-D	iAÎ²5p-A7	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1093	12578830	2003	LP-(Î±Me)-F-(Î±Me)-FD	iAÎ²5p-B1	5	Acetylation	Amidation	Linear	L	Î±Me	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1094	12578830	2003	LPFFD	iAÎ²5p-C1	5	Free	Amidation	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	5	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1095	12578830	2003	Sar-LPFFD	iAÎ²5p-C2	5	Sar	Amidation	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	7	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1096	12578830	2003	(Nme)-Sar-LPFFD	iAÎ²5p-C3	5	(NMe)Sar	Amidation	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	6	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1097	12578830	2003	LPFFD	iAÎ²5p	5	Free	Free	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	15	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	100% inhibition of amyloid fibrillogenesis
1098	12578830	2003	LP-(NMe)-FFD	iAÎ²5p-A1	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1099	12578830	2003	LP-(NMe)-FF-(NMe)-D	iAÎ²5p-A4	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	5	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1100	12578830	2003	LP-(NMe)-F-(NMe)-FD	iAÎ²5p-A5	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1101	12578830	2003	LP-(NMe)-F-(NMe)-F-(NMe)-D	iAÎ²5p-A7	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1102	12578830	2003	LP-(Î±Me)-F-(Î±Me)-FD	iAÎ²5p-B1	5	Acetylation	Amidation	Linear	L	Î±Me	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1103	12578830	2003	LPFFD	iAÎ²5p-C1	5	Free	Amidation	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	<1	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1104	12578830	2003	Sar-LPFFD	iAÎ²5p-C2	5	Sar	Amidation	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	41	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1105	12578830	2003	(Nme)-Sar-LPFFD	iAÎ²5p-C3	5	(NMe)Sar	Amidation	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	25	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1112	15487959	2004	N-((R)-(((2S)-2-((-p-Amidobenzyl)carbamoyl)-1-azetidinyl)carbonyl)cyclohexylmethyl)glycine	Melagatran	1	N.A.	N.A.	Linear	L	N.A.	Synthetic	Anticoagulant	Not reported	10-¹⁰ €“10^-5 M	4	Human plasma protease	Not mentioned	Human plasma	in vivo	None	None	Not reported
1191	10670753	1999	SPTLAYAVP	Human thyrotropin-releasing hormone (TRH)-associated peptide 3 (hTAP-3)	9	Free	Free	Linear	L	None	Product of proteolysis of preproTRH	Serum hTAP-3 concentration was increased in patients with hyperthyroidism	15 min	Not mentioned	3.5	Human serum proteases	Radioimmunoassay	Human serum	in vivo	None	None	Not reported
1192	14980787	2004	LW	Leucyl-tryptophane	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	7.4	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=15 µM
1193	14980787	2004	SY	Seryl-tyrosine	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	5.2	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=41 µM
1194	14980787	2004	VY	Valyl-tyrosine	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	15	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=11 µM
1195	14980787	2004	LY	Leucyl-tyrosine	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	4.3	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=44 µM
1196	14980787	2004	AY	Alanyl-tyrosine	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	9.4	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=40 µM
1197	14980787	2004	YY	Tyrosyl-tyrosine	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	16	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=9 µM
1198	14980787	2004	AD	Alanyl-aspartate	2	Free	Free	Linear	L	None	Synthetic	Angiotensin Coverting Enzyme inhibitor	Not mentioned	Not mentioned	64	Rat plasma proteases	Spectrophotometry	Rat plasma	in vitro	None	None	IC50=>1600 µM
1239	20560643	2009	YaGFMPLW	Peptide 1 (TY027)	8	Free	NH-3,5-Bzl(CF3)2	Linear	Mix	None	Synthetic	Opioid receptor agonist	24 hours	Not mentioned	4.8	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	IC50=15 ±2nM for MVD
1240	20560643	2009	YaGF-Nle-PLW	Peptide 2	8	Free	NH-3,5-Bzl(CF3)2	Linear	Mix	Nle=norleucine	Synthetic analogues of TY027	Opioid receptor agonist	24 hours	Not mentioned	>6	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	IC50=14 ±1.6nM for MVD
1241	20560643	2009	YaGF-Nle-P-Ser(Glc)-W	Peptide 5	8	Free	NH-3,5-Bzl(CF3)2	Linear	Mix	Nle=norleucine, O-Î²-glucosylated serine	Synthetic analogues of TY027	Opioid receptor agonist	24 hours	Not mentioned	>6	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	IC50=13 ±5.8nM for MVD
1242	20560643	2009	YaGF-Nle-PL-Ser(Glc)-W	Peptide 6	9	Free	NH-3,5-Bzl(CF3)2	Linear	Mix	Nle=norleucine, O-Î²-glucosylated serine	Synthetic analogues of TY027	Opioid receptor agonist	24 hours	Not mentioned	>24	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	IC50=17 ±4.3nM for MVD
1670	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	Not mentioned	10 ±1	Angiotensin-converting enzyme	Radioimmunoassay and HPLC	Blood sample of normotensive Sprague-Dawley rat	in vivo	None	None	Not mentioned
1671	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	10 ±1	Angiotensin-converting enzyme	Radioimmunoassay and HPLC	Blood sample of anesthetized spontaneously hypertensive rat	in vivo	None	None	Not mentioned
1672	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	9 ±1	Angiotensin-converting enzyme	Radioimmunoassay and HPLC	Blood sample of mRen-2 transgenic rat	in vivo	None	None	Not mentioned
1673	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~11 ±1	Angiotensin-converting enzyme and losartan(AT1 antagonist)	Radioimmunoassay and HPLC	Blood sample of normotensive Sprague-Dawley rat	in vivo	None	None	Not mentioned
1674	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~11 ±1	Angiotensin-converting enzyme and losartan(AT1 antagonist)	Radioimmunoassay and HPLC	Blood sample of anesthetized spontaneously hypertensive rat	in vivo	None	None	Not mentioned
1675	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~14 ±1	Angiotensin-converting enzyme and losartan(AT1 antagonist)	Radioimmunoassay and HPLC	Blood sample of mRen-2 transgenic rat	in vivo	None	None	Not mentioned
1676	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~60 ±1	Angiotensin-converting enzyme and lisinopril(inhibitor)	Radioimmunoassay and HPLC	Blood sample of normotensive Sprague-Dawley rat	in vivo	None	None	Not mentioned
1677	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~44 ±1	Angiotensin-converting enzyme and lisinopril(inhibitor)	Radioimmunoassay and HPLC	Blood sample of anesthetized spontaneously hypertensive rat	in vivo	None	None	Not mentioned
1678	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~29 ±1	Angiotensin-converting enzyme and lisinopril(inhibitor)	Radioimmunoassay and HPLC	Blood sample of mRen-2 transgenic rat	in vivo	None	None	Not mentioned
1679	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~45 ±1	Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor)	Radioimmunoassay and HPLC	Blood sample of normotensive Sprague-Dawley rat	in vivo	None	None	Not mentioned
1680	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~49 ±1	Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor)	Radioimmunoassay and HPLC	Blood sample of anesthetized spontaneously hypertensive rat	in vivo	None	None	Not mentioned
1681	9740616	1998	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Angiotensinogen	Antihypertensive	30 min	10 µg	~40 ±1	Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor)	Radioimmunoassay and HPLC	Blood sample of mRen-2 transgenic rat	in vivo	None	None	Not mentioned
1682	9806949	1998	NDWF-Dpr-L	MEN 11420	6	Glycosylation	Free	Cyclic	L	Dpr-2,3-Diaminopropionic acid	MEN 10627	Tachykinin NK2 receptor antagonist	Not reported	Not mentioned	44 ±3	Not mentioned	HPLC	Rat blood plasma	in vivo	None	None	Not mentioned
1693	3343338	1987	GRGDS	Anti-cell adhesive pentapeptide	5	Free	Free	Linear	L	None	Central cell- binding domain of fibronectin	Anti metastatic	Not reported	6 µmol	8	Not mentioned	Radioactivity measured by scintillation counter	Blood sample of C57BL/6 mice	in vivo	None	None	Percentage inhibition of melanotic colony formation=90
1696	7439398	1980	ECG	Glutathione	3	Free	Free	Linear	L	Gamma peptide linkage between the carboxyl group of the glutamate side-chain and the amine group of cysteine	Synthetic	Not mentioned	Not reported	25 ng/kg/min of Bradykinin and the rate doubled every 5 min until a final rate of 200 ng/kg/min was	1.6	Not mentioned	Kinetic assay	Human blood plasma sample	in vivo	None	None	Not mentioned
1698	8257427	1993	SDKP	AcSDKP	4	Acetylation	Free	Linear	L	None	Human bone marrow	Negative regulator of proliferation of haematopoietic stem cells	Not reported	1mM	80	None	Radioactivity measured with liquid-scintillation counter	Human venous blood sample	in vitro	None	None	Not mentioned
1699	8257427	1993	SDKP	AcSDKP	4	Acetylation	Free	Linear	L	None	Human bone marrow	Negative regulator of proliferation of haematopoietic stem cells	Not reported	10nM conc.	50	None	Radioactivity measured with liquid-scintillation counter	Human venous blood sample	in vitro	None	None	Not mentioned
1700	8257427	1993	SDKP	AcSDKP	4	Acetylation	Free	Linear	L	None	Human bone marrow	Negative regulator of proliferation of haematopoietic stem cells	Not reported	10-4M conc	10	Rabbit lung angiotensin I converting enzyme	Radioactivity measured with liquid-scintillation counter	Human venous blood sample	in vitro	None	None	Not mentioned
1701	8257427	1993	SDKP	AcSDKP	4	Acetylation	Free	Linear	L	None	Human bone marrow	Negative regulator of proliferation of haematopoietic stem cells	Not reported	10-7M conc.	25	Rabbit lung angiotensin I converting enzyme	Radioactivity measured with liquid-scintillation counter	Human venous blood sample	in vitro	None	None	Not mentioned
1702	10611139	1999	H(2me)wAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	2me-2-methyl(tryptophan)	Analog of GHRP-6	Peptidyl growth hormone causing GH releasing effect.	Not reported	10 to 25 iu of oxytocin	75.9 ±9.3	Blood proteases	LC-MS/MS	Intravenous injection,Blood sample from male Sprague-Dawley rats	in vivo	None	None	Not mentioned
1703	10611139	1999	H(2me)wAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	2me-2-methyl(tryptophan)	Analog of GHRP-6	Peptidyl growth hormone causing GH releasing effect.	Not reported	5 µg/kg	71.9 ±11.2	Blood proteases	LC-MS/MS	Intravenous injection,Blood sample from male Sprague-Dawley rats	in vivo	None	None	Not mentioned
1704	10611139	1999	H(2me)wAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	2me-2-methyl(tryptophan)	Analog of GHRP-6	Peptidyl growth hormone causing GH releasing effect.	Not reported	10 µg/kg	61.4 ±9.5	Blood proteases	LC-MS/MS	Intravenous injection,Blood sample from male Sprague-Dawley rats	in vivo	None	None	Not mentioned
1705	10611139	1999	H(2me)wAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	2me-2-methyl(tryptophan)	Analog of GHRP-6	Peptidyl growth hormone causing GH releasing effect.	Not reported	50 µg/kg	57.0 ±9.1	Blood proteases	LC-MS/MS	Intravenous injection,Blood sample from male Sprague-Dawley rats	in vivo	None	None	Not mentioned
1707	10871321	2000	RPPGF	BK1-5	5	Free	Free	Linear	L	None	Metabolite of bradykinin	Not mentioned	Not reported	106 cpm/200Î¼l/mouse	~90	Aminopeptidase P,Dipeptidyl-peptidaseIV,KininaseII,KininaseI and neutral endopeptidase	HPLC-ESI-MS	Intravenous injection of Bradykinin,Human blood sample	in vivo	None	None	Not mentioned
1708	10871321	2000	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Human blood plasma	Cardioprotective effects	Not reported	106 cpm/200Î¼l/mouse	Not measured as peptide degraded rapidly<30 approx.	Aminopeptidase P,Dipeptidyl-peptidaseIV,KininaseII,KininaseI and neutral endopeptidase	HPLC-ESI-MS	Human blood sample	in vivo	None	None	Not mentioned
1711	3799211	1986	YFQNCPrG	(I-deamino-8-D-arginine vasopressin)DDAVP	9	1-Î²-mercaptopropionic acid	Free	Linear	Mix	None	Modified form of Vasopressin	Antidiuretic agent	Not reported	90mg	200	Plasma proteases	Radioimmunoassay	Blood sample of human uraemic patients(end stage renal failure)	in vivo	US 5500413 A patent	None	Not mentioned
1712	3799211	1986	YFQNCPrG	(I-deamino-8-D-arginine vasopressin)DDAVP	9	1-Î²-mercaptopropionic acid	Free	Linear	Mix	None	Modified form of Vasopressin	Antidiuretic agent	Not reported	45mg	55	Plasma proteases	Radioimmunoassay	Human blood sample	N.A.	None	US 5500413 A patent	Not mentioned
1713	10454085	1999	CYIQNCPLG	Oxytocin	9	Free	Amidation	Cyclic (C1-C6)	L	None	Hypothalamus	Involved in aiding mechanical clearance mechanism and improving fertility	60 minutes	90mg	6.78	Blood protease	Radioimmunoassay	Intravenous injection of oxytocin in normal mares	in vivo	None	None	Prostaglandin F metabolite(PGFM) release on administeration of 10 iu of oxytocin= 18.48 ±3.62 pg/ml
1714	10454085	1999	CYIQNCPLG	Oxytocin	9	Free	Amidation	Cyclic (C1-C6)	L	None	Hypothalamus	Involved in aiding mechanical clearance mechanism and improving fertility	60 minutes	180mg	6.78	Blood protease	Radioimmunoassay	Intravenous injection of oxytocin in normal mares	in vivo	None	None	Prostaglandin F metabolite(PGFM) release on administeration of 25 iu of oxytocin= 20.09 ±3.29 pg/ml
1715	10544005	1999	YIGSR	YIGSR	5	Free	Free	Linear	L	None	Core sequence located at the Î²-1 chain of laminin	Antimetastatic effect.	Not reported	Not mentioned	<1	Blood protease	Radioactivity measured with a gamma counter	Intravenous injection of labelled peptide in C57BL/6 mice	in vivo	None	None	At 1.5Î¼mol reduced number of colonies of B16-BL6 melanoma cells in lung by 50%
1716	10544005	1999	YIGSR	PEG5000 -YIGSR	5	Pegylated by addition of PEG5000	Free	Linear	L	None	Core sequence located at the Î²-1 chain of laminin	Antimetastatic effect.	Not reported	Not mentioned	2.2	Blood protease	Radioactivity measured with a gamma counter	Intravenous injection of labelled peptide in C57BL/6 mice	in vivo	None	None	At 0.15Î¼mol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx.
1717	10544005	2000	YIGSR	PEG12,000 -YIGSR	5	Pegylated by addition of PEG12,000	Free	Linear	L	None	Core sequence located at the Î²-1 chain of laminin	Antimetastatic effect.	Not reported	Not mentioned	2.5	Blood protease	Radioactivity measured with a gamma counter	Intravenous injection of labelled peptide in C57BL/6 mice	in vivo	None	None	At 0.15Î¼mol reduced number of colonies of B16-BL6 melanoma cells in lung by 50%
1718	10544005	2001	YIGSR	PVP6,000 -YIGSR	5	Addition of Polyvinyl pyrrolidone(PVP6,000)	Free	Linear	L	None	Core sequence located at the Î²-1 chain of laminin	Antimetastatic effect.	Not reported	Not mentioned	14.5	Blood protease	Radioactivity measured with a gamma counter	Intravenous injection of labelled peptide in C57BL/6 mice	in vivo	None	None	At 0.015Î¼mol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx.
1728	1939259	1991	APRLRFYSL	Î±-bag cell peptide Î±-BCP(1-9)	9	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	26	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1729	1939259	1991	APRLRFYSL	Î±-bag cell peptide Î±-BCP(1-9)	9	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-6 M conc. of peptide	35	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1730	1939259	1991	PRLRFYSL	Î±-BCP(2-9)	8	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	64	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1731	1939259	1991	APRLRFYS	Î±-BCP(1-8)	8	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	27	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1732	1939259	1991	APRLRF	Î±-BCP(1-6)	6	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	11	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1733	1939259	1991	APRLR	Î±-BCP(1-5)	5	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	16	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1734	1939259	1991	RLRFYSL	Î±-BCP(3-9)	7	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	2.1	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1735	1939259	1991	RLRFYSL	Î±-BCP(3-9)	7	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-6 M conc. of peptide	2.7	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1736	1939259	1991	LRFYSL	Î±-BCP(4-9)	6	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	2.7	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1737	1939259	1991	RFYSL	Î±-BCP(5-9)	5	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	1.5	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1738	1939259	1991	FYSL	Î±-BCP(6-9)	4	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	0.65	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1739	1939259	1991	YSL	Î±-BCP(7-9)	3	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	9.7	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1740	1939259	1991	RLRFYS	Î±-BCP(3-8)	6	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	1.5	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1741	1939259	1991	LRFYS	Î±-BCP(4-8)	5	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	1.5	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1742	1939259	1991	FYS	Î±-BCP(6-8)	3	Free	Free	Linear	L	None	Bag cells in the abdominal ganglion of the marine snail Aplysia	Neurotransmitter	Not reported	10-5 M conc. of peptide	0.48	Aplysia haemolymph proteases	HPLC	Heamolymph of Aplysia	in vitro	None	None	Not given
1754	16467916	2005	(Pen)-Y(Me)-ARGDN-Tic-C	RGD	9	Acetylation	Amidation	Linear	L	Pen=Penicillamine, Methylation at Tyrosine, Tic=tetrahydroisoquinoline carboxylic acid	Human Glioma cells	Integrin Protein	Not reported	Not mentioned	~20	Proteases present in rat brain homogenates suspended in aCSF	RP-HPLC	Rat brain homogenates suspended in aCSF	in vitro	None	None	No activity found
1773	16990557	2006	CNGRCGGK	cNGR	8	Acetylation	Amidation	Cyclic	L	None	Synthetic peptide	Targets CD13/APN which is present on angiogenic vessels so used for molecular imaging	Not reported	0.75Î¼g/g	9.1 ±0.3	Proteases present in the tissue of angiogenetic vessels in mouse	Fluorometery	Mouse tissue of myocardial infarction (MI) model	in vivo	None	None	Not given
1774	16990557	2006	CNGRCGGK	cNGR	8	Acetylation	Amidation	Cyclic	L	None	Synthetic peptide	Targets CD13/APN which is present on angiogenic vessels so used for molecular imaging	Not reported	0.75Î¼g/g	15.4 ±3.4	Mouse plasma proteases	Fluorometery	Mouse plasma of Murine myocardial infarction (MI) model	in vivo	None	None	Not given
1776	17374660	2007	IPP	IPP	3	Free	Free	Linear	L	None	Lactotripeptide	ACE(Angeotensin converting enzyme)-inhibiting peptide	Not reported	Not mentioned	~ 30	Pancreatic proteases	RP-HPLC	Human blood plasma (oral)	in vivo	None	None	Not given
1870	18307313	2007	R-X-R	CAP 1	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 83 µM for S.aureus
1871	18307313	2007	R-X-R	CAP 1	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 50 µM for Methicillin- resistant S.aureus
1872	18307313	2007	R-X-R	CAP 1	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for Methicillin- resistant S.epidermis
1873	18307313	2007	R-X-R	CAP 2	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	2	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for S.aureus
1874	18307313	2007	R-X-R	CAP 2	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	2	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for Methicillin- resistant S.aureus
1875	18307313	2007	R-X-R	CAP 2	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	2	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 3 µM for Methicillin- resistant S.epidermis
1876	18307313	2007	R-X-R	CAP 3	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	10	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 10 µM for S.aureus
1877	18307313	2007	R-X-R	CAP 3	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	10	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.aureus
1878	18307313	2007	R-X-R	CAP 3	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	10	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1879	18307313	2007	R-X-R	CAP 4	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 47 µM for S.aureus
1880	18307313	2007	R-X-R	CAP 4	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.aureus
1881	18307313	2007	R-X-R	CAP 4	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for Methicillin- resistant S.epidermis
1882	18307313	2007	R-X-R	CAP 5	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for S.aureus
1883	18307313	2007	R-X-R	CAP 5	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 9 µM for Methicillin- resistant S.aureus
1884	18307313	2007	R-X-R	CAP 5	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.epidermis
1885	18307313	2007	R-X-R	CAP 6	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 14 µM for S.aureus
1886	18307313	2007	R-X-R	CAP 6	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 9 µM for Methicillin- resistant S.aureus
1887	18307313	2007	R-X-R	CAP 6	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	1	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.epidermis
1888	18307313	2007	R-X-R	CAP 7	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for S.aureus
1889	18307313	2007	R-X-R	CAP 7	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.aureus
1890	18307313	2007	R-X-R	CAP 7	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.epidermis
1891	18307313	2007	R-X-R	CAP 8	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	3	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for S.aureus
1892	18307313	2007	R-X-R	CAP 8	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	3	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.aureus
1893	18307313	2007	R-X-R	CAP 8	2	Free	NHBn	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	3	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 3 µM for Methicillin- resistant S.epidermis
1894	18307313	2007	R-BIP-R	CAP 9	2	Free	Y= structure given in paper	Linear	L	BIP	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	35	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for S.aureus
1895	18307313	2007	R-Bip-R	CAP 9	2	Free	Y= structure given in paper	Linear	L	BIP	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	35	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.aureus
1896	18307313	2007	R-Bip-R	CAP 9	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	35	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.epidermis
1897	18307313	2007	R-Bip-R	CAP 10	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	9	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 9 µM for S.aureus
1898	18307313	2007	R-Bip-R	CAP 10	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	9	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.aureus
1899	18307313	2007	R-Bip-R	CAP 10	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	9	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.epidermis
1900	18307313	2007	R-Bip-R	CAP 11	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	2	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for S.aureus
1901	18307313	2007	R-Bip-R	CAP 11	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	2	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 7 µM for Methicillin- resistant S.aureus
1902	18307313	2007	R-Bip-R	CAP 11	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	2	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1903	18307313	2007	R-Bip-R	CAP 12	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 8 µM for S.aureus
1904	18307313	2007	R-Bip-R	CAP 12	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 8 µM for Methicillin- resistant S.aureus
1905	18307313	2007	R-Bip-R	CAP 12	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.epidermis
1906	18307313	2007	R-Bip-R	CAP 13	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 12 µM for S.aureus
1907	18307313	2007	R-Bip-R	CAP 13	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 12 µM for Methicillin- resistant S.aureus
1908	18307313	2007	R-Bip-R	CAP 13	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 8 µM for Methicillin- resistant S.epidermis
1909	18307313	2007	R-Bip-R	CAP 14	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 10 µM for S.aureus
1910	18307313	2007	R-Bip-R	CAP 14	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 9 µM for Methicillin- resistant S.aureus
1911	18307313	2007	R-Bip-R	CAP 14	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 6 µM for Methicillin- resistant S.epidermis
1912	18307313	2007	R-Bip-R	CAP 15	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 8 µM for S.aureus
1913	18307313	2007	R-Bip-R	CAP 15	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.aureus
1914	18307313	2007	R-Bip-R	CAP 15	2	Free	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1915	18307313	2007	R-X-R	CAP 16	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 145 µM for S.aureus
1916	18307313	2007	R-X-R	CAP 16	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 95 µM for Methicillin- resistant S.aureus
1917	18307313	2007	R-X-R	CAP 16	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 81 µM for Methicillin- resistant S.epidermis
1918	18307313	2007	R-Bip-R	CAP 16	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 145 µM for S.aureus
1919	18307313	2007	R-Bip-R	CAP 16	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 95 µM for Methicillin- resistant S.aureus
1920	18307313	2007	R-Bip-R	CAP 16	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	7	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 81 µM for Methicillin- resistant S.epidermis
1921	18307313	2007	R-X-R	CAP 17	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for S.aureus
1922	18307313	2007	R-X-R	CAP 17	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.aureus
1923	18307313	2007	R-X-R	CAP 17	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1924	18307313	2007	R-Bip-R	CAP 17	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for S.aureus
1925	18307313	2007	R-Bip-R	CAP 17	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.aureus
1926	18307313	2007	R-Bip-R	CAP 17	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	Stable	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1927	18307313	2007	R-X-R	CAP 18	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for S.aureus
1928	18307313	2007	R-X-R	CAP 18	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.aureus
1929	18307313	2007	R-X-R	CAP 18	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.epidermis
1930	18307313	2007	R-Bip-R	CAP 18	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for S.aureus
1931	18307313	2007	R-Bip-R	CAP 18	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.aureus
1932	18307313	2007	R-Bip-R	CAP 18	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	30	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC<3 µM for Methicillin- resistant S.epidermis
1933	18307313	2007	R-X-R	CAP 19	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 29 µM for S.aureus
1934	18307313	2007	R-X-R	CAP 19	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 29 µM for Methicillin- resistant S.aureus
1935	18307313	2007	R-X-R	CAP 19	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 20 µM for Methicillin- resistant S.epidermis
1936	18307313	2007	R-Bip-R	CAP 19	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 29 µM for S.aureus
1937	18307313	2007	R-Bip-R	CAP 19	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 29 µM for Methicillin- resistant S.aureus
1938	18307313	2007	R-Bip-R	CAP 19	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 20 µM for Methicillin- resistant S.epidermis
1939	18307313	2007	R-X-R	CAP 20	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 50 µM for S.aureus
1940	18307313	2007	R-X-R	CAP 20	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 50 µM for Methicillin- resistant S.aureus
1941	18307313	2007	R-X-R	CAP 20	2	Free	CH2CH2Ph	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 10 µM for Methicillin- resistant S.epidermis
1942	18307313	2007	R-Bip-R	CAP 20	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 50 µM for S.aureus
1943	18307313	2007	R-Bip-R	CAP 20	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 50 µM for Methicillin- resistant S.aureus
1944	18307313	2007	R-Bip-R	CAP 20	2	Acetylation	Y= structure given in paper	Linear	L	Bip	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	0.6	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 10 µM for Methicillin- resistant S.epidermis
1945	18307313	2007	R-X-R	CAP 21	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	116	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for S.aureus
1946	18307313	2007	R-X-R	CAP 21	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	116	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.aureus
1947	18307313	2007	R-X-R	CAP 21	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	116	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.epidermis
1948	18307313	2007	R-X-R	CAP 22	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 11 µM for S.aureus
1949	18307313	2007	R-X-R	CAP 22	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 10 µM for Methicillin- resistant S.aureus
1950	18307313	2007	R-X-R	CAP 22	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 4 µM for Methicillin- resistant S.epidermis
1951	18307313	2007	R-X-R	CAP 23	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	67	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for S.aureus
1952	18307313	2007	R-X-R	CAP 23	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	67	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for Methicillin- resistant S.aureus
1953	18307313	2007	R-X-R	CAP 23	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	67	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.epidermis
1954	18307313	2007	R-X-R	CAP 24	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for S.aureus
1955	18307313	2007	R-X-R	CAP 24	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 25 µM for Methicillin- resistant S.aureus
1956	18307313	2007	R-X-R	CAP 24	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	17	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC= 5 µM for Methicillin- resistant S.epidermis
1957	18307313	2007	R-X-R	CAP 25	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	88	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for S.aureus
1958	18307313	2007	R-X-R	CAP 25	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	88	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.aureus
1959	18307313	2007	R-X-R	CAP 25	2	Free	Amidation	Linear	L	X= structure given in paper	Synthetic peptide	Antimicrobial	Not reported	1 mg/mL	88	Trypsin	RP-HPLC	Trypsin	in vitro	None	None	MIC>100 µM for Methicillin- resistant S.epidermis
1995	19762245	2009	YaGFMPLW	TY005	8	Free	O-[3 €™,5 €™-(CF3 )2 Bzl]	Linear	Mix	None	Synthetic peptide	Analgesic	Not reported	50 µg/ml	24	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
1996	19762245	2009	YaGFMPLW	TY027	8	Free	NH-[3 €™,5 €™-(CF3 )2 Bzl]	Linear	Mix	None	Synthetic peptide dreived from opioid and NK1 pharmacophore	Analgesic	Not reported	50 µg/ml	4.8	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
1997	19762245	2009	YcGFCPLW	TY039	8	Free	NH-[3 €™,5 €™-(CF3 )2 Bzl]	Cyclic (C2-C5)	Mix	None	Synthetic peptide	Analgesic	Not reported	50 µg/ml	>6	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
1998	19762245	2009	YcGFcPLW	TY037	8	Free	NH-[3 €™,5 €™-(CF3 )2 Bzl]	Cyclic (C2-C5)	Mix	None	Synthetic peptide	Analgesic	Not reported	50 µg/ml	4.9	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
1999	19762245	2009	YcGF-Nle-PCW	TY035	8	Free	NH-[3 €™,5 €™-(CF3 )2 Bzl]	Cyclic (C2-C7)	Mix	Nle	Synthetic peptide	Analgesic	Not reported	50 µg/ml	>6	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
2000	19762245	2009	YcGF-Nle-PcW	TY038	8	Free	NH-[3 €™,5 €™-(CF3 )2 Bzl]	Cyclic (C2-C7)	Mix	Nle	Synthetic peptide	Analgesic	Not reported	50 µg/ml	>6	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
2010	16023182	2005	KPSSPPEE	Ã…6	8	Acetylation	Amidation	Linear	L	None	Urokinase plasminogen activator (uPA)	Anti tumor	Not reported	100mg/ml	2	Serine Proteases	HPLC, MS-MS	Human blood plasma	in vitro	None	None	Not available
2041	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	55 µg/kg	2.335 ±1.732	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Men) (Intravenous bolus dose)	in vivo	None	None	Not available
2042	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	55 µg/kg	2.774 ±1.797	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Women) (Intravenous bolus dose)	in vivo	None	None	Not available
2043	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	110 µg/kg	2.301 ±0.857	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Men) (Intravenous bolus dose)	in vivo	None	None	Not available
2044	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	110 µg/kg	2.435 ±0.907	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Women) (Intravenous bolus dose)	in vivo	None	None	Not available
2045	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	220 µg/kg	2.028 ±0.472	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Men) (Intravenous bolus dose)	in vivo	None	None	Not available
2046	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	220 µg/kg	2.931 ±0.971	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Women) (Intravenous bolus dose)	in vivo	None	None	Not available
2047	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	180 Î¼g/kg plus 2.0 Î¼g/min €¢kg	2.824 ±0.219	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Men) (Intravenous bolus followed by a continuous infusion of batifiban injection)	in vivo	None	None	73.19 ±19.15% inhibition of platelet aggregation
2048	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	180 Î¼g/kg plus 2.0 Î¼g/min €¢kg	3.032 ±0.383	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Women) (Intravenous bolus followed by a continuous infusion of batifiban injection)	in vivo	None	None	63.67 ±21.94% inhibition of platelet aggregation
2049	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	220 Î¼g/kg plus 2.5 Î¼g/min €¢kg	2.983 ±0.770	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Men) (Intravenous bolus followed by a continuous infusion of batifiban injection)	in vivo	None	None	82.91 ±3.96% inhibition of platelet aggregation
2050	19224155	2009	N5-(aminoiminomethyl)-N2-(3- mercapto-1-oxopropyl)-L-arginylglycyl-L-Î± -aspartyl-L-Î± -trypotophyl-L-Î± -prolyl-L-Î± -cysteinamide,cyclic(1 †’ 6)-disulfide	Batifiban	6	Free	Free	Cyclic (C1-C6)	L	None	Synthetic peptide	Platelet glycoprotein GP …¡b/ …¢a antagonist	Not reported	220 Î¼g/kg plus 2.5 Î¼g/min €¢kg	3.120 ±0.322	Human blood plasma proteases	HPLC, MS-MS	Human blood plasma (Women) (Intravenous bolus followed by a continuous infusion of batifiban injection)	in vivo	None	None	88.98 ±11.615 inhibition of platelet aggregation
2053	21329733	2011	L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]	Octreotide acetate	8	Free	Free	Cyclic (C2-C7)	Mix	2-hydroxy-1-(hydroxymethyl)	Synthetic analog of Somatostatin	Used for treatment of acromegaly	Not reported	30Î¼g/100Î¼l	52.1	Mouse blood proteases	EIA	Mice blood serum (oral delivery in 0.5% Intravail)	in vivo	None	None	Not mentioned
2054	21329733	2011	L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]	Octreotide acetate	8	Free	Free	Cyclic (C2-C7)	Mix	2-hydroxy-1-(hydroxymethyl)	Synthetic analog of Somatostatin	Used for treatment of acromegaly	Not reported	30Î¼g/100Î¼l	25.8	Mouse blood proteases	EIA	Mice blood serum (oral delivery in 1.5% Intravail)	in vivo	None	None	Not mentioned
2055	21329733	2011	L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]	Octreotide acetate	8	Free	Free	Cyclic (C2-C7)	Mix	2-hydroxy-1-(hydroxymethyl)	Synthetic analog of Somatostatin	Used for treatment of acromegaly	Not reported	30Î¼g/100Î¼l	23.6	Mouse blood proteases	EIA	Mice blood serum (oral delivery in 3.0% Intravail)	in vivo	None	None	Not mentioned
2056	21329733	2011	L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]	Octreotide acetate	8	Free	Free	Cyclic (C2-C7)	Mix	2-hydroxy-1-(hydroxymethyl)	Synthetic analog of Somatostatin	Used for treatment of acromegaly	Not reported	30Î¼g/100Î¼l	1.3	Mouse blood proteases	EIA	Mice blood serum (Subcutaneous injection)	in vivo	None	None	Not mentioned
2062	22934681	2012	YaG-MePhe-G	DAMGO	5	Free	Free	Linear	Mix	Methylation at phenylalanine	Synthetic peptide	Opioid peptide	Not reported	5.0 mg/kg	9.2 ± 2.1	Rat blood proteases	ESI-LC ˆ’MS/MS	Rat blood plasma (Intravenous)	in vivo	None	None	Not mentioned
2063	22934681	2012	YaG-MePhe-G	GSH-PEG liposomal DAMGO	5	Free	Free	Linear	Mix	Methylation at phenylalanine	Synthetic peptide	Enhances and prolongs blood to-brain drug delivery of the opioid peptide DAMGO	Not reported	12.5 mg/kg	417 ± 140	Rat blood proteases	ESI-LC ˆ’MS/MS	Rat blood plasma (Intravenous)	in vivo	None	None	Not mentioned
2080	9067297	1996	YGGFLRRl	E-2078 [N-methyl-Tyr1, N-methyl-Arg7-D-Leu8] Dyn A (1 €“8) ethylamide]	N.A.	Methylation	Ethylamide	Linear	Mix	Methylation on Arg7 and Tyr1	Dynorphin A (1 €“ 8) analog	Analgesic	Not reported	10 mg/kg	44	Monkey blood proteases	MALDI-MS	Rhesus monkey blood plasma (Intravenous)	in vivo	7479294	None	Not available
2083	N.A.	2004	AAGIGILTV	Melan-A27-35	9	Free	Free	Linear	L	None	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	5	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= 4 nM
2184	N.A.	2010	K-Sar-htrGtf	Peptide-B	8	Free	Amidation	Linear	Mix	Sar= sarcosine	Glucagon superfamily Peptide A	Insulinotropic peptide	N.A.	2 mg/ ml	18.6	Not mentioned	LC/MS	plasma	in vitro	None	US20110288003	Not mentioned
2243	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	21.2 ±1.1	Human blood plasma proteases	TLC	Human plasma mixed with drug Thioridazine	in vitro	None	None	Not mentioned
2244	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	19.6 ±1.0	Human blood plasma proteases	TLC	Human plasma mixed with drug Fluphenazine	in vitro	None	None	Not mentioned
2245	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	17.2 ±0.9	Human blood plasma proteases	TLC	Human plasma mixed with drug AS-1397	in vitro	None	None	Not mentioned
2246	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	17.1 ±1.0	Human blood plasma proteases	TLC	Human plasma mixed with drug Promethazine	in vitro	None	None	Not mentioned
2247	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	17.1 ±1.1	Human blood plasma proteases	TLC	Human plasma mixed with drug Chlorpromazine	in vitro	None	None	Not mentioned
2248	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	12.5 ±0.1	Human blood plasma proteases	TLC	Human plasma mixed with drug Methotrimeprazine	in vitro	None	None	Not mentioned
2249	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	12.1 ±0.2	Human blood plasma proteases	TLC	Human plasma mixed with drug Methotrimeprazine	in vitro	None	None	Not mentioned
2250	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	11.9 ±0.2	Human blood plasma proteases	TLC	Human plasma mixed with drug Prochlorperazine	in vitro	None	None	Not mentioned
2251	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	11.4 ±0.3	Human blood plasma proteases	TLC	Human plasma mixed with drug Trifluoperazine	in vitro	None	None	Not mentioned
2252	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	12.4 ±0.3	Human blood plasma proteases	TLC	Human plasma mixed with drug Molindone	in vitro	None	None	Not mentioned
2253	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	12.4 ±0.4	Human blood plasma proteases	TLC	Human plasma mixed with drug Loxapine	in vitro	None	None	Not mentioned
2254	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	12.1 ±0.1	Human blood plasma proteases	TLC	Human plasma mixed with drug Clozapine	in vitro	None	None	Not mentioned
2255	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	11.9 ±0.3	Human blood plasma proteases	TLC	Human plasma mixed with drug Haloperidol	in vitro	None	None	Not mentioned
2256	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	11.9 ±0.4	Human blood plasma proteases	TLC	Human plasma mixed with drug Sulpiride	in vitro	None	None	Not mentioned
2257	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	11.3 ±0.4	Human blood plasma proteases	TLC	Human plasma mixed with drug Thiothixene	in vitro	None	None	Not mentioned
2258	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	31.3 ±0.7	Human blood plasma proteases	TLC	Human plasma mixed with Bacitracin	in vitro	None	None	Not mentioned
2259	12444298	2001	YGGFL	Leucine Enkephalin	5	Free	Free	Linear	L	None	Human brain	Regulation of various physiological and behavioral processes	2, 4, 6, 10, 30, 60 and 90, 180 minutes	10 €“8 M	41.1 ±0.9	Human blood plasma proteases	TLC	Human plasma mixed with Bacitracin	in vitro	None	None	Not mentioned
2260	385880	1979	GG	5-Fluoro-4-(N-succinamoylglycylglycine benzyl ester)-2(1H)-pyrimidone (compound 11)	2	5-Fluoro-4-N-succinamoyl	Benzyl ester-2(1H)-pyrimidone	Linear	L	Conjugation of peptide C terminal carboxyl group with amino group of 5 Fluorocytosine	Synthetic	Anticandidal	Not given	Not mentioned	0.3	Sample cells proteases	Spectrophotometry	Sample cells	in vivo	None	None	5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.62,0.62 and 20 µg/mL respectively.
2261	385880	1979	AL	5-Fluoro-4-(N -succinamoyl-L-alanyl-L-leucine)-2-(1H)-pyrimidone (compound 12)	2	5-Fluoro-4-N-succinamoyl	2-(1H)-pyrimidone	Linear	L	Conjugation of peptide C terminal carboxyl group with amino group of 5 Fluorocytosine	Synthetic	Anticandidal	Not given	Not mentioned	1.7	Sample cells proteases	Spectrophotometry	Sample cells	in vivo	None	None	5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.31,0.31 and 10 µg/mL respectively.
2262	385880	1979	AL	5-Fluoro-4-(N-succinamoyl-L-alanyl-L-leucine benzyl ester)-2(1H)-pyrimidone (compound 9)	2	5-Fluoro-4-N-succinamoyl	Benzyl ester-2(1H)-pyrimidone	Linear	L	Conjugation of peptide C terminal carboxyl group with amino group of 5 Fluorocytosine	Synthetic	Anticandidal	Not given	Not mentioned	1.1	Sample cells proteases	Spectrophotometry	Sample cells	in vivo	None	None	5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.31,0.62 and 20 ug/mL respectively.
2263	385880	1979	LL	5-Fluoro-4-(N -succinamoyl-L-leucyl-L-leucine)-2(1 H)-pyrimidone (compound13)	2	5-Fluoro-4-N-succinamoyl	2-(1H)-pyrimidone	Linear	L	Conjugation of peptide C terminal carboxyl group with amino group of 5 Fluorocytosine	Synthetic	Anticandidal	Not given	Not mentioned	2.9	Sample cells proteases	Spectrophotometry	Sample cells	in vivo	None	None	5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.31,0.31 and 10 µg/mL respectively.
2264	385880	1979	AG	N4-( Boc-Ala-Gly)-5-FC (compound 17)	2	N4- Boc	5-FC (5 Fluorocytosine)	Linear	L	Conjugation of peptide C terminal carboxyl group with amino group of 5 Fluorocytosine	Synthetic	Anticandidal	Not given	Not mentioned	2.3	Sample cells proteases	Spectrophotometry	Sample cells	in vivo	None	None	5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.62, 0.62 and 1.25 ug/mL respectively.
2269	4034413	1985	YGGFL	Leucine enkephalin	5	Free	Free	Linear	L	None	Human brain	Analgesic	20 minutes	0.9 nM	14.7	Human serum protease	HPLC	Human serum	in vitro	None	None	Not reported
2270	4034413	1985	YGGFL	Leucine enkephalin analogue	5	Free	Free	Linear	L	Thiomethylene bond replacement between residue 1-2	Derivative of Natural enkephalin	Analgesic	20 minutes	0.9 nM	94	Human serum protease	HPLC	Human serum	in vitro	None	None	Not reported
2271	4034413	1985	YGGFL	Leucine enkephalin analogue	5	Free	Free	Linear	L	Thiomethylene bond replacement between residue 2-3	Derivative of Natural enkephalin	Analgesic	20 minutes	0.9 nM	79.4	Human serum protease	HPLC	Human serum	in vitro	None	None	Not reported
2272	4034413	1985	YGGFL	Leucine enkephalin analogue	5	Free	Free	Linear	L	Thiomethylene bond replacement between residue 4-5	Derivative of Natural enkephalin	Analgesic	20 minutes	0.9 nM	315	Human serum protease	HPLC	Human serum	in vitro	None	None	Not reported
2273	4034413	1985	YaGFL	Leucine enkephalin analogue	5	Free	Free	Linear	Mix	Thiomethylene bond replacement between residue 3-4	Derivative of Natural enkephalin	Analgesic	20 minutes	0.9 nM	>1000	Human serum protease	HPLC	Human serum	in vitro	None	None	Not reported
2277	6121002	1982	PLG	PLG peptide	3	Free	Free	Linear	L	Tritium labeling at Proline	Hypothalamus and pineal gland	Interact with dopaminergic system and improve patients of parkinson disease	Not given	2 - 2.5 Î¼g	20 (t1/2 elimination)	Rat plasma proteases	Radioimmunoassay	Subcutaneously injected to rat plasma	in vivo	None	None	Radiolabelled peptide was administered in rats and blood plasma was taken and analysed by HPLC. Brain level of radioactivity increased with time.
2284	6291099	1982	WMDF	Cholecystokinin-4 (CCK4)	4	Free	Amidation	Linear	L	None	Deudenum of pig	Intestinal hormone	Not given	50 µM	13	Human plasma proteases	HPLC	Human plasma	in vitro	None	None	Not reported
2285	6291099	1982	WMDF	Cholecystokinin-4 (CCK4)	4	Free	Amidation	Linear	L	None	Deudenum of pig	Intestinal hormone	Not given	50 µM	<1	Rat plasma protease	HPLC	Rat Plasma	in vitro	None	None	Not reported
2286	6291099	1982	YMGWMDF	CCK7 (Cholecystokinin-7)	7	Free	Amidation	Linear	L	None	Deudenum of pig	Intestinal hormone	Not given	50 µM	2.5	Human blood proteases	HPLC	Human plasma	in vitro	None	None	Not reported
2287	6291099	1982	DYMGWMDF	CCK8 (Cholecystokinin-8)	8	Free	Amidation	Linear	L	None	Deudenum of pig	Intestinal hormone	Not given	50 µM	18	Human plasma proteases	HPLC	Human plasma	in vitro	None	None	Not reported
2288	6291099	1982	DYMGWMDF	CCK8 (Cholecystokinin-8)	8	Free	Amidation	Linear	L	Sulphation of Tyrosine residue at position 2	Derivative of natural cholecytokinin	Intestinal hormone	Not given	50 µM	50	Human plasma proteases	HPLC	Human plasma	in vitro	None	None	Not reported
2289	6291099	1982	DYMGWMDF	CCK8 (Cholecystokinin-8)	8	Free	Amidation	Linear	L	None	Deudenum of pig	Intestinal hormone	Not given	50 µM	5	Rat plasma protease	HPLC	Rat Plasma	in vitro	None	None	Not reported
2290	6291099	1982	DYMGWMDF	CCK8 (Cholecystokinin-8)	8	Free	Amidation	Linear	L	Sulphation of Tyrosine residue at position 2	Derivative of natural cholecytokinin	Intestinal hormone	Not given	50 µM	17	Rat plasma protease	HPLC	Rat Plasma	in vitro	None	None	Not reported
2291	6291099	1982	RDYWGWLDF	CCK9 (Cholecystokinin-9)	9	Free	Amidation	Linear	L	Sulphation of Tyrosine residue at position 3	Derivative of natural cholecytokinin	Intestinal hormone	Not given	50 µM	2.7	Human plasma proteases	HPLC	Human plasma	in vitro	None	None	Not reported
2295	6522442	1984	YAFGYPS	Dermorphin	7	Free	Free	Linear	L	I125 radiolabeled	Frog skin	Opiod receptor agonist	60 minute	500 Î¼g/kg	1.3	Rat blood proteases	Radioimmunoassay and HPLC	Intravenous injection into tail of rats	in vivo	http://www.anaspec.com/products/product.asp?id=450	None	Not reported
2323	7418787	1979	CYFQNCPRG	Lysine vasopressin	9	Free	Free	Cyclic (C1-C6)	L	None	Human Pituitary	Regulator of fluid and water balance	Not given	0.2 mg	47.4 (t1/2 of specific radioactivity)	None	Liquid scintillation spectrometer	Weakly acidic solution (pH 4.0, acetic acid)	in vitro	None	None	Not reported
2332	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2, 5, 15, 30, 45, and 60min	0.10mg/kg	1 (t1/2 Î±)	Rat blood plasma proteases	HPLC-MS	Intravenous administered to Rat	in vivo	None	None	Not tested
2333	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min	0.10mg/kg	13 (t1/2 Î±)	Dog blood plasma proteases	HPLC-MS	Intravenous administered to Dog	in vivo	None	None	Not tested
2334	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min	0.10mg/kg	4 (t1/2 Î±)	Rabbit blood plasma proteases	HPLC-MS	Intravenous administered to Rabbit	in vivo	None	None	Not tested
2335	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min	0.10mg/kg	5 (t1/2 Î±)	Monkey blood plasma proteases	HPLC-MS	Intravenous administered to Monkey	in vivo	None	None	Not tested
2336	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2, 5, 15, 30, 45, and 60min	0.10mg/kg	15 (t1/2 Î²)	Rat blood plasma proteases	HPLC-MS	Intravenous administered to Rat	in vivo	None	None	Not tested
2337	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min	0.10mg/kg	64 (t1/2 Î²)	Dog blood plasma proteases	HPLC-MS	Intravenous administered to Dog	in vivo	None	None	Not tested
2338	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min	0.10mg/kg	64 (t1/2 Î²)	Rabbit blood plasma proteases	HPLC-MS	Intravenous administered to Rabbit	in vivo	None	None	Not tested
2339	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min	0.10mg/kg	68 (t1/2 Î²)	Monkey blood plasma proteases	HPLC-MS	Intravenous administered to Monkey	in vivo	None	None	Not tested
2340	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min	5 mg/kg	73 (t1/2 Î²)	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2341	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min	5 mg/kg	45 (t1/2 Î²)	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2342	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min	5 mg/kg	51	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2343	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min	50 mg/kg	80	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2344	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min	300 mg/kg	99	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2345	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min	500 mg/kg	122	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2346	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min	1000 mg/kg	204	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2347	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	1 day	5 mg/kg	51	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2348	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	28 day	5 mg/kg	74	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2349	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	1 day	50 mg/kg	80	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2350	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	28 day	50 mg/kg	71	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2351	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	1 day	300 mg/kg	99	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2352	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	28 day	300 mg/kg	100	Rat blood plasma proteases	HPLC-MS	Orally administered to Rat	in vivo	None	None	Not tested
2353	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	1 day	5 mg/kg	45	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2354	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	28 day	5 mg/kg	44	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2355	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	1 day	50 mg/kg	48	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2356	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	28 day	50 mg/kg	50	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2357	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	1 day	300 mg/kg	75	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2358	8991489	1996	RPD	IRI-695 peptide	3	Acetylation	Isobutyl citrate	Linear	L	C14 Radiolabeling	Synthetic	Anxiolytic and antidepressant	28 day	300 mg/kg	76	Dog blood plasma proteases	HPLC-MS	Orally administered to Dog	in vivo	None	None	Not tested
2359	9062685	1997	pGlu-NC(C)PRG	[pGIu4,Cyt6]AVP(4-9)	6	Free	Amidation	Linear	L	pGlu = pyroglutamate	Human kidney cells	Antidiuretic hormone	5, 10, 30, 60 and 120 min	10 ng/kg	40	Rat blood proteases	HPLC	Subcutaneously injected to rat	in vivo	None	None	Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2360	9062685	1997	NCPR	[Cys6]AVP(5-8)	4	Free	Free	Linear	L	At 2 position cystine is replaced by cysteine	Human kidney cells	Antidiuretic hormone	5, 10, 30, 60 and 120 min	1 ng/kg	10	Rat blood proteases	HPLC	Subcutaneously injected to rat	in vivo	None	None	Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2361	9062685	1997	pGlu-NSPRG	No.302	6	Free	Amidation	Linear	L	pGlu = pyroglutamate	Human kidney cells	Antidiuretic hormone	5, 10, 30, 60 and 120 min	0.1, 1 and 10ng/kg	9	Rat blood proteases	HPLC	Subcutaneously injected to rat	in vivo	None	None	Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2362	9062685	1997	NSPR	Analogue of [Cys6]AVP(5-8)	4	Free	Free	Linear	L	None	Human kidney cells	Antidiuretic hormone	5, 10, 30, 60 and 120 min	10 ng/kg	223	Rat blood proteases	HPLC	Subcutaneously injected to rat	in vivo	None	None	Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2368	9589822	1998	Mpr-Har-GDWPC	Eptifibatide	7	Mpr=mercaptopropionyl	Amidation	Cyclic (disulfide bridge between cysteine and mercaptopropionyl)	L	None	Venom of pygmy rattlesnake	Antithrombotic	1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hours	135 Î¼g/kg	1.13 ±0.17 (t1/2 termination)	Human blood plasma proteases	HPLC	Intravenous injection to Human	in vitro	http://www.prospecbio.com/Eptifibatide_11_124/	None	Not tested
2369	9589822	1998	Mpr-Har-GDWPC	Eptifibatide	7	Mpr=mercaptopropionyl	Amidation	Cyclic (disulfide bridge between cysteine amide and mercaptopropionyl)	L	None	Venom of pygmy rattlesnake	Antithrombotic	1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hours	135 Î¼g/kg	5 ±2.5 (t1/2 distribution)	Human blood plasma proteases	HPLC	Intravenous injection to Human	in vitro	http://www.prospecbio.com/Eptifibatide_11_124/	None	Not tested
2370	9932163	1998	VVVPP	Cemadotin-HCl	5	Free	Free	Linear	L	None	Synthetic analogue of Dolastatin 15	Antimitotic	24 hour	10 - 27.5mg	10	Human blood proteases	Radioimmunoassay	Intravenous administration to human	in vivo	None	None	Cancer patient was administered with Cemadotin for 24 hours intravenously at dose of 10mg. Reduction in liver metastasis was observed by sonographic examination.
2371	10354413	1999	YGG	Thioimreg compound 11	3	Free	Free	Linear	L	Peptide bonds at position 1,2 was replaced by thioamide linkages	Thioanalogue of natural Imreg	Immunostimulant	3.5 hours	Not given	46	Rat blood proteases	HPLC	Rat whole blood	in vitro	None	None	125 mg/kg of 11 resulted in a significant increase in activated T helper cells (CD4+CD45+, 28%, P e 0.048). This is accompanied by a significant reduction in NK cells (20-27%, P e 0.02) at 50 and 100 mg/kg
2372	10354413	1999	YGG	Imreg	3	Free	Free	Linear	L	None	Human leucocyte	Immunostimulant and in clinical trial to treat AIDS	3.5 hours	Not given	<1	Rat blood proteases	HPLC	Rat whole blood	in vitro	None	None	Immunophenotyping assay is performed to study immunological effect like stimulation of NK cells and lymphoproliferative properties. T cell proliferation was observed at even at 100mg/kg
2373	10354413	1999	YGG	Thioimreg compound 8	3	Free	Free	Linear	L	Peptide bonds at position 2,3 was replaced by thioamide linkage	Thioanalogue of natural Imreg	Immunostimulant	3.5 hours	Not given	>180	Rat blood proteases	HPLC	Rat whole blood	in vitro	None	None	A weak in vitro induction of T (PHA) and B (PWM) cell proliferation (1.5 to 2-fold increase) by the thioanalogues
2374	10573295	1999	DPLPEF	Enkephalin	6	Free	Amidation	Linear	L	None	Natural (Human brain)	Analgesic	0, 60, 120, 180, and 300 min	1mM	30	Mouse plasma proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse plasma	in vitro	None	None	Not tested
2375	10573295	1999	DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	None	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse plasma proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse plasma	in vitro	None	None	Not tested
2376	10573295	1999	p-[Cl-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para chlorination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse plasma proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse plasma	in vitro	None	None	Not tested
2377	10573295	1999	p-[Br-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para bromination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse plasma proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse plasma	in vitro	None	None	Not tested
2378	10573295	1999	p-[F-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para florination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse plasma proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse plasma	in vitro	None	None	Not tested
2379	10573295	1999	p-[I-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para iodination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse plasma proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse plasma	in vitro	None	None	Not tested
2380	10573295	1999	DPLPEF	Enkephalin	6	Free	Amidation	Linear	L	None	Natural (Human brain)	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse brain proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse brain proteases	in vitro	None	None	Not tested
2381	10573295	1999	DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Hydroxylation of amino group of Phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse brain proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse brain proteases	in vitro	None	None	Not tested
2382	10573295	1999	p-[Cl-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para chlorination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse brain proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse brain proteases	in vitro	None	None	Not tested
2383	10573295	1999	p-[Br-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para bromination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse brain proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse brain proteases	in vitro	None	None	Not tested
2384	10573295	1999	p-[F-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para florination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse brain proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse brain proteases	in vitro	None	None	Not tested
2385	10573295	1999	p-[I-Phe4]DPLPEF	Enkephalin analog	6	Free	Free	Linear	L	Para iodination of amino group of phenylalanine	Derivative of Natural enkephalin	Analgesic	0, 60, 120, 180, and 300 min	1mM	>300	Mouse brain proteases	HPLC , reverse phase HPLC, Partition coefficient	Mouse brain proteases	in vitro	None	None	Not tested
2413	7911441	2014	FCFWKTCT	Octreotide	8	Free	Free	Cyclic (C2-C7)	L	None	Somatostatin analogue	Growth Hormone Inhibitor	Not mentioned	125 Î¼g/kg	113	Patient blood proteases	Not mentioned	Patients with severe renal impairment	in vivo	None	None	Octreotide considerably inhibits pentagastrin stimulated gastric acid secretion and significantly diminishes exocrine pancreatic function.
2414	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	10 Î¼g/kg	5.9 ±2.5 (t1/2 Î±)	New Zeland female rabbits blood protease	Radioimmunoassay	Intravenous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2415	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	10 Î¼g/kg	106 ±22 (t1/2 Î²)	New Zeland female rabbits blood protease	Radioimmunoassay	Intravenous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2416	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	1 Î¼g/kg	6.6 ±2.7 (t1/2 Î±)	New Zeland female rabbits blood protease	Radioimmunoassay	Subcutaneous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2417	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	1 Î¼g/kg	112 ±41 (t1/2 Î²)	New Zeland female rabbits blood protease	Radioimmunoassay	Subcutaneous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2418	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	10 Î¼g/kg	5.3 ±1.1 (t1/2 Î±)	New Zeland female rabbits blood protease	Radioimmunoassay	Subcutaneous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2419	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	10 Î¼g/kg	103 ±19 (t1/2 Î²)	New Zeland female rabbits blood protease	Radioimmunoassay	Subcutaneous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2420	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	100 Î¼g/kg	7.8 ±2.0 (t1/2 Î±)	New Zeland female rabbits blood protease	Radioimmunoassay	Subcutaneous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2421	9040091	1997	pGlu-HWSYwLRP	Meterelin	9	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid	Gonadotropic cells in the anterior pituitary gland	Behavior influencing hormones	5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an	100 Î¼g/kg	173 ±13 (t1/2 Î²)	New Zeland female rabbits blood protease	Radioimmunoassay	Subcutaneous injected in New Zeland female rabbits	in vivo	None	None	Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2458	7714746	1994	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Opoid	Nociception regulating peptide	Not mentioned	0.10mM, 10 mL	17.7	Aminopeptidases present in nasal mucosa of rat	HPLC	Nasal administration to Male Sprague Dawley derived rats	in vivo	None	None	Not reported
2459	7714746	1994	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Opoid	Nociception regulating peptide	Not mentioned	0.10mM, 10 mL	23.9	Aminopeptidases present in nasal mucosa of rat	HPLC	Nasal administration to Male Sprague Dawley derived rats	in vivo	None	None	Not reported
2460	7714746	1994	DGGFL	Leu-enkephalin analogue	5	Free	Free	Linear	L	None	Opoid	Nociception regulating peptide	Not mentioned	0.10mM, 10 mL	21.2	Aminopeptidases present in nasal mucosa of rat	HPLC	Nasal administration to Male Sprague Dawley derived rats	in vivo	None	None	Not reported
2461	7957536	1994	HwAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	Trp methylated at position 2	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	24 hours	0.5 Î¼g/kg	50	Human serum proteases	Chemiluminescence immunometric assay	Twelve adult male volunteers	in vivo	None	None	Mean ED50 values were 0.50 Î¼g/kg and Emax values were 55.1 Î¼g/kg
2462	7957536	1994	HwAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	Trp methylated at position 2	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	24 hours	1 Î¼g/kg	51	Human serum proteases	Chemiluminescence immunometric assay	Twelve adult male volunteers	in vivo	None	None	Mean ED50 values were 0.50 Î¼g/kg and Emax values were 55.1 Î¼g/kg
2463	7957536	1994	HwAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	Trp methylated at position 2	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	24 hours	2 Î¼g/kg	58	Human serum proteases	Chemiluminescence immunometric assay	Twelve adult male volunteers	in vivo	None	None	Mean ED50 values were 0.50 Î¼g/kg and Emax values were 55.1 Î¼g/kg
2465	7991443	1994	YEPGKSS	C-7 Sorbin	7	Free	Amidation	Linear	L	None	Derived from Sorbin	Electrolyte absorbing peptide	1, 2, 4, 8, 16, and 32 min	200 Î¼g/kg/h	7.5 ±1.5	Rat blood proteases	Radioimmunoassay	Male Sprague-Dawley rats blood	in vivo	None	None	Increases absorption of water and ions
2466	7991443	1994	YEPGKSS	Tritiated C-7 Sorbin	7	Free	Amidation	Linear	L	[2-dehydro-Pro1.5]C is attached and tritiated	Derived from Sorbin	Electrolyte absorbing peptide	1, 2, 4, 8, 16, 32, and 64 min	2.8 MBq	17.9 ±1.5	Rat blood proteases	Radioimmunoassay	Male Sprague-Dawley rats blood	in vivo	None	None	Increases absorption of water and ions
2467	8020889	1994	fCFwKTCT	SMS 201-995 (Somatostatin analog octreotide)	8	Free	Free	Cyclic (C2-C7)	Mix	None	Somatostatin analogue	Growth Hormone Inhibitor	2 hours	2 nmol	1.2 ±0.2 (elimination half life)	Rat plasma proteases	Liquid scintillation counting	Injected into mesenteric veins rat	in vivo	None	None	Peptides bound with high affinity and specificity to rat cortex membranes with pIC50= 9.53 ± 0.07
2468	8020889	1994	fCFwKTCT	N-Î±-(Î±-D-glucosyl(1-4)-1-deoxy-D-fructosyl)-octreotide-SDZ CO-611	8	N-alpha-(alpha-D-glucosyl(1-4)-1-deoxy-D-fructosyl)	Free	Cyclic (C2-C7)	Mix	None	Somatostatin analogue	Growth Hormone Inhibitor	2 hours	2 nmol	1.9 ±0.3 (elimination half life)	Rat plasma proteases	Liquid scintillation counting	Injected into mesenteric veins rat	in vivo	None	None	Peptides bound with high affinity and specificity to rat cortex membranes with pIC50= 9.53 ± 0.08
2473	8082705	1994	EAKSQGGSN	Facteur thymique serique	9	Free	Free	Linear	L	None	Thymic peptide hormone	Thymic hormone used to treat autoimmune disorder	5 minutes	300-500 kBq/kg	02-Mar	Rats blood proteases	Radioimmunoassay	Intravenouly injected in male Wistar rats	in vivo	7011613	None	The basal IRI level at 24 h after alloxan injection was significantly lower in alloxan-treated samples than in controls (12.1 + 5.2 vs. 28.7 + 6.3/zU/ml, P < 0.05)
2475	8289671	1994	fCFwKTCT	Octreotide	8	Free	Free	Cyclic (C2-C7)	Mix	None	Somatostatin	Growth Hormone Inhibitor	60 minutes	30 ng/kg/min	90	Human serum proteases	Not mentioned	Human serum	in vivo	6128648	None	It is a potent and well-tolerated inhibitor of basal and stimulated secretion of endogenous insulin, glucagon, and growth hormone when given intravenous infusion at a rate of 30 ng/ kg/min
2490	8545255	1995	HwAWfK	Hexarelin	6	Free	Free	Linear	Mix	Methylated at position 2 of D-trp	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	0.5, 1, 2, 3, 5, 10, 15, 20, 30,40, 60, 80, 120, 150, 240, and 300 min	1 Î¼g/kg	119.84 ±22.5	Dog blood proteases	Radioimmunoassay	Intravenous injection to male and female dogs	in vivo	None	None	Not reported
2491	8545255	1995	HwAWfK	Hexarelin	6	Free	Free	Linear	Mix	Methylated at position 2 of D-trp	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose.	1 Î¼g/kg	25 ±5.02	Dog blood proteases	Radioimmunoassay	Subcutaneous injection to male and female dogs	in vivo	None	None	Not reported
2492	8545255	1995	HwAWfK	Hexarelin	6	Free	Free	Linear	Mix	Methylated at position 2 of D-trp	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose.	10 Î¼g/kg	33.3 ±8.83	Dog blood proteases	Radioimmunoassay	Subcutaneous injection to male and female dogs	in vivo	None	None	Not reported
2493	8545255	1995	HwAWfK	Hexarelin	6	Free	Free	Linear	Mix	Methylated at position 2 of D-trp	Growth hormone-releasing hormone-6	Growth hormone-releasing peptide	1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose.	100 Î¼g/kg	36.7 ±12.01	Dog blood proteases	Radioimmunoassay	Subcutaneous injection to male and female dogs	in vivo	None	None	Not reported
2506	12489813	2002	RPPGF	Bradykinin	5	Free	Free	Linear	L	None	Kininogen	Vasodilating peptide	Not mentioned	100 ng/ml	15	Rat blood proteases	Radioimmunoassay using new radioionated analogue RPPG(125I)F	Cultured rat aortic smooth muscle cells	in vitro	None	None	Not reported
2513	16302271	2006	GKAFRR	Human Glandular Kallikrein 2 (hK2)-activated thapsigargin prodrug	6	Acetylation	Free	Linear	L	Ligated with potent cytotoxin thapsigargin, L12ADT	Human glandular kallikrein 2 (hK2)	Antitumor peptide	24 hours	6 mg/kg	40	Mice blood proteases	Not mentioned	Balb-C mice	in vivo	None	None	Intratumoral concentrations reached levels comparable to the in vitro IC50 of the prodrug with concentrations of 1.25 mM seen at 1 and 4 hr.
2565	16828890	2006	pGlu-NSPR	NC-1900 (Analogue of arginine vasopressin)	5	Free	Addition of lycinamide	Linear	L	pGlu=pyroglutamic acid	Synthetic analogue of arginine vasopressin	Neuropeptide	0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36 and 48 h	0.55mM	19	Mice blood proteases	HPLC-UV	Subcutaneously and Intravenously injected in mice	in vitro	None	None	Single subcutaneous injection of NC-1900 tended to improve the scopolamine-induced memory deficits, but the effects were far from enough to make the animals €™ memory recover, which suggested that either a higher dose or multi- injections of NC-1900 were needed to promote its effects
2566	16828890	2006	pGlu-NSPR	NC-1900 (Analogue of arginine vasopressin)	5	Free	Addition of lycinamide	Linear	L	conjugated with cationic bovine serum albumin conjugated pegylated nanoparticles (CBSA-NPs), pGlu=pyroglutamic acid	Synthetic analogue of arginine vasopressin	Neuropeptide	0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36 and 48 h	0.55mM	78	Mice blood proteases	HPLC-UV	Subcutaneously and Intravenously injected in mice	in vitro	None	None	The memory impairments were greatly improved, and then to normal when the mice were treated with NC-1900 loaded in CBSA-NPs
2568	8218482	1993	YRGDS	RGD containing peptide	5	Free	Free	Linear	L	None	Extra Cellular Matrix proteins	Antitumor peptide	Not mentioned	0.2 mL	30 (t1/2 first phase)	Mice blood proteases	Radioimmunoassay	Intravenously injected to C57BL6 mice	in vivo	None	None	Less effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface.
2569	8218482	1993	YRGDS	RGD containing peptide	5	Free	Free	Linear	L	None	Extra Cellular Matrix proteins	Antitumor peptide	Not mentioned	0.2 mL	2.7 (t1/2 second phase)	Mice blood proteases	Radioimmunoassay	Intravenously injected to C57BL6 mice	in vivo	None	None	Less effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface.
2570	8218482	1993	YRGDS	RGD containing peptide	5	Free	Free	Linear	L	I125 radiolabeling, covalently attached to an isocyanate-containing poly urethane prepolymer	Extra Cellular Matrix proteins	Antitumor peptide	Not mentioned	0.2 mL	0.5 (t1/2 first phase)	Mice blood proteases	Radioimmunoassay	Intravenously injected to C57BL6 mice	in vivo	None	None	Less effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface.
2571	8218482	1993	YRGDS	RGD containing peptide	5	Free	Free	Linear	L	I125 radiolabeling, covalently attached to an isocyanate-containing poly urethane prepolymer	Extra Cellular Matrix proteins	Antitumor peptide	Not mentioned	0.2 mL	11.3 (t1/2 second phase)	Mice blood proteases	Radioimmunoassay	Intravenously injected to C57BL6 mice	in vivo	None	None	Less effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface.
2573	17258819	2007	CYFQNCPRG	Vasopressin, 8-L-Arginine	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min	15 Î¼Ci (555 kBq)	1.06 ±0.19 (fast phase)	Rat blood proteases	Radioimmunoassay	Female homozygous Brattleboro rats and male Wistar rats	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antidiuretic activity 408 IU/mg
2574	17258819	2007	CYFQNCPRG	Vasopressin, 8-L-Arginine	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min	15 Î¼Ci (555 kBq)	5.96 ±0.58 (slow phase)	Rat blood proteases	Radioimmunoassay	Female homozygous Brattleboro rats and male Wistar rats	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antidiuretic activity 408 IU/mg
2575	17258819	2007	CYFQNCPRG	Vasopressin, 8-L-Arginine	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min	15 Î¼Ci (555 kBq)	1.00 ±0.15 (fast phase)	Rat blood proteases	Radioimmunoassay	Female homozygous Brattleboro rats and male Wistar rats along with OPC-31260	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antidiuretic activity 408 IU/mg
2576	17258819	2007	CYFQNCPRG	Vasopressin, 8-L-Arginine	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min	15 Î¼Ci (555 kBq)	8.90 ±0.37 (slow phase)	Rat blood proteases	Radioimmunoassay	Female homozygous Brattleboro rats and male Wistar rats along with OPC-31261	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antidiuretic activity 408 IU/mg
2577	17684103	2007	CYFQNCPRG	125I-vasopressin	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	1,2 and 3 minutes	50 or 0.4 pmol of vasopressin with 33 kBq	~ 1.5	Mice blood proteases	Radioimmunoassay	Saline treated IRAP+/+ mice	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antiduretic activity
2578	17684103	2007	CYFQNCPRG	125I-vasopressin	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	1,2 and 3 minutes	50 or 0.4 pmol of vasopressin with 33 kBq	1	Mice blood proteases	Radioimmunoassay	Insulin-treated IRAP+/+ mice	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antiduretic activity
2579	17684103	2007	CYFQNCPRG	125I-vasopressin	9	Free	Free	Cyclic (C1-C6)	L	I125 labeling	Human Vasopressin	Anti-diuretic peptide	1,2 and 3 minutes	50 or 0.4 pmol of vasopressin with 33 kBq	3	Mice blood proteases	Radioimmunoassay	Insulin-treated IRAP-/- mice.	in vivo	http://www.polypeptide.com/vasopressin-8-l-arginin	None	antiduretic activity
2580	15828822	2005	GViTRIR	Peptide1	7	Acetylation	N-Ethylmaleimidation	Linear	Mix	None	Second type 1 repeat of thrombospondin-1	Antiangiogenic activity	Not mentioned	5mg/kg	<1	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = >100nM
2581	15828822	2005	Sar-GViTXIRP	Compond 5 (ABT-526)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.2	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2582	15828822	2005	Sar-GViTXIRP	Compond 5 (ABT-526)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	1.2	Mouse plasma proteases	Not mentioned	Mouse plamsa	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2583	15828822	2005	Sar-GViTXIRP	Compond 5 (ABT-526)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.5	Monkey plasma proteases	Not mentioned	Monkey plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2584	15828822	2005	Sar-GViTXIRP	Compond 5 (ABT-526)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.5	Proteases from dog plasma	Not mentioned	Dog plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2585	15828822	2005	Sar-GViT-(Dallo-Ile)-IRP	Compond 6 (ABT-510)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	4th AA is D isoform of allo- Ile, Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.2	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2586	15828822	2005	Sar-GViT-(Dallo-Ile)-IRP	Compond 6 (ABT-510)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	4th AA is D isoform of allo- Ile, Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.15	Mouse plasma proteases	Not mentioned	Mouse plamsa	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2587	15828822	2005	Sar-GViT-(Dallo-Ile)-IRP	Compond 6 (ABT-510)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	4th AA is D isoform of allo- Ile, Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	1.2	Monkey plasma proteases	Not mentioned	Monkey plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2588	15828822	2005	Sar-GViT-(Dallo-Ile)-IRP	Compond 6 (ABT-510)	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	4th AA is D isoform of allo- Ile, Sar- Sarcosine	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.8	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2589	15828822	2005	GViT-(Nva)-IRP	Compund 4	8	Acetylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine, Nva-Norvaline	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.3	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 = 0.07 ± 0.004 nM,
2590	15828822	2005	Sar-GViT-(Nva)-IRP	Compound 7	9	NHIsp	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine , Nva-Norvaline	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.9	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 =29 ± 0.003 nM, Inhibition of HMVEC tube formation with IC50 = >1000nM
2591	15828822	2005	Sar-GViT-(Nva)-IRP	Compound 8	9	Succinylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine ,Nva-norvaline	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.2	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 =0.26 ± 0.110 nM, Inhibition of HMVEC tube formation with IC50 = 10-5nM
2592	15828822	2005	Sar-GViT-(NMeNva)-IRP	Compound 9	9	Acetylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine , NMeNva- N-methyl-norvaline	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	1	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 =0.54 ± 0.150 nM, Inhibition of HMVEC tube formation with IC50 = 50-25nM
2593	15828822	2005	Sar-GViT-NMeNva-IRP	Compound 10	9	Succinylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine , NMeNva- N-methyl-norvaline	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	2.1	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 =0.45 ± 0.110 nM, Inhibition of HMVEC tube formation with IC50 = 10 -5nM
2594	15828822	2005	Sar-GViT-NMeNva-IRP	Compound 11	9	Succinylation	N-Ethylmaleimidation	Linear	Mix	Sar- Sarcosine , NMeNva- N-methyl-norvaline	Synthetic (derived from peptide 1)	Antiangiogenic activity	Not mentioned	5mg/kg	0.3	Rat plasma proteases	Not mentioned	Rat plasma	in vivo	None	None	Inhibition of HMVEC migration with IC50 =0.06 ± 0.030 nM, Inhibition of HMVEC tube formation with IC50 = 0.25- 0.10nM
2606	17408666	2007	ARPYSFGL	Cydiastatin 4	8	Free	Amidation	Linear	L	None	Synthetic	Neuropeptides	30 °C for 20 minutes	1nmol	16.5	M. sexta larval midgut tissue proteases	RP-HPLC	Midgut tissues of M. sexta	in vitro	None	None	Not reported
2607	17408666	2007	ARPYSFGL	Cydiastatin 5	8	Free	Amidation	Linear	L	None	Synthetic	Neuropeptides	30 °C for 20 minutes	1nmol	2.5	M. sexta larval midgut lumen proteases	RP-HPLC	Midgut Lumen of M. sexta	in vitro	None	None	Not reported
2613	17498958	2007	Pyr-HP	Thyrotropin-releasing hormone (TRH)	3	Free	Amidation	Linear	L	Pyr=pyroglutamic acid	Hypothalamus	Stimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland	37 °C for 1-120 minutes	200Î¼M	~3	Homogenate of Caco-2 cells proteases	LC-MS	Homogenate of Caco-2 cells	in vitro	None	None	Not reported
2614	17498958	2007	Pyr-HP	Peptide1 (Thyrotropin-releasing hormone (TRH) analogue)	3	Free	D-glucopyranuronamide	Linear	L	Pyr=pyroglutamic acid	Synthetic derived from TRH	Stimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland	37 °C for 1-120 minutes	200Î¼M	~20	Homogenate of Caco-2 cells proteases	LC-MS	Homogenate of Caco-2 cells	in vitro	None	None	Not reported
2615	17498958	2007	QHP	Peptide2 (Thyrotropin-releasing hormone (TRH) analogue)	3	2-aminooctanoic acid	D-glucopyranuronamide	Linear	L	None	Synthetic derived from TRH	Stimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland	37 °C for 1-120 minutes	200Î¼M	~20	Homogenate of Caco-2 cells proteases	LC-MS	Homogenate of Caco-2 cells	in vitro	None	None	Not reported
2631	18249125	2009	HSSKLQ	Prostate Specific Antigen (Prodrug 2)	6	Mu (Morpholino)	Cyclopamine	Linear	L	None	Synthetic	Prostate-specific antigen (PSA)-activated prodrugs against prostate cancer	0.5-18 hours at room temperature	100 µM	22	PSA enzymes	Hydrolysis and RP-HPLC	NA	in vitro	None	None	Not reported
2632	18249125	2009	SSKYQ	Prostate Specific Antigen (Prodrug 3)	5	Mu (Morpholino)	Cyclopamine	Linear	L	None	Synthetic	Prostate-specific antigen (PSA)-activated prodrugs against prostate cancer	0.5-18 hours at room temperature	100 µM	3.2	PSA enzymes	Hydrolysis and RP-HPLC	NA	in vitro	None	None	Not reported
2663	22186872	2011	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	Room Temperature	1mg/mL	<5	Hydolytic activity of bacterial strain B-9	HPLC and LC/ITMS	Bacterial strain B-9 cell culture	in vitro	None	None	Not reported
2665	22186872	2011	YGGFL	[Leu5]Enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid neuropeptide in neurons of both the central and peripheral nervous system.	Neurotransmitter	Room Temperature	1mg/mL	<5	Hydolytic activity of bacterial strain B-9	HPLC and LC/ITMS	Bacterial strain B-9 cell culture	in vitro	None	None	Not reported
2667	22186872	2011	CYIQNCPLG	Oxytocin	9	Free	Amidation	Cyclic (C1-C6)	L	None	Hypothalamus	Cause contraction of the uterus during labor and intiate milk release from breast	Room Temperature	1mg/mL	1	Hydolytic activity of bacterial strain B-9	HPLC and LC/ITMS	Bacterial strain B-9 cell culture	in vitro	None	None	Not reported
2669	22186872	2011	CYFQNCPRG	Vasopressin	9	Free	Amidation	Cyclic (C1-C6)	L	None	Anti-diuretic hormone secreted by pitutiary gland	Anti-diuretic and regulates retention of water	Room Temperature	1mg/mL	>7	Hydolytic activity of bacterial strain B-9	HPLC and LC/ITMS	Bacterial strain B-9 cell culture	in vitro	None	None	Not reported
2679	23813302	2013	Sar-RVYIHPa	TRV027	8	Sar=Sarcosine	Free	Linear	Mix	D-Ala at 8th position	Synthetic Î²-arrestin-biased agonist	Beta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitment	Not mentioned	0.01 - 20 Î¼g/kg/min dose	<2 (intial half life)	Human plasma proteases	LC/MS/MS	Human plasma	in vivo	None	None	Not reported
2680	23813302	2013	Sar-RVYIHPa	TRV027	8	Sar=Sarcosine	Free	Linear	Mix	D-Ala at 8th position	Synthetic Î²-arrestin-biased agonist	Beta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitment	Not mentioned	0.01 - 20 Î¼g/kg/min dose	~ 10 (Terminal half life)	Human plasma proteases	LC/MS/MS	Human plasma	in vivo	None	None	Not reported
2711	25894376	2015	PLLQATL	P7 (Basic fibroblast growth factor- binding peptide)	7	Free	Free	Linear	L	None	Basic Fibroblast growth factor 2- binding peptide	Anti-proliferative and anti-angiogenic	37 °C for 1-48hours	0.3478Î¼M	1.5	Human plasma proteases	HPLC	Human plasma	in vitro	20414975	None	Not reported
2784	19344673	2009	SCSlPQT	Mouse [D-Leu-4]OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Blood collected after 5-120 minutes after peptide delivery	1mg/200ul	30	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intraperitoneal route of delivery)	in vivo	11495687	None	Not reported
2785	19344673	2009	SCSlPQT	Mouse [D-Leu-4]OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Blood collected after 5-120 minutes after peptide delivery	1mg/200ul	35	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Subcutaneous Route of delivery)	in vivo	11495687	None	Not reported
2786	19344673	2009	SCSlPQT	Mouse [D-Leu-4]OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Blood collected after 5-120 minutes after peptide delivery	1mg/200ul	42	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intra-muscular route of delivery)	in vivo	11495687	None	Not reported
2787	19344673	2009	SCSlPQT	Mouse [D-Leu-4]OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Blood collected after 5-120 minutes after peptide delivery	1mg/200ul	41.1	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intranasal route of delivery)	in vivo	11495687	None	Not reported
2788	19157421	2009	GPE	Glypromate	3	Free	Free	Linear	L	None	N-terminal cleavage product of human insulin-like growth factor-1 (IGF-1) in the brain	Neuroprotective	Blood collected after 0.5-12 hours after peptide delivery	3 -10 mg/kg/h dose	5	Rat plasma proteases	LC-MS	Sprague-Dawley rats plasma (Dose i/v injected)	in vivo	None	None	Not reported
2789	19157421	2009	GPE	NNZ-2566 (Glycyl-L-2-methylprolyl-L- glutamic acid)	3	Free	Free	Linear	L	Methylation of alpha-C of Pro	Glypromate analogue	Neuroprotective	Blood collected after 0.5-12 hours after peptide delivery	3 -10 mg/kg/h dose	49	Rat blood proteases	LC-MS	Sprague-Dawley rats brain (Dose i/v injected)	in vivo	None	None	NNZ-2566-treated animals(i/v) exhibited an average infarct area of 79.8 ±10.4 mm2 (3 mg/kg/h, pb0.01) and 21.3 ±7.5 mm2 (10 mg/kg/h) as compare to ET-1 induced an infarct area of 153.1 ±20.1 mm2 (mean ±s.e.m) in saline-treated rat; Total injury size was 22.2 ±5.7 mm2 following 30 mg/kg (76% protection; Dunnett's multiple comparison test) and only 4.6 ±2.3 mm2 following 60 mg/kg (95% protection; Dunnett's multiple comparison test).
2790	19157421	2009	GPE	NNZ-2566 (Glycyl-L-2-methylprolyl-L- glutamic acid)	3	Free	Free	Linear	L	Methylation of alpha-C of Pro	Glypromate analogue	Neuroprotective	Blood collected after 0.5-12 hours after peptide delivery	3 -10 mg/kg/h dose	74	Rat brain proteases	LC-MS	Sprague-Dawley rats blood (Dose i/v injected)	in vivo	None	None	NNZ-2566-treated animals(i/v) exhibited an average infarct area of 79.8 ±10.4 mm2 (3 mg/kg/h, pb0.01) and 21.3 ±7.5 mm2 (10 mg/kg/h) as compare to ET-1 induced an infarct area of 153.1 ±20.1 mm2 (mean ±s.e.m) in saline-treated rat; Total injury size was 22.2 ±5.7 mm2 following 30 mg/kg (76% protection; Dunnett's multiple comparison test) and only 4.6 ±2.3 mm2 following 60 mg/kg (95% protection; Dunnett's multiple comparison test).
2791	21903490	2011	CRKEVY	cTP6( Cyclic thymic hexapeptide)	6	Free	Free	Cyclic (Amide bond between C1-Y6)	L	None	Synthetic analog of TP5(Thymopentin)	Immunomodulatory drug	Blood collected after 5 minutes-8 hours after peptide delivery	100 µg/ml	2.24 ±0.423	Rhesus monkey plasma proteases	LC-MS	Rhesus monkey plasma	in vivo	None	None	Not reported
2792	21903490	2011	CRKEVY	cTP6( Cyclic thymic hexapeptide)	6	Free	Free	Cyclic (Amide bond between C1-Y6)	L	None	Synthetic analog of TP5(Thymopentin)	Immunomodulatory drug	Blood collected after 5 minutes-8 hours after peptide delivery	200 µg/ml	2.95 ±0.157	Rhesus monkey plasma proteases	LC-MS	Rhesus monkey plasma	in vivo	None	None	Not reported
2793	21903490	2011	CRKEVY	cTP6( Cyclic thymic hexapeptide)	6	Free	Free	Cyclic (Amide bond between C1-Y6)	L	None	Synthetic analog of TP5(Thymopentin)	Immunomodulatory drug	Blood collected after 5 minutes-8 hours after peptide delivery	300 µg/ml	2.56 ±0.27	Rhesus monkey plasma proteases	LC-MS	Rhesus monkey plasma	in vivo	None	None	Not reported
2794	21903490	2011	RKEVY	TP5(Thymopentin)	5	Free	Free	Linear	L	None	Thymopentin	Immunomodulatory drug	Not mentioned	Not mentioned	30	Human plasma proteases	Not mentioned	Human plasma	in vivo	None	None	Not reported
2795	24139844	2013	SKLQ	Conjuagte 1 (conjugates of 4-aminocyclophosphamide (4-NH2-CPA))	4	Succinylation	Amidated CPA	Linear	L	None	Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA)	Anti-cancer	Not mentioned	Not mentioned	6.5	PSA(Prostate-specific antigen )	HPLC	Conjuagte 1+PSA(Prostate-specific antigen)	in vitro	None	None	Not reported
2796	24139844	2013	HSSKLQ	Conjuagte 2(conjugates of 4-aminocyclophosphamide (4-NH2-CPA))	6	Succinylation	Amidated CPA	Linear	L	None	Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA)	Anti-cancer	Not mentioned	Not mentioned	12	PSA(Prostate-specific antigen )	HPLC	Conjuagte 2+PSA(Prostate-specific antigen)	in vitro	None	None	pEC50-8.59 ±0.9minutes, Emax 9.30 ±0.26nmol/well
2797	24139844	2013	Hyp-AS-Chg-Q	Conjuagte 3(conjugates of 4-aminocyclophosphamide (4-NH2-CPA))	5	Bn-glutarylation	Amidated CPA	Linear	L	None	Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA)	Anti-cancer	Not mentioned	Not mentioned	55	PSA(Prostate-specific antigen )	HPLC	Conjuagte 3+PSA(Prostate-specific antigen)	in vitro	None	None	pEC50-8.19 ±1.0minutes, Emax 9.44 ±0.3 nmol/well
2802	25453979	2014	SCSlPQT	MA(D-Leu-4)OB3	7	Myristoylation	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in sterile phosphate buffered saline(PBS, pH 7.2) at a concentration of 0.1 mg	2	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum(Subcutaneous Route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2803	25453979	2014	SCSlPQT	MA(D-Leu-4)OB3	7	Myristoylation	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in sterile phosphate buffered saline(PBS, pH 7.2) at a concentration of 0.1 mg	4.5	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intraperitoneal route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2804	25453979	2014	SCSlPQT	MA(D-Leu-4)OB3	7	Myristoylation	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in sterile phosphate buffered saline(PBS, pH 7.2) at a concentration of 0.1 mg	5.9	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intra-muscular route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2805	25453979	2014	SCSlPQT	MA(D-Leu-4)OB3	7	Myristoylation	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	28.9	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Oral route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2806	25453979	2014	SCSlPQT	MA(D-Leu-4)OB3	7	Myristoylation	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	8.2	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intranasal route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2807	25453979	2014	SCSlPQT	(D-Leu-4)OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	34	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum(Subcutaneous Route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2808	25453979	2014	SCSlPQT	(D-Leu-4)OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	49	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intraperitoneal route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2809	25453979	2014	SCSlPQT	(D-Leu-4)OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	36	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intra-muscular route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2810	25453979	2014	SCSlPQT	(D-Leu-4)OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	20	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Oral route of delivery)	in vivo	None	None	Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2811	25453979	2014	SCSlPQT	(D-Leu-4)OB3	7	Free	Free	Linear	Mix	None	Synthetic peptide amide with leptin-like activity	Regulate energy balance by inhibiting hunger	Not mentioned	Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio	41	Mice serum proteases	Competitive ELISA	Male Swiss Webster mice serum (Intranasal route of delivery)	in vivo	None	None	Stimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS
2822	1329046	1992	D-Nal-QWAVGHLF	[N Psi P]BN(6-14) [Bombesin antagonist]	9	Free	Amidation	Linear	Mix	D-Nal =Napthylalanine	Bombesin analogue	Growth inhibitors	0-1080 minutes	50Î¼M	197	Degradative enzymes or SCLC cell line proteases	RP-HPLC	SCLC cell line NCI-H345	in vitro	None	None	IC50= 5nM, Peptide were added at a 1 Î¼M dose to inhibit growth of SCLC cell line
2823	1329046	1992	fQWAVGHL	[P]BN(6-13)PA [Bombesin antagonist]	8	Free	Propylamidation	Linear	Mix	None	Bombesin analogue	Growth inhibitors	0-360 minutes	50Î¼M	559	Degradative enzymes or SCLC cell line proteases	RP-HPLC	SCLC cell line NCI-H345	in vitro	None	None	IC50= 3nM, Peptide were added at a 1 Î¼M dose to inhibit growth of SCLC cell line
2824	1329046	1992	fQWAVGHL-Cpa	[P Psi C]BN(6-14) [Bombesin antagonist]	9	Free	Amidation	Linear	Mix	Cpa=Chlorophenylalanine	Bombesin analogue	Growth inhibitors	0-360 minutes	50Î¼M	154	Degradative enzymes or SCLC cell line proteases	RP-HPLC	SCLC cell line NCI-H345	in vitro	None	None	IC50= 10nM, Peptide were added at a 1 Î¼M dose to inhibit growth of SCLC cell line
2825	1329046	1992	fQWAVaHL	[FA]BN(6-13)M [Bombesin antagonist]	8	Fluoryl amide	Methy esterification	Linear	Mix	None	Bombesin analogue	Growth inhibitors	0-1080 minutes	50Î¼M	1388	Degradative enzymes or SCLC cell line proteases	RP-HPLC	SCLC cell line NCI-H345	in vitro	None	None	IC50= 9nM, Peptide were added at a 1 Î¼M dose to inhibit growth of SCLC cell line
2844	1730807	1992	HwAWfK	GHRP (Growth Hormone releasing peptide)	6	Free	Amidation	Linear	Mix	None	Growth Hormone releasing peptide	Release growth hormone	Not mentioned	100Î¼g/kg	20	Human serum proteases	Radioimmunoassay	Human serum	in vivo	None	None	GH response elicited by 300 Î¼g/kg on oral administeration of peptide
2845	1763193	1991	aSTTTNYT	Peptide T (Dala1-peptide T-NH2)	8	Free	Amidation	Linear	Mix	None	Synthetic derived from the external envelope protein of HIV IIIB	HIV-entry inhibitor	Not mentioned	Intravenous test dose of 0.033 mg/Kg of peptide T	30-60	AIDS patient plasma proteases	Radioimmunoassay , HPLC	AIDS patient plasma	in vivo	None	None	Not reported
2892	3215483	1988	YGGFM	MET-enkephalin (Methionine-enkephalin)	5	Free	Free	Linear	L	None	Enkephalin	Neurotransmitter	37 °C for 1-180 minutes	300pg (pooled platelet-poor plasma)	12.8	Human plasma proteases	TLC (Thin-layer chromatography)	Human plasma	in vitro	None	None	Not reported
2893	3215483	1988	YGGFL	LEU-enkephalin (Leucine-enkephalin)	5	Free	Free	Linear	L	None	Enkephalin	Neurotransmitter	37 °C for 1-180 minutes	300pg (pooled platelet-poor plasma)	7	Human plasma proteases	TLC (Thin-layer chromatography)	Human plasma	in vitro	None	None	Not reported
2896	3360050	1988	yRGF(4NO2)P	BW443 (Enkephalin Analogue)	5	Free	Amidation	Linear	Mix	4 nitro groups linked to Phenylalanine (phe) at 4th position	Enkephalin analogue	Antinociceptive and antitussive	Blood collected 10 minutes to 8 hours after peptide infusion	0.1-10 µg/kg peptide	2.0 ±0.4	Proteases from Human plasma	Radioimmunoassay	Human plasma	in vivo	None	None	Not reported
2902	3492729	1986	YGGFM	MET-enkephalin (Methionine-enkephalin)	5	Free	Free	Linear	L	None	Enkephalin	Neurotransmitter	Blood collected 5-60 minutes after peptide infused	1-20mM	<2	Proteases from rhesus monkey plasma	RP-HPLC	Rhesus monkey plasma	in vitro	None	None	Not reported
2903	3768731	1986	WAGGDASGE	DSIP (Delta sleep inducing peptide)	9	Free	Free	Linear	L	None	Neuropeptide secreted from hypothamus	Stress reliever, stimulates LH, somatostatin	Blood collected 2-60 minutes after peptide injected	0.1mg/Kg	7.24 ±0.77	Proteases from dog plasma	Radioimmunoassay	Mongrel dog plasma(Dose i/v injected)	in vivo	None	None	Not reported
2904	3768731	1986	AGGDASGE	des-Trp-DSIP	8	Free	Free	Linear	L	None	DSIP analogue	Anticarcinogenic	Blood collected 2-60 minutes after peptide injected	0.1mg/Kg	7.55 ±0.52	Proteases from dog plasma	Radioimmunoassay	Mongrel dog plasma(Dose i/v injected)	in vivo	None	None	Not reported
2905	3768731	1986	WAaGDASGE	D-Ala3-DSIP	9	Free	Free	Linear	Mix	None	DSIP analogue	Anticarcinogenic	Blood collected 2-60 minutes after peptide injected	0.1mg/Kg	8.19 ±0.30	Proteases from dog plasma	Radioimmunoassay	Mongrel dog plasma(Dose i/v injected)	in vivo	None	None	Not reported
2906	3768731	1986	WAGaDASGE	D-Ala4-DSIP	9	Free	Free	Linear	Mix	None	DSIP analogue	Anticarcinogenic	Blood collected 2-60 minutes after peptide injected	0.1mg/Kg	12.9 ±0.83	Proteases from dog plasma	Radioimmunoassay	Mongrel dog plasma(Dose i/v injected)	in vivo	None	None	Not reported
2907	3768731	1986	WAGaDASGE	D-Ala4-DSIP-NH2	9	Free	Amidation	Linear	Mix	None	DSIP analogue	Anticarcinogenic	Blood collected 2-60 minutes after peptide injected	0.1mg/Kg	10.2 ±0.69	Proteases from dog plasma	Radioimmunoassay	Mongrel dog plasma(Dose i/v injected)	in vivo	None	None	Not reported
2916	1777964	1991	APGPR	CLAP(Prpcolipase activation peptide)	5	Free	Free	Linear	L	None	Derived from colipase	Procolipase activation peptide	Room Temperature(25C)	500nM/L	5	Proteases from Human serum	ELISA	Human Serum	in vitro	None	None	Not reported
2917	1777964	1991	APGPR	CLAP(Prpcolipase activation peptide)	5	Free	Free	Linear	L	None	Derived from colipase	Procolipase activation peptide	Room Temperature(25C)	0.5 µM	4	Proteases from Human urine	ELISA	Human urine	in vitro	None	None	Not reported
2941	2498387	1989	p-Glu-HWSYsLRP	Buserelin	9	Free	Ethylamide	Linear	Mix	D-Ser(tBu) at 6th position, Pglu=pyr- Glutamate	Analogue of LHRH (Luteinizing hormone-releasing hormone)	Stimulates release of LH, FSH and estradiol	Blood collected 0-6 hours after peptide injection	500 µg/kg	11.2 (elimination t1/2 after 10-60 min of i/v injection)	Proteases from serum of women with endometriosis	Radioimmunoassay, HPLC	(Dose i/v injected)Serum of women with endometriosis	in vivo	None	None	Serum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values
2942	2498387	1989	p-Glu-HWSYsLRP	Buserelin	9	Free	Ethylamide	Linear	Mix	D-Ser(tBu) at 6th position	Analogue of LHRH (Luteinizing hormone-releasing hormone)	Stimulates release of LH, FSH and estradiol	Blood collected 0-6 hours after peptide injection	500 µg/kg	50.4 (elimination t1/2 after 60-120 mins of i/v injection)	Proteases from serum of women with endometriosis	Radioimmunoassay, HPLC	(Dose i/v injected)Serum of women with endometriosis	in vivo	None	None	Serum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values
2943	2498387	1989	p-Glu-HWSYsLRP	Buserelin	9	Free	Ethylamide	Linear	Mix	D-Ser(tBu) at 6th position	Analogue of LHRH (Luteinizing hormone-releasing hormone)	Stimulates release of LH, FSH and estradiol	Blood collected 0-6 hours after peptide injection	500 µg/kg	82.7 (elimination t1/2 after 120-360 mins of i/v injection)	Proteases from serum of women with endometriosis	Radioimmunoassay, HPLC	(Dose i/v injected)Serum of women with endometriosis	in vivo	None	None	Serum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values
2944	2521208	1989	CYFQNCPRG	VP (Vasopressin)	9	Free	Amidation	Cyclic (C1-C6)	L	None	Anti-diuretic hormone secreted by pitutiary gland	Anti-diuretic and regulates retention of water	Not mentioned	500 µg/kg	80 (elimination t1/2 after 6-24h of i/v injection)	Proteases from urine of women with endometriosis	Radioimmunoassay, HPLC	(Dose i/v injected)urine of women with endometriosis	in vivo	None	None	Not mentioned
2945	2521208	1989	CYFQNCPRG	VP (Vasopressin)	9	Free	Amidation	Cyclic (C1-C6)	L	None	Anti-diuretic hormone secreted by pitutiary gland	Anti-diuretic and regulates retention of water	Not mentioned	Exogenously administered	0.9(fast component)	Proteases from Rabbit plasma	Radioimmunoassay	Rabbit plasma	in vivo	None	None	Not mentioned
2946	2521208	1989	CYFQNCPRG	VP (Vasopressin)	9	Free	Amidation	Cyclic (C1-C6)	L	None	Anti-diuretic hormone secreted by pitutiary gland	Anti-diuretic and regulates retention of water	Not mentioned	Exogenously administered	5.4(lower phase)	Proteases from Rabbit plasma	Radioimmunoassay	Rabbit plasma	in vivo	None	None	Not mentioned
2947	2521208	1989	CYFQNCPRG	VP (Vasopressin)	9	Free	Amidation	Cyclic (C1-C6)	L	None	Anti-diuretic hormone secreted by pitutiary gland	Anti-diuretic and regulates retention of water	Not mentioned	Endogenously administered	1.3	Proteases from Rabbit plasma	Radioimmunoassay	Rabbit plasma	in vivo	None	None	Not mentioned
2950	2687064	1989	fCFwKTCT	Sandostatinor SMS 201-995	8	Free	OL	Cyclic (C2-C7)	Mix	None	Analogue of somatostatin	Inhibitor of Growth hormone secretion	Blood collected 12hours after peptide injection	50 µg	144 ±15	Proteases from Human plasma (type 1 diabetic patients)	Radioimmunoassay	(Dose s/c injected)Human plasma (type 1diabetic patients)	in vivo	None	None	Plasma glucagon and growth hormone levels were significantly reduced after SMS 201-995
2979	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	0.75	Proteases from Human serum	HPLC	Human serum	in vitro	None	None	Not reported
2980	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	1.3	Proteases from Human plasma	HPLC	Human plasma	in vitro	None	None	Not reported
2981	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	1.7	Proteases from Human blood	HPLC	Human blood	in vitro	None	None	Not reported
2982	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	0.5	Proteases from Horse serum	HPLC	Horse serum	in vitro	None	None	Not reported
2983	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	3.5	Proteases from Fetal calf serum	HPLC	Fetal calf serum	in vitro	None	None	Not reported
2984	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	1.75	Proteases from Heat inactivated calf serum	HPLC	Heat inactivated calf serum	in vitro	None	None	Not reported
2985	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	4	Proteases from Mouse serum	HPLC	Mouse serum	in vitro	None	None	Not reported
2986	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	7	Proteases from Human serum	HPLC	Human serum + 1Î¼M catropril	in vitro	None	None	Not reported
2987	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	5.5	Proteases from Horse serum	HPLC	Horse serum	in vitro	None	None	Not reported
2988	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	18	Proteases from Fetal calf serum	HPLC	Fetal calf serum + 1Î¼M catropril	in vitro	None	None	Not reported
2989	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	11.5	Proteases from Heat inactivated calf serum	HPLC	Heat inactivated calf serum + 1Î¼M catropril	in vitro	None	None	Not reported
2990	8217216	1993	SDKP	AcSDKP (Acetyl-SDKP)	4	Acetylation	Free	Linear	L	None	Isolated from fetal calf bone marrow	Natural hemoregulatory	37 °C for 24 hours	4 X lO-7M, 10 µCi	6	Proteases from Mouse serum	HPLC	Mouse serum + 1Î¼M catropril	in vitro	None	None	Not reported
2991	8218482	1993	YRGDS	Pentapeptide	5	Free	Free	Linear	L	None	Synthetic RGD containing peptide	Cell attachment property	Not mentioned	Not mentioned	30 (Half life of 1st phase)	Proteases from mouse bood	HPLC	Mouse blood	in vivo	None	None	Not reported
2992	8218482	1993	YRGDS	Pentapeptide	5	Free	Free	Linear	L	None	Synthetic RGD containing peptide	Cell attachment property	Not mentioned	Not mentioned	2.7 (Half life of 2nd phase)	Proteases from mouse bood	HPLC	Mouse blood	in vivo	None	None	Not reported
2993	8218482	1993	YRGDS	YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer)	5	Free	Free	Linear	L	Peptide covalently attached to Isocyanate containing polyurethane prepolymer	Synthetic RGD containing peptide	Cell attachment property	Not mentioned	Not mentioned	0.5 (Half life of 1st phase)	Proteases from mouse bood	HPLC	Mouse blood	in vivo	None	None	Not reported
2994	8218482	1993	YRGDS	YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer)	5	Free	Free	Linear	L	Peptide covalently attached to Isocyanate containing polyurethane prepolymer	Synthetic RGD containing peptide	Cell attachment property	Not mentioned	Not mentioned	11.3(Half life of 2nd phase)	Proteases from mouse bood	HPLC	Mouse blood	in vivo	None	None	Not reported
2995	8218482	1993	YRGDS	125I-YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer)	5	Free	Free	Linear	L	Peptide covalently attached to Isocyanate containing polyurethane prepolymer	Synthetic RGD containing peptide	Cell attachment property	Not mentioned	Not mentioned	7	Proteases from mouse bood	HPLC	Mouse blood	in vivo	None	None	Not reported
2996	8289671	1994	fCFwKTCT	Octreotide	8	Free	Free	Cyclic (C2-C7)	Mix	None	Somatostatin analogue	Inhibitor of growth hormone secretion	Blood sample collected after 15-60 minutes	500 µg/ml	90	Proteases from Human plasma	Not mentioned	Human plasma	in vivo	None	None	30ng/kg/min of peptide suppress C-peptide, Insulin, glucagon and growth hormone conc. Below basal level in islet cell clamp study
3009	8545255	1995	HwAWfK	Hexarelin	6	Free	Amidation	Linear	Mix	None	GHRH analogue	Stimulates growth hormone release	Blood sample collected after 0.5-300 minutes	1 µg/kg	120	Proteases from dog plasma	Radioimmunoassay	(Dose i/v injected)Dog plasma	in vivo	None	None	Not reported
3016	8395230	1993	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	37 °C for 15-60 minutes	10 µg/L of peptide	29 ±1	Neutral endopeptides in Human umbilical vein endothelial cells	Radioimmunoassay	Human umbilical vein endithelial cells	in vitro	None	None	Not reported
3017	8395230	1993	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	37 °C for 15-240 minutes	10 µg/L of peptide	244 ±20	Neutral endopeptides in Human umbilical vein endothelial cells	Radioimmunoassay	Human umbilical vein endithelial cells+ Lisinopril	in vitro	None	None	Not reported
3018	8395230	1993	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	37 °C for 15-60 minutes	10 µg/L of peptide	46 ±2	Neutral endopeptides in Human umbilical vein endothelial cells	Radioimmunoassay	Human umbilical vein endithelial cells+ phosphoramidon	in vitro	None	None	Not reported
3019	8395230	1993	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	37 °C for 15-240 minutes	10 µg/L of peptide	381 ±51	Neutral endopeptides in Human umbilical vein endothelial cells	Radioimmunoassay	Human umbilical vein endithelial cells + Lisinopril +phosphoramidon	in vitro	None	None	Not reported
3020	8395230	1993	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	37 °C for 15-240 minutes	10 µg/L of peptide	386 ±52	Neutral endopeptides in Human umbilical vein endothelial cells	Radioimmunoassay	Human umbilical vein endithelial cells+ Lisinopril +phosphoramidon+amastatin	in vitro	None	None	Not reported
3021	8395230	1993	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Endogenous peptide of kinin family	Vasodilator, Inflammatory mediator	37 °C for 15-240 minutes	10 µg/L of peptide	257 ±22	Neutral endopeptides in Human umbilical vein endothelial cells	Radioimmunoassay	Human umbilical vein endithelial cells + Lisinopril +phosphoramidon+amastain + DL-2-mercaptomethyl- 3-guanidinoethyl thiopropionic acid	in vitro	None	None	Not reported
3030	2991517	1985	(Cbc)KFAP	Compound 16 (Ketomethylene pentapeptide analogue)	4	Cbc=Cyclobutanecarboxylic acid	Free	Linear	L	Proline ring is tritiated	Pentapeptide analogue of the ketomethylene-containing angiotensin converting enzyme (ACE) inhibitor	Angiotensin converting enzyme (ACE) inhibitor and anti-hypertensive	Not mentioned	2mg	24.4	Proteases from rat blood	Liquid scintillation spectrometer	(Dose i/v injected) Rat blood	in vivo	None	None	Potent ACE-inhibitor with I50 =7.0nM
3031	2991517	1985	5(S)-benzamido-4-oxo-6-phenylhexanoyl-P	Compound 1 (Ketomethylene pentapeptide analogue)	1	5(S)-benzamido-4-oxo-6-phenylhexanoyl	Free	Linear	L	Proline ring is tritiated	Pentapeptide analogue of the ketomethylene-containing angiotensin converting enzyme (ACE) inhibitor	Angiotensin converting enzyme (ACE) inhibitor and anti-hypertensive	Not mentioned	2mg	11.6	Proteases from rat blood	Liquid scintillation spectrometer	(Dose i/v injected) Rat blood	in vivo	None	None	Potent ACE-inhibitor with I50 =70nM
3039	2624887	1989	pyr-Glu-LTFTPNW	CC-2 (Corpora cardiaca)	8	Free	Amidation	Linear	L	pyr-Glu= Pyro-Glutamic acid	Hypertrehalosaemic hormone in cockroaches	Activate fat body glycogen phosphorylase and increase haemolymph trehalose	2 hours	1-2pmol	13.2	Proteases from Haemolymph of american cockroach	Not mentioned	Haemolymph of american cockroach	in vivo	None	None	Increase in carbohydrates in haemolymph; simulates activation of glycogen phosphorylase and induction of trehalose synthesis
3075	12083977	2002	PHWSYlLRP	Leuprorelin	9	5-oxo	Ethylacetate	Linear	Mix	None	Synthetic agonist analogue of gonadotropin-releasing hormone	Suppression of gonadal steroid synthesis, resulting in pharmacological castration	Not mentioned	100Î¼g/kg	8.4 ±4(t1/2Î±)	Diestrous female rats blood proteases	Radioimmunoassay	Intravenous injection in diestrous female rats	in vivo	None	None	Not mentioned
3076	12083977	2002	PHWSYlLRP	Leuprorelin	9	5-oxo	Ethylacetate	Linear	Mix	None	Synthetic agonist analogue of gonadotropin-releasing hormone	Suppression of gonadal steroid synthesis, resulting in pharmacological castration	Not mentioned	100Î¼g/kg	33.2 ±6.8(t1/2Î²)	Diestrous female rats blood proteases	Radioimmunoassay	Intravenous injection in diestrous female rats	in vivo	None	None	Not mentioned
3077	12083977	2002	PHWSYlLRP	Leuprorelin	9	5-oxo	Ethylacetate	Linear	Mix	None	Synthetic agonist analogue of gonadotropin-releasing hormone	Suppression of gonadal steroid synthesis, resulting in pharmacological castration	Not mentioned	1mg	2.9 ±60.5(t1/2Î²)	Diestrous female rats blood proteases	Radioimmunoassay	Intravenous injection in 6 healthy humans serum	in vivo	None	None	Not mentioned
3078	12083977	2002	PHWSYlLRP	Leuprorelin	9	5-oxo	Ethylacetate	Linear	Mix	None	Synthetic agonist analogue of gonadotropin-releasing hormone	Suppression of gonadal steroid synthesis, resulting in pharmacological castration	Not mentioned	1mg	3.6 ±1.2(t1/2Î²)	Diestrous female rats blood proteases	Radioimmunoassay	Subcutaneous injection in 6 healthy humans serum	in vivo	None	None	Not mentioned
3079	12083977	2002	PHWSYlLRP	Leuprorelin	9	5-oxo	Ethylacetate	Linear	Mix	None	Synthetic agonist analogue of gonadotropin-releasing hormone	Suppression of gonadal steroid synthesis, resulting in pharmacological castration	Not mentioned	10 µg	32(t1/2Î²)	Pregnant female rats blood proteases	Radioimmunoassay	Subcutaneous injection in pregnant rats	in vivo	3083092	None	Not mentioned
3081	15452596	2004	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid ligand	Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.	Not mentioned	Not mentioned	2.17 ±0.05	Enkephalin-degrading enzymes present in blood serum	Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography	Breast fed healthy infants(0-1years)serum sample	in vivo	O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et	None	Not mentioned
3082	15452596	2004	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid ligand	Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.	Not mentioned	Not mentioned	2.48 ±0.007	Enkephalin-degrading enzymes present in blood serum	Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography	Formula fed healthy infants(0-1years)serum sample	in vivo	O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et	None	Not mentioned
3083	15452596	2004	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid ligand	Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.	Not mentioned	Not mentioned	2.26 ±0.06	Enkephalin-degrading enzymes present in blood serum	Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography	Serum sample of healthy infant boys(0-1 years)	in vivo	O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et	None	Not mentioned
3084	15452596	2004	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid ligand	Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.	Not mentioned	Not mentioned	2.51 ±0.08	Enkephalin-degrading enzymes present in blood serum	Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography	Serum sample of healthy infant girls(0-1 years)	in vivo	O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et	None	Not mentioned
3085	15452596	2004	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid ligand	Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.	Not mentioned	Not mentioned	2.37 ±0.05	Enkephalin-degrading enzymes present in blood serum	Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography	Serum sample of children(0-1 years)	in vivo	O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et	None	Not mentioned
3086	15452596	2004	YGGFL	Leu-enkephalin	5	Free	Free	Linear	L	None	Endogenous opioid ligand	Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.	Not mentioned	Not mentioned	3.10 ±0.05	Enkephalin-degrading enzymes present in blood serum	Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography	Serum sample of adults	in vivo	O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et	None	Not mentioned
3093	19023544	2008	RKDVY	TP5 (Thymopentin)	5	Free	Free	Linear	L	None	Synthetic peptide of thymic hormone	Immunomodulator	Not mentioned	Not mentioned	5.6 ±0.7	Rabbit plasma proteases	HPLC	heparinized rabbit plasma	in vitro	http://www.drugbank.ca/drugs/DB00112	None	IL2 concentration in mouse serum:0.65pg/ml,macrophage clearance index(K value)=0.0132 ±0.0008,phagocytic index(Î± value=3.43 ±0.29.
3119	21036718	2010	QWAVGHLM	177Lu-AMBA	9	177Lu,DO3A-CH2CO-G-(4-aminobenzoyl)	Amidation	Linear	L	None	Synthetic Bombesin like peptide	Clinical trials for use as systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients.	Not mentioned	10Î¼g/mouse	0.52 ±0.05(t1/2Î±)	Mice plasma proteases	Radio-HPLC	Intravenous injection in PC-3M-luc-C6 tumour-bearing mice	in vivo	http://www.drugbank.ca/drugs/DB00138	None	In vitro stability =24.3 ±21.9% after 48 hours
3120	21036718	2010	QWAVGHLM	177Lu-AMBA	9	177Lu,DO3A-CH2CO-G-(4-aminobenzoyl)	Amidation	Linear	L	None	Synthetic Bombesin like peptide	Clinical trials for use as systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients.	Not mentioned	10Î¼g/mouse	26.6 ±11.7(t1/2Î²)	Mice plasma proteases	Radio-HPLC	Intravenous injection in PC-3M-luc-C6 tumour-bearing mice	in vivo	http://www.drugbank.ca/drugs/DB00139	None	In vitro stability =24.3 ±21.9% after 48 hours
3123	21986100	2011	YaGFlC	DALCE [(D-Ala2, Leu5, Cys6)-enkephalin]	6	Free	Free	Linear	Mix	None	Enkephalin derative	Treatment of ischemia	Not mentioned	1mg/Kg	9.1 ±2.4	Rats plasma proteases	LC-MS	Intravenous injection in male Sprague €“Dawley rats	in vivo	http://www.drugbank.ca/drugs/DB00142	None	Not mentioned
3124	21986100	2011	YaGFl	DADLE [(D-Ala2, Leu5)-enkephalin]	5	Free	Free	Linear	Mix	None	Opoid peptide	Neuromodulator	Not mentioned	1mg/Kg(200-250Î¼l)	4.6	Rats plasma proteases	HPLC with tandem LC/MS/MS	Rat plasma	in vivo	http://www.drugbank.ca/drugs/DB00143	None	Not mentioned
3125	21986100	2011	YaGFlC	CMD-Cys-DALCE	6	Free	Thiolated carboxymethyl dextran(CMD) cysteine conjugated via disulfide bond	Linear	Mix	None	Enkephalin derative	Treatment of ischemia	Not mentioned	4.5 mg/kg corresponding to 1 mg/kg of DALCE	56 ±6.0	Rats plasma proteases	LC-MS	Intravenous injection in male Sprague €“Dawley rats	in vivo	http://www.drugbank.ca/drugs/DB00144	None	Not mentioned
3154	23099431	2012	HwAWfK	GHRP-6 (Growth Hormone-Releasing Peptide-6)	6	Free	Amidation	Linear	Mix	None	Synthetic molecule structurally related to Met-enkephalin	Cytoprotective,antioxidant in nature	Not mentioned	100 Î¼g/kg of the body weight	0.14 ±0.03(t1/2Î±)	human plasma proteases	LC-MS	Intravenous bolus administartion in 9 healthy male subjects	in vivo	http://www.drugbank.ca/drugs/DB00173	None	Not mentioned
3155	23099431	2012	HwAWfK	GHRP-6 (Growth Hormone-Releasing Peptide-6)	7	Free	Amidation	Linear	Mix	None	Synthetic molecule structurally related to Met-enkephalin	Cytoprotective,antioxidant in nature	Not mentioned	100 Î¼g/kg of the body weight	2.96 ±1.12(t1/2Î²)	human plasma proteases	LC-MS	Intravenous bolus administartion in 9 healthy male subjects	in vivo	http://www.drugbank.ca/drugs/DB00174	None	Not mentioned
3156	23099431	2012	HwAWfK	GHRP-6 (Growth Hormone-Releasing Peptide-6)	8	Free	Amidation	Linear	Mix	None	Synthetic molecule structurally related to Met-enkephalin	Cytoprotective,antioxidant in nature	Not mentioned	200 Î¼g/kg of the body weight	0.15 ±0.06(t1/2Î±)	human plasma proteases	LC-MS	Intravenous bolus administartion in 9 healthy male subjects	in vivo	http://www.drugbank.ca/drugs/DB00175	None	Not mentioned
3157	23099431	2012	HwAWfK	GHRP-6 (Growth Hormone-Releasing Peptide-6)	9	Free	Amidation	Linear	Mix	None	Synthetic molecule structurally related to Met-enkephalin	Cytoprotective,antioxidant in nature	Not mentioned	200 Î¼g/kg of the body weight	3.27 ±2.07(t1/2Î²)	human plasma proteases	LC-MS	Intravenous bolus administartion in 9 healthy male subjects	in vivo	http://www.drugbank.ca/drugs/DB00176	None	Not mentioned
3171	7899230	1994	YGGFL	Leucine enkephalin	5	Free	Free	Linear	L	None	Leucine enkephalin	Opioid peptide	Not reported	0.63 mg/ml	40	Sheep nasal wash fluid proteases	HPLC	Sheep nasal wash fluid	in vitro	http://www.drugbank.ca/drugs/DB00190	None	Not reported
3172	7899230	1994	YGGFL	Leucine enkephalin	5	Free	Free	Linear	L	None	Leucine enkephalin	Opioid peptide	Not reported	20 µg/ml	12	Sheep nasal mucosal proteases	HPLC	Sheep nasal mucosal tissue homogenate	in vitro	http://www.drugbank.ca/drugs/DB00191	None	Not reported
3173	7899230	1994	GGFL	des-tyrosine leucine enkephalin	4	Free	Free	Linear	L	None	des-tyrosine leucine enkephalin	Opioid peptide	Not reported	0.63 mg/ml	13	Sheep nasal wash fluid proteases	HPLC	Sheep nasal wash fluid	in vitro	http://www.drugbank.ca/drugs/DB00192	None	Not reported
3174	7899230	1994	GGFL	des-tyrosine leucine enkephalin	4	Free	Free	Linear	L	None	des-tyrosine leucine enkephalin	Opioid peptide	Not reported	20 µg/ml	7	Sheep nasal mucosal proteases	HPLC	Sheep nasal mucosal tissue homogenate	in vitro	http://www.drugbank.ca/drugs/DB00193	None	Not reported
3177	8082705	1994	EAKSQGGSN	Facteur thymique serique (FTS)	9	Free	Free	Linear	L	None	Thymic peptide hormone	Suppressed hyperglycemia	Not reported	Not reported	2 to 3	Rats blood proteases	Radioimmunoassay	Intravenouly injected in male Wistar rats	in vivo	http://www.drugbank.ca/drugs/DB00196	None	Plasma glucose in FTS-treated group=15.7 ± 1.8 (mmol/l)while in control Plasma glucose=28.3 ±2.1 ( µmol/l)
3179	8035644	1994	GCRFGTCT	ADM 15-22	8	Free	Free	Linear	L	None	Carboxy terminal 15-52 fragment of adrenomedullin	An inhibitor of the cellular actions of adrenomedullin	Not reported	Intraarterial doses of 0.01-0.3 nmol	55 to 80	Cat blood proteases	HPLC	Hind limb vascular bed of the cat	in vivo	http://www.drugbank.ca/drugs/DB00198	None	Not reported
3180	8035644	1994	RPPGFSPFR	Bradykinin	9	Free	Free	Linear	L	None	Not mentioned	A potent endothelium-dependent vasodilator which leads to drop in blood pressure	Not reported	Intraarterial doses of 0.01-0.3 nmol	20 to 45	Cat blood proteases	HPLC	Hind limb vascular bed of the cat	in vivo	http://www.drugbank.ca/drugs/DB00199	None	Not reported
4019	38737283	2024	LAEAKVLANRELDKYGVSDFYKRLINKAKTVEGVEALKLHILAALP-FRRG-(E5C3)-(GN)	ABD035-immunoGN	N.A.	P1h3	His-tag	Linear	L	Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N	Synthetic	Antitumor	Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min	0.1 μmol/kg	35.22	BALB/c mice serum protease	ELISA	BALB/c mice serum	In Vivo	None	None	Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation
4020	38737283	2024	FRRG-(E5C3)-(GN)	immunoGN	N.A.	P1h3	His-tag	Linear	L	Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N	Synthetic	Antitumor	Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min	0.1 μmol/kg	4.599	BALB/c mice serum protease	ELISA	BALB/c mice serum	In Vivo	None	None	Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation
4021	38737283	2024	DIQMTQSPSSLSAVGDRVTITCRASQSISSYLNWYQQKPGKAPKLLIYRNSPLQSGVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQTYRVPPTFGQGTKVEIKR-FRRG-(E5C3)-(GN)	dAb7h8-immunoGN	N.A.	P1h3	His-tag	Linear	L	Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N	Synthetic	Antitumor	Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min	0.1 μmol/kg	31.25	BALB/c mice serum protease	ELISA	BALB/c mice serum	In Vivo	None	None	Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation
4030	38642503	2024	VPALR	VPALR-SUL	5	Free	Sul = Sulpiride	Linear	L	None	Derived from the Ku70 domain	Antidepressant	Blood samples were collected from the orbital venous plexus at various time points (5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 5 h, 7 h, 9 h, 12 h, 24 h	Equivalent of 3 mg/kg of sulpiride	17.49 ± 13.50	Male SD rats plasma protease	LC-MS/MS	Male SD rats plasma	In Vivo	None	None	VPALR-SUL showed almost 100% cell viability at all tested concentrations, which indicates excellent biocompatibility with HT22 nerve cells and minimal cytotoxicity
4031	38613996	2024	AGILKRW	PepH3	7	Free	Amidation	Linear	L	None	Synthetic	Anticancer	At different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C	1 mM	21.00 ± 2.91	Human serum protease	RP-HPLC	Human serum	In Vitro	None	None	IC50 > 100.0 for TNBC MDA-MB-231 Monolayer
4048	38399408	2024	N.A.	BI-X	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment Of Human Ocular Disease	serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals.	0.25 mg/eye	3	Cynomolgus Monkeys Plasma Protease	Immunocapture-LC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Affinity binding site to human albumin (KD = 1.4 nM)
4049	38399408	2024	N.A.	BI-X	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment Of Human Ocular Disease	serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals.	0.25 mg/eye	13.2	Cynomolgus Monkeys Plasma Protease	Immunocapture-LC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Affinity binding site to human albumin (KD = 1.4 nM)
4050	38399408	2024	N.A.	BI-X	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment Of Human Ocular Disease	serial blood samples were taken in EDTA anticoagulant pre-dose and at 1 h, 2 h, 4 h, 24 h, 48 h, 72 h, 96 h, and 168 h and 2, 4, 6, 8, and 10 weeks after dosing or until the last in-life timepoint of the animals.	0.25 mg/eye	11.8	Cynomolgus Monkeys Plasma Protease	Immunocapture-LC-MS/MS	Cynomolgus monkeys plasma	In Vivo	None	None	Affinity binding site to human albumin (KD = 1.4 nM)
4057	38312052	2024	KXCRGDCFCX	Maraciclatide (99mTc)	7	Acetylation	Free	Cyclic(Ac-Cys8 Bond, Cys2-Cys6 Disulfide Bond)	L	Radiolabelled with technetium, X= Unknown Structure	synthetic	Novel Diagnostic Imaging Agent For A Range Of Pathological Conditions	Blood and plasma samples were collected at 10 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, and 7 days post-administration	The data acquired from all participants who received 99mTc-maraciclatide within the expected clinical range (15, 75 µg, 150) were pooled	1 (Terminal Elimination Half Life)	Human Plasma Protease	Gamma counter	Human plasma	In Vivo	https://pubchem.ncbi.nlm.nih.gov/compound/73050806	None	N.A.
4061	38104907	2024	Y-(d-Dab)-RFFwKTF	[Al18F]NODA-MPAA-HTA	8	Conjugating 18F nuclide with a modified KE108 peptide, MPAA modification at N terminal	The amino group of KE108 peptide conjugated with the carboxyl group of NODA	Cyclic(d-Dab2-Phe8)	Mix	D-Tryp amino acid substituition, d-Dab = Diaminobutyric acid	18F-radiolabeled somatostatin analogue	Used for PET imaging of Neuroendocrine tumors (NETs)	Blood samples were collected from the retroorbital plexus into capillary at 5, 10, 15, 30,60 and 120 min	N.A.	37.63 ± 13.05 (Elimination Half Life)	BALB/c mice blood protease	Gamma counter	BALB/c mice blood sample	In Vivo	None	None	Affinity of [Al18F]NODA-MPAA-HTA (Kd = 8.77 ± 1.14 nM, n = 4)
4118	38863646	2024	N.A.	(89Zr, Mn)-WPMNs	N.A.	Free	Free	Linear	L	Mn and 89Zr labeling, MNPs modified with WL12-SH	WL12 derivative	Targets PD-L1	Blood samples were collected from orbital vein at 1, 3, 5, 10, 15, 20, 30, 45 min and 1, 1.5, 2, 3, 4, 14, 24, 48, 72, 96 h	0.5 mg/ml	0.1234 (Fast) (Metabolic Half Life)	KM mouse blood protease	Radioactivity assay using γ-counter	KM mouse blood	In Vivo	None	None	N.A.
4119	38863646	2024	N.A.	(89Zr, Mn)-WPMNs	N.A.	Free	Free	Linear	L	Mn and 89Zr labeling, MNPs modified with WL12-SH	WL12 derivative	Targets PD-L1	Blood samples were collected from orbital vein at 1, 3, 5, 10, 15, 20, 30, 45 min and 1, 1.5, 2, 3, 4, 14, 24, 48, 72, 96 h	0.5 mg/ml	1.554 (Slow) (Distribution Half Life)	KM mouse blood protease	Radioactivity assay using γ-counter	KM mouse blood sample	In Vivo	None	None	N.A.
4120	38697423	2024	N.A.	DAE Rum55	N.A.	N.A.	N.A.	N.A.	D	N.A.	Ruminococcus sp. CAG55	Epimerase	50 °C	N.A.	4.5 (Activity Half Life)	N.A.	N.A.	N.A.	In Vitro	None	None	D-allulose/D-psicose 3-epimerase (DAE/DPE, EC 5.1.3.30) and D-tagatose 3-epimerase (DTE, EC 5.1.3.31), of which DAE usually exhibits higher catalytic activity
4121	38697423	2024	N.A.	E268R-EKL16	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Ruminococcus sp. CAG55 derivative	Epimerase	50 °C	N.A.	135.3 (Activity Half Life)	N.A.	N.A.	N.A.	In Vitro	None	None	D-allulose/D-psicose 3-epimerase (DAE/DPE, EC 5.1.3.30) and D-tagatose 3-epimerase (DTE, EC 5.1.3.31), of which DAE usually exhibits higher catalytic activity
4122	38753095	2024	N.A.	Xyn10-HB	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	GH10 xylanase from Halalkalibacterium halodurans C-125	GH10 xylanase	pH 8.5 and 60 °C	N.A.	3 (Activity Half Life)	N.A.	N.A.	N.A.	In Vitro	None	None	Xyn10-HB produced active XOS with antioxidant activity determined by the DPPH radical scavenging method (IC50 of 0.54 mg/mL after 4 h)
4123	38115231	2024	N.A.	Trx1P	N.A.	N.A.	N.A.	Linear	L	N.A.	Derived from E. coli thioredoxin (Trx).	N.A.	N.A.	N.A.	124 ± 15 (T1/2 Cis-Trans Isomerizations)	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4124	38115231	2024	N.A.	Trx1Thp	N.A.	N.A.	N.A.	Linear	L	Incorporation of 4-thiaproline (Thp) at position cisPro76	Derived from E. coli thioredoxin (Trx).	N.A.	N.A.	N.A.	33 ± 3 (T1/2 Cis-Trans Isomerizations)	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4166	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) = 1.56 against S. aureus
4167	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) >100 against E.coli
4168	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) >100 against B.subtilis
4169	38097378	2023	CR	Au_CR	2	Au gold particle conjuagtion at N terminal through formation of Au-S bond	Amidation	Linear	L	None	Synthetic	Antimicrobial	Blood samples collected at 5 min and at 1, 3, 5,24, and 48 h	10 mg/kg	∼17.5	Mice plasma protease	ICP-MS	Mice plasma	In Vivo	None	None	MIC(μg/mL) = 1.56 against C.albicans
4178	37875481	2023	N.A.	IL-15-Cy7	N.A.	Free	Free	Linear	L	Cy7	Derived from Interleukin-15	Antitumor	The blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h)	N.A.	0.69	Mice blood protease	Fluorescence spectrophotometry	Mice blood	In Vivo	None	None	Not mentioned
4179	37875481	2023	N.A.	biNV-IL-15-Cy7	N.A.	Free	Free	Linear	L	Cy7	Derived from Interleukin-15	Antitumor	The blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h)	N.A.	5.66	Mice blood protease	Fluorescence spectrophotometry	Mice blood	In Vivo	None	None	Not mentioned
4189	37397495	2023	SLAFVDVLN	Peptide	9	Free	Free	Linear	L	Removing an Asp residue	Isolated from Merluccius productus fish protein hydrolysate	Inhibits BACE-1	Blood was taken after 0, 5, and 30 min and 2, 6, and 24 h after injectio	4 mg/kg	0.69	Mouse plasma protease	Mass spectrometry	Mouse plasma	In Vivo	None	None	Ki(µM)= 0.0940 BACE-1 activity with peptide which has reduced activity due to inhibition by peptide
4221	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	1.5 mg/kg	0.306	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vivo	None	None	N.A.
4222	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	4.5 mg/kg	0.344	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vivo	None	None	N.A.
4223	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	13.5 mg/kg	0.547	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vivo	None	None	N.A.
4224	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	1 mg/kg	0.805	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	N.A.
4225	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	1 mg/kg	0.248	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	N.A.
4226	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	5 mg/kg	0.46	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	N.A.
4227	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	5 mg/kg	0.437	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	N.A.
4228	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	75 mg/kg	0.341	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	N.A.
4229	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	75 mg/kg	0.391	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	N.A.
4230	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	1 mg/kg	0.665	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
4231	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	1 mg/kg	0.668	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
4232	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	5 mg/kg	0.655	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
4233	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	5 mg/kg	0.648	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
4234	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	75 mg/kg	0.615	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
4235	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	75 mg/kg	0.62	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
4236	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	5 mg/kg	0.888	Monkeys Plasma Protease	LC-MS/MS	Monkeys plasma	In Vivo	None	None	N.A.
4237	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice	50 mg/kg	0.956	Monkeys Plasma Protease	LC-MS/MS	Monkeys plasma	In Vivo	None	None	N.A.
4238	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	1 day	3.2 mg/kg	1.956	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
4239	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	plasma samples were collected from patients before the CEND-1 infusion and at 3 min (±1 min), 15 min (±3 min), 30 min (±3 min), 1 hour (±5 min), ¾ h (±10 min) and 6/8 h (±10 min) after completion of the infusion (cycle 1 day 1 of nab-paclitaxel+gemcitabine chemotherapy treatment) (Combination therapy after 7 days of run in therapy)	3.2 mg/kg	1.725	Human plasma protease	N.A.	Human plasma after nab-paclitaxel and gemcitabine	In Vivo	None	None	N.A.
4240	36982773	2023	CRGDKGPDC	CEND-1	9	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	iRGD cyclic peptide	Antitumor	plasma samples were collected from patients before the CEND-1 infusion and at 3 min (±1 min), 15 min (±3 min), 30 min (±3 min), 1 hour (±5 min), ¾ h (±10 min) and 6/8 h (±10 min) after completion of the infusion (cycle 1 day 1 of nab-paclitaxel+gemcitabine chemotherapy treatment) (Combination therapy after 7 days of run in therapy)	3.2 mg/kg	1.598	Human plasma protease	LC-MS/MS	Human plasma after nab-paclitaxel and gemcitabine	In Vivo	None	None	N.A.
4242	36873181	2023	DH-α-(4-pentenyl)-Ala-NPQIR	DR3penA	8	Free	Amidation	Linear	L	α-(4-pentenyl)-Ala introduced at positions 3 of DR8	DR8 analog	Alleviates Pulmonary Fibrosis	Samples were taken from the mixture at 0, 15, 30, 60, 120 and 240 min	10 mmol/L	174.63 ± 31.66	Mice serum protease	RP-HPLC	C57BL/6 mice serum	In Vitro	None	None	DR3penA has Minimum effective concentration is 2.5 μmol/L in both TGF-β1-induced NIH3T3 cells and A549 cells
4243	36873181	2023	DHN-α-(4-pentenyl)-Ala-PQIR	DR4penA	8	Free	Amidation	Linear	L	α-(4-pentenyl)-Ala introduced at positions 4 of DR8	DR8 analog	Alleviates Pulmonary Fibrosis	Samples were taken from the mixture at 0, 15, 30, 60, 120 and 240 min	10 mmol/L	270.65 ± 16.43	Mice serum protease	RP-HPLC	C57BL/6 mice serum	In Vitro	None	None	DR8 has Minimum effective concentrations are 20 μmol/L in TGF-β1-induced NIH3T3 cells and 10 μmol/L in A549 cells
4249	36719326	2023	RGDfK	68Ga(AAZ3A-endoHB)-c(RGD)	5	Ga labelling, conjugation of AAZ3A-endoHB-NCS to c(RGD)(cyclo(Arg-Gly-Asp-D-Phe-Lys) peptide at N terminus	Free	Cyclic (RGDfK)	Mix	None	Synthetic	Positron Emission Tomography (PET) imaging	37 °C	N.A.	Stable upto 4 hour	Human serum protease	UPLC-UV-RA	Human serum	In Vitro	None	None	N.A.
4271	36595440	2023	(y-D-Glu)-(4S)-aminoproline-LEX	TP0597850 (18)	4	Tripeptide linker {5-aminopentanoic acid [Ape(5)]–Glu–Asp} of 1 was replaced by a shorter linker (γ-D-Glu), X = Structure given in paper	Free	Linear	L	X=Structure given in paper	Synthetic	MMP2 Inhibitors	N.A.	N.A.	265	N.A.	N.A.	N.A.	N.A.	None	None	Ki = 0.034 nM for MM2 inhibition
4388	37329900	2023	N.A.	KAN-101	N.A.	N.A.	N.A.	N.A.	N.A.	Liver-targeting glycosylation signature conjugated to a deaminated gliadin peptide	N.A.	Liver-Targeted Immune Tolerance Therapy	N.A.	0·15 mg/kg, 0·3 mg/kg, 0·6 mg/kg, 1·2 mg/kg, 1·5 mg/kg	3·72 to 31·72	Human protease	N.A.	Human	In Vivo	None	None	N.A.
4416	36557850	2022	pGlu-HWSYlLRP	Leuprolide	9	pGlu = Pyroglutamate	NHEt (Ethylamine)	Linear	Mix	d-Leucine6 substituitions	Synthetic	Anticancer (Treatment of Advanced Prostate Cancer)	Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min)	0.1 mg/kg	38.2 ± 4.3 (Terminal Elimination Half Life)	Male SD Rats Plasma Protease	UPLC-MS/MS	Male SD rats plasma	In Vivo	None	None	N.A.
4417	36557850	2022	HWSYlLRP	LOC	9	Free	Leuprolide acetate with the hydroxyl groups of leuprolide acetate	Linear	Mix	Ole = oleic acid conjugation	Synthetic	Anticancer (Treatment of Advanced Prostate Cancer)	Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min)	0.122 mg/kg	172 ± 66 (Terminal Elimination Half Life)	Male SD Rats Plasma Protease	UPLC-MS/MS	Male SD rats plasma	In Vivo	None	None	N.A.
4418	36557850	2022	pGlu-HWSYlLRP	Leuprolide	9	pGlu = Pyroglutamate	NHEt (Ethylamine)	Linear	Mix	d-Leucine6 substituitions	Synthetic	Anticancer (Treatment of Advanced Prostate Cancer)	Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min)	0.1 mg/kg	166 ± 38	Male SD Rats Plasma Protease	UPLC-MS/MS	Male SD rats plasma after LOC peptide administration	In Vivo	None	None	N.A.
4437	36443291	2022	FSSE	Entry 1 (aka P5779)	4	Free	Amidation	Linear	L	None	Synthetic	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	2.0 ± 0.1	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 68.5 nM
4438	36443291	2022	azaF-SS-azaE	Entry 2 (Azapeptide 51)	4	Aza-Phe at postion 1	Amidation, Aza-glutamic acid (azaE4) modification at position 4 (E4)	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	>120	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 90 nM
4439	36443291	2022	azaF-SSE	Entry 3 (Azapeptide 52)	4	Aza-Phe at postion 1	Amidation	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	>120	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 249 nM
4440	36443291	2022	FSS-azaE	Entry 4 (Azapeptide 53)	4	Free	Aza-glutamic acid (azaE4) modification at position 4 (E4)	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	2.6 ± 0.11	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 396.8 nM
4441	36443291	2022	azaF-SSE	Entry 5 (Azapeptide 54)	4	Aza-Phe at postion 1	Amidation	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	>120	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 127.4 nM
4442	36443291	2022	azaF-SSQ	Entry 6 (Azapeptide 55)	4	Aza-Phe at postion 1	Amidation, Q amino acid subtituition at place of E at C terminal	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	24.4 ± 1.6	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 159.3 nM
4443	36443291	2022	azaF-SSQ	Entry 7 (Azapeptide 56)	4	Aza-Phe at postion 1	Amidation, Q amino acid subtituition at place of E at C terminal	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	>120	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 348.7 nM
4444	36443291	2022	azaF-SS-azaQ	Entry 8 (Azapeptide 57)	4	Aza-Phe at postion 1	Amidation, Aza-glutamine (azaQ4)	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	>120	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 83 nM
4445	36443291	2022	FSS-azaQ	Entry 9 (Azapeptide 58)	4	Free	Amidation, Aza-glutamine (azaQ4)	Linear	L	None	P5779 analogues	Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	2.9 ± 0.20	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	HMGb1:MD-2 inhibition (IC50) = 422.9 nM
4446	36443291	2022	RPPGFSPFR	Entry 1 (Bradykinin)	9	Free	Free	Linear	L	None	Derived from kininogen	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	5.29 ± 0.5	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	EC50(nM) = 44.4 (PEG2 induction in Fibroblasts)
4447	36443291	2022	azaR-PPGFSPFR	Entry 2 (azaR1-BK)	9	Modified at position 1 with an aza-amino acid (aza-arginine)	Free	Linear	L	None	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	2.46 ± 0.05	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4448	36443291	2022	R-azaP-PGFSPFR	Entry 3(azaP2-BK)	9	Free	Free	Linear	L	Modified at position 2 with an aza-amino acid (aza-proline)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	5.40 ± 1.1	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	EC50(nM) = 61.1 (PEG2 induction in Fibroblasts)
4449	36443291	2022	RP-azaP-GFSPFR	Entry 4 (azaP3-BK)	9	Free	Free	Linear	L	Modified at position 3 with an aza-amino acid (aza-proline)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	2.63 ± 0.25	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4450	36443291	2022	RPP-azaG-FSPFR	Entry 5 (azaG4-BK)	9	Free	Free	Linear	L	Modified at position 4 with an aza-amino acid (aza-glycine)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	4.33 ± 1.3	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4451	36443291	2022	RPPG-azaF-SPFR	Entry 6 (azaF5-BK)	9	Free	Free	Linear	L	Modified at position 5 with an aza-amino acid (aza-phenylalanine)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	14.7 ± 1.6	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4452	36443291	2022	RPPGFS-azaP-FR	Entry 7 (azaP7-BK)	9	Free	Free	Linear	L	Modified at position 7 with an aza-amino acid (aza-proline)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	2.38 ± 0.03	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4453	36443291	2022	RPPGFSP-azaF-R	Entry 8 (azaF8-BK)	9	Free	Free	Linear	L	Modified at position 8 with an aza-amino acid (aza-phenylalanine)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	39.3 ± 2.5	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	EC50(nM) = 99.6 (PEG2 induction in Fibroblasts)
4454	36443291	2022	RPPGFSPF-azaR	Entry 9 (azaR9-BK)	9	Free	Free	Linear	L	Modified at position 9 with an aza-amino acid (aza-arginine)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	42.6 ± 0.8	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4455	36443291	2022	R-azaP-PGFSP-azaF-R	Entry 10 ([azaP2, azaF8]-BK)	9	Free	Free	Linear	L	Modified at both positions 2 and 8 with aza-amino acids (aza-proline and aza-phenylalanine, respectively)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	29.2 ± 3.8	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	EC50(nM) = 80.6 (PEG2 induction in Fibroblasts)
4456	36443291	2022	RPPG-azaF-SP-azaF-R	Entry 11 ([azaF5, azaF8]-BK)	9	Free	Free	Linear	L	Modified at both positions 5 and 8 with aza-amino acids (aza-phenylalanine)	Aza-bradykinin analogues	Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure	Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)	0.1 mg/ml	105.8 ± 1.8	C57Bl/6 J mouse serum protease	LC-MS/MS	C57BL/6 J male mouse serum	In Vitro	None	None	N.A.
4490	36232550	2022	CYIQNCGKG	ASK2131	9	Free	Free	Cyclic (C1-C6 Disulfide Bond)	L	Native oxytocin peptide was modified with a substitution of the Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group and with a substitution of Gly for the Pro7	OXT analogs	Antiobesity	Serial blood samples (200 µL per time point) were obtained via tail nick using K3EDTA microvettes prior to and 1, 2, 4, 6, 12, and 24-h post-drug administration	300 nmol/kg	2.3	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	EC50 = 1.1 nM (ASK2131 profile against OXTR )
4491	36232550	2022	CYIQNCGKG	ASK2131	9	Free	Free	Cyclic (C1-C6 Disulfide Bond)	L	Native oxytocin peptide was modified with a substitution of the Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group and with a substitution of Gly for the Pro7	OXT analogs	Antiobesity	Serial blood samples (200 µL per time point) were obtained via tail nick using K3EDTA microvettes prior to and 1, 2, 4, 6, 12, and 24-h post-drug administration	300 nmol/kg	2.3	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	hV1aR, EC50 (nM) > 1000
4492	36232550	2022	CYIQNCGKG	ASK2131	9	Free	Free	Cyclic (C1-C6 Disulfide Bond)	L	Native oxytocin peptide was modified with a substitution of the Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group and with a substitution of Gly for the Pro7	OXT analogs	Antiobesity	Serial blood samples (200 µL per time point) were obtained via tail nick using K3EDTA microvettes prior to and 1, 2, 4, 6, 12, and 24-h post-drug administration	300 nmol/kg	2.3	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	hV2R, EC50 (nM) = 0.36
4497	36135098	2022	QDTDTWA	GNRs-AAP1-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	0.29 (T1/2 a)	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4498	36135098	2022	QDTDTWA	GNRs-AAP1-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	37.81 (T1/2 b )	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4499	36135098	2022	WTDAQTD	GNRs-AAP1-1-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	0.18 (T1/2 a)	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4500	36135098	2022	WTDAQTD	GNRs-AAP1-1-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	7.7 (T1/2 b)	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4501	36135098	2022	TADWTDQ	GNRs-AAP1-2-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	0.2 (T1/2 a)	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4502	36135098	2022	TADWTDQ	GNRs-AAP1-2-Cy5	7	Free	Free	Linear	L	Cy5 conjugation	AAP1/AAP1-1/AAP1-2 modified GNRs	Antiadhesive property	At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution	1 mg/ml	5 (T1/2 Β )	Mouse serum protease	HPLC	1 mL mouse serum	In Vitro	None	None	N.A.
4520	36075899	2022	N.A.	S-20-1	N.A.	N.A.	N.A.	Cyclic	L	Modified by adding negative charge	Synthetic	Antiviral (Against Infection By Sars-Cov-2 )	Blood samples were collected at 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h	50 mg/kg	14.53 (Terminal Elimination Half Life)	C57Bl/6 mice plasma protease	LC-MS/MS	C57BL/6 mice plasma	In Vivo	None	None	IC50 (μM) = 0.8 in HUH 7 cells
4521	36075899	2022	N.A.	S-20-1	N.A.	N.A.	N.A.	Cyclic	L	Modified by adding negative charge	Synthetic	Antiviral (Against Infection By Sars-Cov-2 )	Blood samples were collected at 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h	50 mg/kg	24.29 (Terminal Elimination Half Life)	C57Bl/6 mice plasma protease	LC-MS/MS	C57BL/6 mice plasma	In Vivo	None	None	IC50 (μM) = 0.8 in HUH 7 cells
4522	36047255	2022	H-r-Dmt-KF-PEG-DSPE, c(RGD)-PEG-DSPE	MTP/RGD-CAL/TAN NS	4 for MTP, 3 for cRGD	Free	MTP/RGD comodified with CAL/TAN NS	Linear	L(cRGD), Mix(MTP)	Dmt: 2',6'-dimethyltyrosine	Synthetic	Treatment of Acute Myocardial Infarction (Ami)	Blood samples were obtained at determined times until 72 h after injection and 15 μL of heparin (1000 U/mL) was added to each sample	10 mg/kg	8.22	AMI rats plasma protease	N.A.	AMI rats plasma	In Vivo	None	None	Blank MTP/RGD NS and RGD-PEG-DSPE groups showed over 85% of cell viability. In contrast, drugs contained formulations exhibited cytotoxicity to some extent
4523	36047255	2022	Hr-Dmt-KF	MTP-CAL/TAN NS	5	Free	MTP/RGD comodified with CAL/TAN NS (PEG-DSPE)	Linear	Mix	Dmt: 2',6'-dimethyltyrosine at position 3, D-Arg2 modification	Synthetic	Treatment of Acute Myocardial Infarction (Ami)	Blood samples were obtained at determined times until 72 h after injection and 15 μL of heparin (1000 U/mL) was added to each sample	10 mg/kg	4.59	AMI rats plasma protease	N.A.	AMI rats plasma	In Vivo	None	None	Blank MTP/RGD NS and RGD-PEG-DSPE groups showed over 85% of cell viability. In contrast, drugs contained formulations exhibited cytotoxicity to some extent.
4526	35999612	2022	RGD	cRGD-Exo/TP	3	DSPE-PEG	Free	Cyclic (RGD)	L	DiR labeled	Synthetic	Targeted delivery of triptolide against malignant melanoma	Scanned at interval times (1, 2, 4, 6, 12, and 24 h)	N.A.	27.14 ± 2.55	Mice plasma protease	IVIS at 750/780 nm	BALB/c nude mice plasma	In Vivo	None	None	Tumor inhibition rate of 65.73 ± 3.29% in the cRGD-Exo/TP
4546	35890224	2022	K-(PEG)4-E	177Lu-Palm-3PRGD2	2	Lys1 linked with (palmitoyl-Glu-OH)	Glu3 linked with (PEG4-c(RGDfK))2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between	Synthetic	Antitumor	N.A.	0.74 MBq	4.49 (T1/2a)	KM mice blood protease	Gamma counter	KM mice blood sample	In Vivo	None	None	N.A.
4547	35890224	2022	E	177Lu-3PRGD2	1	PEG4	Glu linked with [PEG4-c(RGDfK)]2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4	Synthetic	Antitumor	N.A.	0.74 MBq	1.94 (T1/2a)	KM mice blood protease	Gamma counter	KM mice blood sample	In Vivo	None	None	N.A.
4548	35890224	2022	K-(PEG)4-E	177Lu-Palm-3PRGD2	2	Lys1 linked with (palmitoyl-Glu-OH)	Glu3 linked with (PEG4-c(RGDfK))2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between	Synthetic	Antitumor	N.A.	0.74 MBq	73.42 (T1/2Β)	KM mice blood protease	Gamma counter	KM mice blood sample	In Vivo	None	None	N.A.
4549	35890224	2022	E	177Lu-3PRGD2	1	PEG4	Glu linked with [PEG4-c(RGDfK)]2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4	Synthetic	Antitumor	N.A.	0.74 MBq	11.81 (T1/2Β)	KM mice blood protease	Gamma counter	KM mice blood sample	In Vivo	None	None	N.A.
4550	35890224	2022	K-(PEG)4-E	177Lu-Palm-3PRGD2	2	Lys1 linked with (palmitoyl-Glu-OH)	Glu3 linked with (PEG4-c(RGDfK))2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between	Synthetic	Antitumor	N.A.	0.74 MBq	63.71 (Slow)	C57Bl/6 mice blood protease	Gamma counter	C57BL/6 mice blood sample	In Vivo	None	None	N.A.
4551	35890224	2022	E	177Lu-3PRGD2	1	PEG4	Glu linked with [PEG4-c(RGDfK)]2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4	Synthetic	Antitumor	N.A.	0.74 MBq	14.54 (Slow)	C57Bl/6 mice blood protease	Gamma counter	C57BL/6 mice blood sample	In Vivo	None	None	N.A.
4552	35890224	2022	K-(PEG)4-E	177Lu-Palm-3PRGD2	2	Lys1 linked with (palmitoyl-Glu-OH)	Glu3 linked with (PEG4-c(RGDfK))2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between	synthetic	Antitumor	N.A.	0.74 MBq	2.08 (Fast)	C57Bl/6 mice blood protease	Gamma counter	C57BL/6 mice blood sample	In Vivo	None	None	N.A.
4553	35890224	2022	E	177Lu-3PRGD2	1	PEG4	Glu linked with [PEG4-c(RGDfK)]2	Cyclic (3PRGD2)	Mix	177Lu radiolabeling at PEG4	synthetic	Antitumor	N.A.	0.74 MBq	1.06 (Fast)	C57Bl/6 mice blood protease	Gamma counter	C57BL/6 mice blood sample	In Vivo	None	None	N.A.
4558	35850571	2022	WYVYPSM	dTBP2	7	Free	Free	Linear	L	None	dTCTP-binding peptide-2	Antiinflammatory	Blood samples were collected from the orbital sinus at 0.083, 0.25, 0.5, 1, 2, 4, and 8 h after dosing with dTBP2 or PEG-dTBP2	10 mg/kg	1.01 ± 0.25	ICR male mice orbital sinus plasma protease	LC-MS/MS	ICR Male mice orbital sinus plasma	In Vivo	None	None	dTBP2 results in 30% inhibition of inflammatory cell infiltration in BALF compared to the OVA-challenged group
4559	35850571	2022	WYVYPSM	PEG-dTBP2	7	PEGylation (mPEG)	Free	Linear	L	None	dTCTP-binding peptide-2	Antiinflammatory	Blood samples were collected from the orbital sinus at 0.083, 0.25, 0.5, 1, 2, 4, and 8 h after dosing with dTBP2 or PEG-dTBP2	10 mg/kg	2.57 ± 1.11	ICR male mice orbital sinus plasma protease	LC-MS/MS	ICR Male mice orbital sinus plasma	In Vivo	None	None	PEG-dTBP2 results in 45% inhibition, indicating that PEGylation enhances the anti-inflammatory effects of dTBP2
4568	35807500	2022	AEWCP	TIPP	5	Free	Free	Linear	L	None	From calf thymus extracts	Treatment of Asthma	At 0.5, 1, 2, 5, 10, 15, 20, and 40 min post administration (eight mice at each time points), blood samples were taken from an inner canthus	50 mg/kg	5.99 ± 1.82	Mice plasma protease	LC-MS/MS	Mice plasma	In Vivo	None	None	TIPP inhibits degranulation and inflammation in RBL-2H3 cells and pretreatment with 200 microgram/mL of TIPP for 20 minutes reduces the level of biomarkers of allergic response and inflammation i.e β-hexosaminidase, Histamine, IL-4
4572	35772783	2022	DHNNPQaR	DR7dA	8	Free	Amidation	Linear	Mix	Replacing the isoleucine (Ile7) residue with D-alanine7 (D-Ala)	DR8 analog	Ameliorated Tumor Growth Factor (Tgf)-B1-Induced Fibrogenesis And Bleomycin-Induced Pf	An aliquot of 40 ml was taken at 0, 15, 30, 60, 120 and 240 min	10 mM	201.08 ± 58.86	Mouse serum protease	RP-HPLC	Mouse serum	In Vitro	None	None	DR7dA showed no cytotoxic effects in A549 and NIH3T3 cells even at high concentrations (up to 160 μM)
4573	35772783	2022	DHNNPQIR	DR8	8	Free	Amidation	Linear	L	None	Derived from rapeseed protein	Ameliorated Tumor Growth Factor (Tgf)-B1-Induced Fibrogenesis And Bleomycin-Induced Pf	An aliquot of 40 ml was taken at 0, 15, 30, 60, 120 and 240 min	10 mM	70.19 ± 6.83	Mouse serum protease	RP-HPLC	Mouse serum	In Vitro	None	None	The effective concentration of DR8 was higher than that of DR7dA in both cell lines, indicating that DR7dA is more potent in inhibiting fibrosis
4575	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.04 mmol/kg	0.3 (Elimination Half Life)	Male SD rats plasma protease	ICP-MS	Male SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4576	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.04 mmol/kg	0.28 (Elimination Half Life)	Female SD rats plasma protease	ICP-MS	Female SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4577	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.04 mmol/kg	0.57(Elimination Half Life)	(P) SD rats plasma protease	ICP-MS	(P) SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4578	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.1 mmol/kg	0.31 (Elimination Half Life)	Male SD rats plasma protease	ICP-MS	Male SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4579	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.1 mmol/kg	0.32 (Elimination Half Life)	Female SD rats plasma protease	ICP-MS	Female SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4580	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.1 mmol/kg	0.65 (Elimination Half Life)	(P) SD rats plasma protease	ICP-MS	(P) SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4581	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.2 mmol/kg	0.3 (Elimination Half Life)	Male SD rats plasma protease	ICP-MS	Male SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4582	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.2 mmol/kg	0.32 (Elimination Half Life)	Female SD rats plasma protease	ICP-MS	Female SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4583	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3	0.2 mmol/kg	0.22 (Elimination Half Life)	(P) SD rats plasma protease	ICP-MS	(P) SD rats plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4584	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.04 mmol/kg	0.76 (Elimination Half Life)	Male dogs plasma protease	ICP-MS	Male dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4585	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.04 mmol/kg	0.74 (Elimination Half Life)	Female dogs plasma protease	ICP-MS	Female dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4586	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.04 mmol/kg	0.8 (Elimination Half Life)	(P) dogs plasma protease	ICP-MS	(P) dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4587	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.1 mmol/kg	0.7 (Elimination Half Life)	Male dogs plasma protease	ICP-MS	Male dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4588	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.1 mmol/kg	0.67 (Elimination Half Life)	Female dogs plasma protease	ICP-MS	Female dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4589	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.1 mmol/kg	0.33 (Elimination Half Life)	(P) dogs plasma protease	ICP-MS	(P) dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4590	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.2 mmol/kg	0.69 (Elimination Half Life)	Male dogs plasma protease	ICP-MS	Male dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4591	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.2 mmol/kg	0.63 (Elimination Half Life)	Female dogs plasma protease	ICP-MS	Female dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4592	35703463	2022	TVRTSAD	MT218	7	Free	ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker	Linear	L	None	ZD2 analog	Cancer targeting contrast agent	Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.	0.2 mmol/kg	0.048 (Elimination Half Life)	(P) dogs plasma protease	ICP-MS	(P) dogs plasma	In Vivo	None	None	MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4602	35659720	2022	LPLTPLP	DTX-P7	7	DTX	Free	Linear	L	None	Docetaxel (DTX) and heptapeptide (P7) Fusion protein	Anticancer (Treatment Of Non-Small Cell Lung Cancer)	1, 2, 4, 12, 24, 48 and 72 h after injection, the mice were anesthetized, and approximately 0.5 ml of blood was collected	60 mg/kg	Longer Half Life	BALB/c mice plasma protease	HPLC	BALB/c mice bearing A549 tumors plasma	In Vivo	None	None	IC50 = 11.4 nM for DTX-P7 in A549 cells
4603	35659720	2022	LPLTPLP	DTX-P7	7	DTX	Free	Linear	L	None	Docetaxel (DTX) and heptapeptide (P7) Fusion protein	Anticancer (Treatment Of Non-Small Cell Lung Cancer)	1, 2, 4, 12, 24, 48 and 72 h after injection, the mice were anesthetized, and approximately 0.5 ml of blood was collected	60 mg/kg	Longer Half Life	BALB/c mice plasma protease	HPLC	BALB/c mice bearing A549 tumors plasma	In Vivo	None	None	IC50 = 0.62 nM for DTX-P7 in H1975 cells
4614	35582852	2022	lKlW	CP	8	Free	PNAM37 linked through NH2 group	Cyclic(N-C terminal bond)	Mix	D-leucine at position 1 and 3	Synthetic	Drug delivery vectors	Blood samples (0.2 mL) were taken prior to dose administration and at 1, 5, 10, 20, 30, 60, 120, 180, 240, 360, 480, and 1440 min after dose administratio	1 μCi	14.6 ± 2.9 (Elimination Half Life)	Rats plasma protease	Liquid scintillation counter	Rats plasma	In Vivo	None	None	For concentrations of 1 mg/mL CP , cell viabilities drop to about 75% for the 4T1 cell line
4620	35438695	2022	SFQ	SFQSeM	3	Free	Selenium methylated conjugation at C terminal	Linear	L	None	From soybeans	Effective Se nutritional supplement	N.A.	N.A.	81.60 ± 11.88	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4621	35430336	2022	KPSSPPEE	A6 peptide	8	Acetylation	Amidation	Linear	L	None	Synthetic	Antitumor	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4678	34910492	2022	SETSKSF	68Ga-DOTA-SETSKSF	7	68Ga labelled	Free	Cyclic	L	None	Synthetic	Used For Positron Emission Tomography imaging of PD-L1 expression in tumors	N.A.	N.A.	14.48 ± 3.26	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4679	34910492	2022	SETSKSF	68Ga-DOTA-SETSKSF	7	68Ga labelled	Free	Cyclic	L	None	Synthetic	Used For Positron Emission Tomography imaging of PD-L1 expression in tumors	N.A.	5.29 ± 0.21 (%ID/g)	N.A.	N.A.	N.A.	H1975 tumor model	In Vitro	None	None	N.A.
4680	34910492	2022	SETSKSF	68Ga-DOTA-SETSKSF	7	68Ga labelled	Free	Cyclic	L	None	Synthetic	Used For Positron Emission Tomography imaging of PD-L1 expression in tumors	N.A.	0.89 ± 0.10 (%ID/g)	N.A.	N.A.	N.A.	A549 tumor model	In Vitro	None	None	N.A.
4719	N.A.	2022	N.A.	Test 1	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	100 (Terminal Half Life)	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4720	N.A.	2022	N.A.	Test 2	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	101 (Terminal Half Life)	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4721	N.A.	2022	N.A.	Test 3	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	105 (Terminal Half Life)	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4722	N.A.	2022	N.A.	Test 4	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	GLP-1 analogs	Antidiabetes	Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks)	10 nmol/kg	109 (Terminal Half Life)	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vivo	None	EP 2021080747 W	N.A.
4755	35910276	2022	N.A.	BA17	N.A.	Free	Free	Linear	L	None	Isolated from B. licheniformis	Serine protease	50°C	N.A.	90 (Enzyme Activity)	N.A.	Zymography	N.A.	In Vitro	None	None	N.A.
4756	35910276	2022	N.A.	BA17	N.A.	Free	Free	Linear	L	None	Isolated from B. licheniformis	Serine protease	60 °C	N.A.	12 (Enzyme Activity)	N.A.	Zymography	N.A.	In Vitro	None	None	N.A.
4763	35488338	2022	N.A.	FRAP-smTG	N.A.	Frap (A Fusion Tag)	Free	Linear	L	None	TGm1 variant	Used to generate protein crosslinking or attachment of small molecules	60 ℃	0.4 mg/mL	< 2 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4764	35488338	2022	N.A.	FRAP-TGm1	N.A.	Frap (A Fusion Tag)	Free	Linear	L	None	TGm1 variant	Used to generate protein crosslinking or attachment of small molecules	60 ℃	0.4 mg/mL	11.31 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4765	35488338	2022	N.A.	FRAPD-TGm1	N.A.	Frap (A Fusion Tag)	Free	Linear	L	additional modification (Asp residue)	TGm1 variant	Used to generate protein crosslinking or attachment of small molecules	60 ℃	0.4 mg/mL	21.97 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	N.A.
4770	35133860	2022	N.A.	E187A	N.A.	Free	Free	Linear	L	Residue Glu187 of the Ca1 site in the catalytic domain was replaced by Ala	Derived from preTSS	Collagenolytic protease	70°C	N.A.	N.A.	N.A.	N.A.	N.A.	In Viro Study	None	None	When the residue Glu187 of the Ca1 site in the catalytic domain was replaced by Ala, the resulting variant E187A was completely inactivated after incubation at 70°C for 3 h
4819	35259149	2022	RKDVY	TP5-MA	5	Free	Free	Linear	L	Conjugating a myristic acid-acylated lysine to a permissive site of TP5, Radiolabeling C14 at Lys2	Myristic Acid-Modified Tp5	Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids)	One hundred microliter plasma samples were collected at the following time intervals: 0.5, 5, 10, 20, 30, and 45 min and 1, 2, 3, 4, 6, 8,and 10 h after peptide administration.	1 mg/kg	1.75 ± 0.72	Wistar rats plasma protease	LC-MS/MS	Wistar rats plasma	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5
4820	35259149	2022	RKDVY	TP5	5	Free	Free	Linear	L	None	Synthetic	Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids)	One hundred microliter plasma samples were collected at the following time intervals: 0.5, 5, 10, 20, 30, and 45 min and 1, 2, 3, 4, 6, 8,and 10 h after peptide administration.	1 mg/kg	0.022 ± 0.004	Wistar rats plasma protease	LC-MS/MS	Wistar rats plasma	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5
4821	35259149	2022	RKDVY	TP5-MA	5	Free	Free	Linear	L	Conjugating a myristic acid-acylated lysine to a permissive site of TP5, Radiolabeling C14 at Lys2	Myristic Acid-Modified Tp5	Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids)	37 °C	N.A.	4.42	Human plasma protease	LC-MS/MS	1 mg/mL human plasma	In Vitro	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5
4844	35059568	2021	Hoo-FOP-hle-Pff-F	JPE-1375	7	Hoo = L-hydroorotic acid	Amidation	Linear	Mix	hle5 = D-homoleucine, Pff6 = Phe(4-F), Orn = Ornithine,Replaces the C-terminal Arg of PMX53 with a hydrophobic amino acid	Peptidomimetic C5a receptor antagonists	C5Ar1 Antagonists	Serial blood samples were collected at 10, 15, 30, 45, and 60 min, and at 2, 4, 6, and 24 h via a tail vein	1 mg/kg	0.13 (Elimination Half Life)	Mice plasma protease	LC-MS	Mice plasma	In Vivo	None	None	The inhibition of TNF levels also presented a similar median effective concentration (EC50) for PMX53 (5.9 μM)
4845	35059568	2021	FOP-Cha-WR	PMX53	6	Acetylation	Free	Cyclic(Orn-Arg N-C bond)	Mix	cha4 = D-cyclohexylalanine, O2 = Ornithine	Peptidomimetic C5a receptor antagonists	C5Ar1 Antagonists	Serial blood samples were collected at 10, 15, 30, 45, and 60 min, and at 2, 4, 6, and 24 h via a tail vein	1 mg/kg	1.3 (Elimination Half Life)	Mice plasma protease	LC-MS	Mice plasma	In Vivo	None	None	The inhibition of TNF levels also presented a similar median effective concentration (EC50) for JPE-1375 (4.5 μM)
4846	35056979	2021	FRRG	Al-ProD	4	Maleimide	DOX	Linear	L	None	Albumin-binding maleimide and cathepsin B-cleavable peptide conjugate	Antitumor	blood samples were collected from mice at pre-determined times (0, 3 h, 6 h, 9 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h, and 144 h)	3 mg/kg	3.1	BALB/C nude mice plasma protease	Fluorescence assay	BALB/c nude mice plasma	In Vivo	None	None	The IC50 value of HSA-bound Al-ProD in MDA-MB231 breast cancer cells is 7.33 µM, On day 20, the tumor volume in the Al-ProD-treated group was 347.42 ± 25.9 mm³, significantly smaller than the free DOX group (580.25 ± 139.92 mm³) and saline group (1810.98 ± 544.56 mm³)
4893	34575581	2021	OP-(d-Cha)-WR	C5a receptor 1 antagonist (PMX205)	5	HC = Hydrocinnamate, O1: ornithine	Free	Cyclic	Mix	D-Cha3: cyclohexylalanine	Lipophilic analogue of PMX53	Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury	Blood samples were collected at 0.04, 0.25, 0.5, 0.75, 1, 1.5, 1, 4, 6, and 24 h for both groups and then 48, 72, 96, and 120 h	1 mg/kg	0.84 (Terminal Elmination Half Life)	Mice plasma protease	LC-MS/MS	Mice plasma	In Vivo	None	None	IC50 = 31 nM for PMX205
4894	34575581	2021	OP-(d-Cha)-WR	C5a receptor 1 antagonist (PMX205)	5	HC = Hydrocinnamate, O1: ornithine	Free	Cyclic	Mix	D-Cha3: cyclohexylalanine	Lipophilic analogue of PMX53	Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury	Samples (n = 4) were quenched at regular intervals of 5 min, 10 min, 15 min, 30 min and 60 min	1 µg/ml	0.17 (Elimination Half Life)	Mice plasma protease	LC-MS/MS	Mice plasma	In Vivo	None	None	IC50 = 31 nM for PMX205
4895	34575581	2021	OP-(d-Cha)-WR	C5a receptor 1 antagonist (PMX205)	5	HC = Hydrocinnamate, O1: ornithine	Free	Cyclic	Mix	D-Cha3: cyclohexylalanine	Lipophilic analogue of PMX53	Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury	Blood sample was collected at 2.5, 5, 10, 15, 30, 45, 60, and 90 min	1 μg/mL	0.33 (Elimination Half Life)	Mice spinal cord homogenate protease	LC-MS/MS	Mice spinal cord homogenate	In Vivo	None	None	IC50 = 31 nM for PMX205
4911	34254101	2021	GG	Glycylglycine model dipeptide	2	Free	Free	Linear	L	None	Synthetic	N.A.	60 °C and pD 7.4	Equimolar amounts of Hf-NU-1000 and GG	231	N.A.	1H-NMR	Equimolar amounts of Hf-NU-1000 (Metal-organic Framework)(Hf6O8-based NU-1000) and GG	In Vitro	None	None	A glycylglycine model dipeptide was hydrolysed with a rate constant of kobs = 8.33 × 10−7 s−1
4912	34206631	2021	YGGFL	Leu-ENK	5	Free	Free	Linear	L	None	Opioid peptide	Analgesic	Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min	315 µmol/L	25	Mice plasma protease	UPLC	Mice dipotassium ethylenediaminetetraacetic acid containing pooled plasma	In Vitro	None	None	N.A.
4913	34206631	2021	YGGFL	KK 103	6	N terminal of Tyr linked with NH bond with R1 = Structure given in paper	Free	Linear	L	None	Synthetic	Analgesic	Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min	315 µmol/L	37	Mice plasma protease	UPLC	Mice dipotassium ethylenediaminetetraacetic acid containing pooled plasma	In Vitro	None	None	N.A.
4914	34206631	2021	YGGFL	KK 103	6	N terminal of Tyr linked with NH bond with R1 = Structure given in paper	Free	Linear	L	None	Synthetic	Analgesic	Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min	315 µmol/L	>95% Remained	CSF Protease	UPLC	Pooled human cerebrospinal fluid	In Vitro	None	None	N.A.
4915	34206631	2021	YGGFL	Leu-ENK	5	Free	Free	Linear	L	None	Opioid peptide	Analgesic	Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min	315 µmol/L	>80% Remained	CSF Protease	UPLC	Pooled human cerebrospinal fluid	In Vitro	None	None	N.A.
4916	34201398	2021	KRRVRWIIW	optP7	9	Free	Free	Linear	L	None	Synthetic	Antimicrobial	For 0, 0.5, 1, 3, 6, and 24 h at 37 °C	100 μM	13	Human serum protease	UPLC-MS	Human serum	In Vitro	None	None	MIC(µM) = 3 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 0.8 for E.coli in growth media MH,MIC(µM) = 1.5 for K. pneumoniae in growth media MH,MIC(µM) = 1.5 for A. baumannii in growth media MH,MIC(µM) = 0.8 for VRE in growth media MH,MIC(µM) = 6 for MRSA in growth media MH
4922	34122400	2021	RKDVY	TP5	5	Free	Free	Linear	L	None	derived from thymopoietin	Immunomodulatory	15 min at 37°C	10 µg/mL	3.2 ± 0.5	Human serum protease	HPLC	Human serum	In Vitro	None	None	The cytotoxicity of CbTP was lower than that of parental peptide CATH2
4924	34064291	2021	RGDfK	111In-DOTA-EB-cRGDfK	5	Radiolabelled with 111ln, DOTA, EvansBlue dye	Free	Cyclic	L	None	Synthetic	For Spect imaging and potential theranostic	Blood samples (10 μL) were collected by heart puncture under 2% isoflurane anesthesia at 0.083, 0.5, 2, 4, 24, 48, 72, 96, and 168 h	1.85 MBq	77.3 (Terminal Half Life)	U-87 mg tumor bearing mice plasma protease	Radioactivity assay	U-87 mg tumor-bearing mice plasma	In Vivo	None	None	IC50(nM) =71.7
4925	34064291	2021	RGDfK	111In-DOTA-cRGDfK	5	Radiolabelled with 111ln, DOTA	Free	Cyclic	L	None	Synthetic	For Spect imaging and potential theranostic	Blood samples (10 μL) were collected by heart puncture under 2% isoflurane anesthesia at 0.083, 0.5, 2, 4, 24, 48, 72, 96, and 168 h	1.85 MBq	17.2 (Terminal Half Life)	U-87 mg tumor bearing mice plasma protease	Radioactivity assay	U-87 mg tumor-bearing mice plasma	In Vivo	None	None	IC50(nM) =35.2
4945	33822591	2021	KX	PEG−DNP-Lys conjugates 6C	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0)	Synthetic	Increases Half Life	pH 7.4	N.A.	87 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4946	33822591	2021	KX	PEG−DNP-Lys conjugates 6C	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0)	Synthetic	Increases Half Life	pH 7.4	N.A.	87 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4947	33822591	2021	KX	PEG−DNP-Lys conjugates 6C	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a two-carbon spacer between the β-carbon and the triazole, Mod = NC−, X = Structure given in paper (n=0)	Synthetic	Increases Half Life	pH 7.4	N.A.	1030 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4948	33822591	2021	KX	PEG−DNP-Lys conjugates 7	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1)	Synthetic	Increases Half Life	pH 7.4	N.A.	256 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4949	33822591	2021	KX	PEG−DNP-Lys conjugates 7	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1)	Synthetic	Increases Half Life	pH 7.4	N.A.	724 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4950	33822591	2021	KX	PEG−DNP-Lys conjugates 7	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a three-carbon spacer between the β-carbon and the triazole, Mod = PhSO2−, X = Structure given in paper (n=1)	Synthetic	Increases Half Life	pH 7.4	N.A.	2490 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4951	33822591	2021	KX	PEG−DNP-Lys conjugates 8	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a four-carbon spacer between the β-carbon and the triazole, Mod = MeSO2−, X = Structure given in paper (n=2)	Synthetic	Increases Half Life	pH 7.4	N.A.	1570 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4952	33822591	2021	KX	PEG−DNP-Lys conjugates 8	1	DNP	PEG20 KDa, MeO	Linear	L	GDM linker with a four-carbon spacer between the β-carbon and the triazole, Mod = MeSO2−, X = Structure given in paper (n=2)	Synthetic	Increases Half Life	pH 7.4	N.A.	5310 (b-Elimination Half-Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
4955	33791863	2021	DRVYIHP	125I-Ang1–7	7	Free	Free	Linear	L	125I labeled	Synthetic	Role in Renal and Cardiovascular Homeostasis	Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration	4.5 mM	0.6	Rats plasma protease	Radioactivity assay	Rats plasma	In Vivo	None	None	Ang1–7 exhibited 4.2±0.1%, 3.7±0.6%, 4.4±0.2%, and 2.6±0.4% binding capacity in D.D. water, PBS 50 mM, PBS10mM, and acetate bufer, respectively
4956	33791863	2021	DRVYIHP	125I-Ang Conj.	7	Thiol bisphosphonate,Maleimidopropionyl,PEG conjugated at N terminus	Free	Linear	L	125I labeled	Synthetic	Role in Renal and Cardiovascular Homeostasis	Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration	4.5 mM	3.4	Rats plasma protease	Radioactivity assay	Rats plasma	In Vivo	None	None	Ang Conj. values were 20.4±0.5%,6.8±0.6%, 8.4±0.2%, and 11.6±0.2%
4957	33791863	2021	DRVYIHP	125I-Ang Conj	7	Thiol bisphosphonate,Maleimidopropionyl,PEG conjugated at N terminus	Free	Linear	L	125I labeled	Synthetic	Role in Renal and Cardiovascular Homeostasis	Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration	4.5 mM	6.6	Rats plasma protease	Radioactivity assay	Rats plasma	In Vivo	None	None	Ang Conj. values were 20.4±0.5%,6.8±0.6%, 8.4±0.2%, and 11.6±0.2%
4960	33674401	2021	pCl-F-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic(C-C NC terminal bond)	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	76	Whole body	Dosimetry	whole body	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4961	33674401	2021	pCl-Phe-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	92	Human kidney homogenate protease	Dosimetry	Human kidney homogenate	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4962	33674401	2021	pCl-Phe-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	97	Human spleen	Dosimetry	Human spleen	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4963	33674401	2021	pCl-Phe-cyclo(c-Y-(D-4-amino-Phe)(Cbm))-KTC)y	177Lu-DOTA-LM3	9	DOTA	Amidation	Cyclic	Mix	DOTA-LM3 conjugation, Cbm = Carbamoyl, 177Lu labeling, pCl-Phe = P-Chloro Phenyalanine	SST analog	Treating Metastatic Neuroendocrine Neoplasms (Nens)	N.A.	7 ± 1 GBq	111	Human metastases	Dosimetry	Human metastases	In Vivo	None	None	Partial Remission: 17 patients (36.2%), Stable Disease: 23 patients (48.9%), Progressive Disease: 7 patients (14.9%) (The efficacy of the peptide 177Lu-DOTA-LM3 for peptide receptor radionuclide therapy (PRRT) in patients with metastatic neuroendocrine neoplasms )
4968	33665501	2021	Poly(L-glutamic acid)	PLG-Pt	n	Free	Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid	Linear	L	None	Synthetic	Anticancer	At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats	3 mg/kg	1.9	Rats plasma protease	ICP-MS	Rats plasma	In Vivo	None	None	IC50 (μg mL−1) = 4.8 in SKOV3 cells
4969	33665501	2021	Poly(L-glutamic acid)	PEG-PLG-Pt	n	PEGylation	Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid	Linear	L	PEGylation	Synthetic	Anticancer	At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats	3 mg/kg	8.8	Rats plasma protease	ICP-MS	Rats plasma	In Vivo	None	None	IC50 (μg mL−1) = 11 in SKOV3 cells
4970	33665501	2021	Poly(L-glutamic acid)	PEG-pHe-PLG-Pt (pH 7.4)	n	PEG-CDM	Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid	Linear	L	Poly(L-glutamic acid) is grafted with methoxy poly(ethylene glycol) (PEG) using a pH-sensitive linker, 2-propionic-3-methylmaleic anhydride = CDM	Synthetic	Anticancer	At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats	3 mg/kg	7.9	Rats plasma protease	ICP-MS	Rats plasma	In Vivo	None	None	IC50 (μg mL−1) = 8.5 in SKOV3 cells
4971	33665501	2021	Poly(L-glutamic acid)	PEG-pHe-PLG-Pt (pH 6.5)	n	PEG-CDM	Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid	Linear	L	Poly(L-glutamic acid) is grafted with methoxy poly(ethylene glycol) (PEG) using a pH-sensitive linker, CDM = 2-propionic-3-methylmaleic anhydride	Synthetic	Anticancer	At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats	3 mg/kg	N.A.	Rats plasma protease	ICP-MS	Rats plasma	In Vivo	None	None	IC50 (μg mL−1) = 5.8 in SKOV3 cells
4972	33665501	2021	PLGLAG-Poly(L-glutamic acid)	PEG-MMP-PLG-Pt	n+6	PEGylation	Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid	Linear	L	PEGylation through an MMP-sensitive peptide linker (PLGLAG), CDM = 2-propionic-3-methylmaleic anhydride	Synthetic	Anticancer	At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats	3 mg/kg	7.8	Rats plasma protease	ICP-MS	Rats plasma	In Vivo	None	None	IC50 (μg mL−1) = 6.9 in SKOV3 cells
4988	33607165	2021	RRPYIL	NT(8:13)	6	Free	Free	Linear	L	None	Neuropeptide	Analgesic	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	0.98 ± 0.08	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 1.65 ± 0.06 for hNTS1
4989	33607165	2021	KKPYIL	JMV438	6	Both Arg residues in positions 1 and 2 were replaced by two Lys	Free	Linear	L	None	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	1.57 ± 0.27	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 4.00 ± 0.35 for hNTS1
4990	33607165	2021	KΨ[CH2NH]KPYIL	JMV449	6	Free	Free	Linear	L	Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	8.37 ± 2.02	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 2.02 ± 0.80 for hNTS1
4991	33607165	2021	KΨ[CH2NH]K-Sip-YIL	JMV5170	6	Free	Free	Linear	L	Pro10 was then substituted by the silylated proline analog silaproline(Sip) , Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	22.1 ± 1.9	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 296 ± 51 for hNTS1
4992	33607165	2021	KΨ[CH2NH]KPYI-TMSAla	JMV5206	6	Free	substitution of Leu13 by the (L)-(Trimethylsilyl)-Alanine (TMSAla)	Linear	L	Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	2.13 ± 0.19	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 2.45 ± 0.17 for hNTS1
4993	33607165	2021	KΨ[CH2NH]K-Sip-YI-TMSAla	JMV5296	6	Free	Free	Linear	L	Di-substitution with both Sip and TMSAla, Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	20.6 ± 4.15	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 610 ± 31 for hNTS1
5026	33801382	2021	fQWAVGH	[177Lu]Lu-NeoB	7	Acetylation, 177Lu Labelling	Aminoethylamide -NH-CH(CH2-CH(CH3)2)2	Linear	Mix	None	Derived from the antagonist GRPR peptide SB3	Antitumor (Treatment of Gastrointestinal Stromal Tumors)	N.A.	N.A.	40.2 (Distribution Half Life)	N.A.	N.A.	N.A.	N.A.	https://pmc.ncbi.nlm.nih.gov/articles/PMC6150197/	None	[177Lu]Lu-NeoB tumor uptake in 400 pmol group mice (~11% ID/g) was found to be higher than that observed in 800 pmol group mice (~7% ID/g)
5027	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	25 IU/kg	31	HemA mice plasma protease	Chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5028	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	50 IU/kg	30	HemA mice plasma protease	Chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5029	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	100 IU/kg	25	HemA mice plasma protease	Chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5030	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	100 IU/kg	32.7	Cynomolgus monkeys plasma protease	Chromogenic activity assays	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5031	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role in clotting	N.A.	300 IU/kg	33.6	Cynomolgus monkeys plasma protease	Chromogenic activity assays	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5032	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	100 IU/kg	29.3	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5033	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	300 IU/kg	34	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5034	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	200 IU/kg	31.8	HemA mice plasma protease	chromogenic activity assays	HemA mice plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5035	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	200 IU/kg	29.9	VWF Het mice plasma protease	chromogenic activity assays	VWF Het mice plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5036	32078672	2020	MQIELSTCFFLCLLRFCFSATRRYYLGAVELSWDYMQSDLGELPVDARFPPRVPKSFPFNTSVVYKKTLFVEFTDHLFNIAKPRPPWMGLLGPTIQAEVYDTVVITLKNMASHPVSLHAVGVSYWKASEGAEYDDQTSQREKEDDKVFPGGSHTYVWQVLKENGPMASDPLCLTYSYLSHVDLVKDLNSGLIGALLVCREGSLAKEKTQTLHKFILLFAVFDEGKSWHSETKNSLMQDRDAASARAWPKMHTVNGYVNRSLPGLIGCHRKSVYWHVIGMGTTPEVHSIFLEGHTFLVRNHRQASLEISPITFLTAQTLLMDLGQFLLFCHISSHQHDGMEAYVKVDSCPEEPQLRMKNNEEAEDYDDDLTDSEMDVVRFDDDNSPSFIQIRSVAKKHPKTWVHYIAAEEEDWDYAPLVLAPDDRSYKSQYLNNGPQRIGRKYKKVRFMAYTDETFKTREAIQHESGILGPLLYGEVGDTLLIIFKNQASRPYNIYPHGITDVRPLYSRRLPKGVKHLKDFPILPGEIFKYKWTVTVEDGPTKSDPRCLTRYYSSFVNMERDLASGLIGPLLICYKESVDQRGNQIMSDKRNVILFSVFDENRSWYLTENIQRFLPNPAGVQLEDPEFQASNIMHSINGYVFDSLQLSVCLHEVAYWYILSIGAQTDFLSVFFSGYTFKHKMVYEDTLTLFPFSGETVFMSMENPGLWILGCHNSDFRNRGMTALLKVSSCDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSQNGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGTSTEPSEGSAPGTSESATPESGPGTSESATPESGPGTSESATPESGPGSEPATSGSETPGSEPATSGSETPGSPAGSPTSTEEGTSTEPSEGSAPGTSTEPSEGSAPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPASSEITRTTLQSDQEEIDYDDTISVEMKKEDFDIYDEDENQSPRSFQKKTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG/MIPARFAGVLLALALILPGTLCAEGTRGRSSTARCSLFGSDFVNTFDGSMYSFAGYCSYLLAGGCQKRSFSIIGDFQNGKRVSLSVYLGEFFDIHLFVNGTVTQGDQRVSMPYASKGLYLETEAGYYKLSGEAYGFVARIDGSGNFQVLLSDRYFNKTCGLCGNFNIFAEDDFMTQEGTLTSDPYDFANSWALSSGEQWCERASPPSSSCNISSGEMQKGLWEQCQLLKSTSVFARCHPLVDPEPFVALCEKTLCECAGGLECACPALLEYARTCAQEGMVLYGWTDHSACSPVCPAGMEYRQCVSPCARTCQSLHINEMCQERCVDGCSCPEGQLLDEGLCVESTECPCVHSGKRYPPGTSLSRDCNTCICRNSQWICSNEECPGECLVTGQSHFKSFDNRYFTFSGICQYLLARDCQDHSFSIVIETVQCADDRDAVCTRSVTVRLPGLHNSLVKLKHGAGVAMDGQDIQLPLLKGDLRIQHTVTASVRLSYGEDLQMDWDGRGRLLVKLSPVYAGKTCGLCGNYNGNQGDDFLTPSGLAEPRVEDFGNAWKLHGDCQDLQKQHSDPCALNPRMTRFSEEACAVLTSPTFEACHRAVSPLPYLRNCRYDVCSCSDGRECLCGALASYAAACAGRGVRVAWREPGRCELNCPKGQVYLQCGTPCNLTCRSLSYPDEECNEACLEGCFCPPGLYMDERGDCVPKAQCPCYYDGEIFQPEDIFSDHHTMCYCEDGFMHCTMSGVPGSLLPDAVLSSPLSHRSKRSLSCRPPMVKLVCPADNLRAEGLECTKTCQNYDLECMSMGCVSGCLCPPGMVRHENRCVALERCPCFHQGKEYAPGETVKIGCNTCVCRDRKWNCTDHVCDATCSTIGMAHYLTFDGLKYLFPGECQYVLVQDYCGSNPGTFRILVGNKGCSHPSVKCKKRVTILVEGGEIELFDGEVNVKRPMKDETHFEVVESGRYIILLLGKALSVVWDRHLSISVVLKQTYQEKVCGLCGNFDGIQNNDLTSSNLQVEEDPVDFGNSWKVSSQCADTRKVPLDSSPATCHNNIMKQTMVDSSCRILTSDVFQDCNKLVDPEPYLDVCIYDTCSCESIGDCAAFCDTIAAYAHVCAQHGKVVTWRTATLCPQSCEERNLRENGYEAEWRYNSCAPACQVTCQHPEPLACPVQCVEGCHAHCPPGKILDELLQTCVDPEDCPVCEVAGRRFASGKKVTLNPSDPEHCQICHCDVVNLTCEACQEPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSEPATSGSETPGTSESATPESGPGTSTEPSEGSAPGSPAGSPTSTEEGTSESATPESGPGSEPATSGSETPGTSESATPESGPGSPAGSPTSTEEGSPAGSPTSTEEGASSDKNTGDYYEDSYEDISAYLLSKNNAIEPRSFSDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc-VWF-XTEN (construct 4) (BIVV001)	3,611	Free	Free	Linear	L	Three amino acid residues (GAP) from the FVIII/XTEN junction and 9 amino acids (PPVLKRHQA) from the FVIII B-domain linker were removed, LVPR thrombin site located between DʹD3 and Fc on constructs 1 and 2 was replaced with an FVIII acidic region 2 (a2) thrombin site	Synthetic	Role In Clotting	N.A.	200 IU/kg	26.9	DKO mice plasma protease	chromogenic activity assays	DKO mice plasma	In Vivo	PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf	None	ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5071	32888078	2020	QHTQITKV	Human Lau-PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	2.96	Simulated intestinal fluid protease	HPLC	Simulated intestinal fluid	In Vitro	None	None	N.A.
5072	32888078	2020	QHSQITKV	Mouse Lau- PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.3	Simulated intestinal fluid protease	HPLC	Simulated intestinal fluid	In Vitro	None	None	N.A.
5073	32888078	2020	QHTQITKV	Human Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	N.A.	Simulated intestinal fluid protease	HPLC	Simulated intestinal fluid	In Vitro	None	None	N.A.
5074	32888078	2020	QHSQITKV	Mouse Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	4.52	Simulated intestinal fluid protease	HPLC	Simulated intestinal fluid	In Vitro	None	None	N.A.
5075	32888078	2020	QHTQITKV	Human Lau-PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.6	50% W/V liver homogenate protease	HPLC	50% w/v liver homogenate	In Vitro	None	None	N.A.
5076	32888078	2020	QHSQITKV	Mouse Lau- PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.95	50% W/V liver homogenate protease	HPLC	50% w/v liver homogenate	In Vitro	None	None	N.A.
5077	32888078	2020	QHTQITKV	Human Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	18.5	50% W/V liver homogenate protease	HPLC	50% w/v liver homogenate	In Vitro	None	None	N.A.
5078	32888078	2020	QHSQITKV	Mouse Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	1.36	50% W/V liver homogenate protease	HPLC	50% w/v liver homogenate	In Vitro	None	None	N.A.
5079	32888078	2020	QHTQITKV	Human Lau-PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.15	50% V/V mouse plasma protease	HPLC	50% v/v mouse plasma	In Vitro	None	None	N.A.
5080	32888078	2020	QHSQITKV	Mouse Lau- PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	5.86	50% V/V mouse plasma protease	HPLC	50% v/v mouse plasma	In Vitro	None	None	N.A.
5081	32888078	2020	QHTQITKV	Human Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.11	50% V/V Mouse Plasma Protease	HPLC	50% v/v Mouse plasma	In Vitro	None	None	N.A.
5082	32888078	2020	QHSQITKV	Mouse Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.87	50% V/V Mouse Plasma Protease	HPLC	50% v/v Mouse plasma	In Vitro	None	None	N.A.
5083	32888078	2020	QHTQITKV	Human Lau-PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.36	50% W/V Brain Homogenate Protease	HPLC	50% w/v Brain Homogenate	In Vitro	None	None	N.A.
5084	32888078	2020	QHSQITKV	Mouse Lau- PTEN-PDZ	8	N-Lauryl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.2	50% W/V Brain Homogenate Protease	HPLC	50% w/v Brain Homogenate	In Vitro	None	None	N.A.
5085	32888078	2020	QHTQITKV	Human Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.16	50% W/V Brain Homogenate Protease	HPLC	50% w/v Brain Homogenate	In Vitro	None	None	N.A.
5086	32888078	2020	QHSQITKV	Mouse Myr-PTEN-PDZ	8	N-myristoyl	Free	Linear	L	Lipidation	Synthetic	Treatment of Alzheimer's diseases	Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min	Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)	0.25	50% W/V Brain Homogenate Protease	HPLC	50% w/v Brain Homogenate	In Vitro	None	None	N.A.
5128	32603666	2020	V	V-Gem	1	Free	Gemicitabine	Linear	L	None	Derived from Gemcitabine	Anticancer	2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min	76 nmol/g	46.2	Mice blood plasma protease	LC-MS/MS	Mice blood plasma (analyte = Gemcitabine)	In Vivo	None	None	N.A.
5129	32603666	2020	V	V-Gem	1	Free	Gemicitabine	Linear	L	None	Derived from Gemcitabine	Anticancer	2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min	76 nmol/g	128	Mice blood plasma protease	LC-MS/MS	Mice blood plasma (analyte = dFdU)	In Vivo	None	None	N.A.
5130	32603666	2020	V	V-Gem	1	Free	Gemicitabine	Linear	L	None	Derived from Gemcitabine	Anticancer	2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min	76 nmol/g	3.7	Mice blood plasma protease	LC-MS/MS	Mice blood plasma (analyte = Prodrug)	In Vivo	None	None	N.A.
5131	32603666	2020	V	V-Gem	1	Free	Gemicitabine	Linear	L	None	Derived from Gemcitabine	Anticancer	2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min	228 nmol/g	39.1	Mice blood plasma protease	LC-MS/MS	Mice blood plasma (analyte = Gemcitabine)	In Vivo	None	None	N.A.
5132	32603666	2020	V	V-Gem	1	Free	Gemicitabine	Linear	L	None	Derived from Gemcitabine	Anticancer	2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min	228 nmol/g	216	Mice blood plasma protease	LC-MS/MS	Mice blood plasma (analyte = dFdU)	In Vivo	None	None	N.A.
5133	32582624	2020	RRPYIL	NT(8-13)	6	Free	Free	Linear	L	None	Derived from NT	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	1.0 ± 0.1	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 1.5 ± 0.03 for hNTS1
5134	32582624	2020	KKPYIL	Entry 1	6	KK amino acid substiuitions	Free	Linear	L	None	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	1.6 ± 0.3	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 4.0 ± 0.4 for hNTS1
5135	32582624	2020	Kψ(CH2NH)KPYIL	Entry 2	6	Kψ[CH2NH]K substiuition at position 1	Free	Linear	L	None	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	8.4 ± 2.0	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 2.0 ± 0.8 for hNTS1
5136	32582624	2020	KKPYI	Entry 3	5	KK amino acid substiuitions	TMSAla conjugation	Linear	L	None	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	1.6 ± 0.3	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 0.018 ± 0.004 for hNTS1
5137	32582624	2020	Kψ(CH2NH)KPYI	Entry 4	5	Kψ[CH2NH]K substiuition	TMSAla conjugation	Linear	L	None	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	2.0 ± 0.2	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 2.5 ± 0.2 for hNTS1
5138	32582624	2020	KK-Sip-YIL	Entry 5	6	KK amino acid substiuitions	Free	Linear	L	Sip amino acid substiution	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	4.5 ± 0.8	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 14 ± 11 for hNTS1
5139	32582624	2020	Kψ(CH2NH)K-Sip-YIL	Entry 6	6	Kψ[CH2NH]K substiuition	Free	Linear	L	Sip amino acid substiution	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	22 ± 2	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 300 ± 50 for hNTS1
5140	32582624	2020	KK-Sip-YI	Entry 7	5	Kψ[CH2NH]K substiuition	TMSAla conjugation	Linear	L	Sip amino acid substiution, TMSAla substuition	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	3.5 ± 0.1	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 55 ± 5 for hNTS1
5141	32582624	2020	Kψ(CH2NH)K-Sip-YI	Entry 8	5	Kψ[CH2NH]K substiuition	TMSAla conjugation	Linear	L	Sip amino acid substiution, TMSAla substuition	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	20 ± 4	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 610 ± 30 for hNTS1
5142	32582624	2020	KKPKIL	Entry 9	6	KK amino acid substiuitions	Free	Linear	L	Substiution of Y amino acid with K	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	2.9 ± 0.2	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 7 600 ± 1 000 for hNTS1
5143	32582624	2020	Kψ(CH2NH)KPKIL	Entry 10	6	Kψ[CH2NH]K substiuition	Free	Linear	L	Substiution of Y amino acid with K	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	5.0 ± 0.2	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 6 600 ± 2 0003 for hNTS1
5144	32582624	2020	KKPKI	Entry 11	5	KK amino acid substiuitions	TMSAla-OH conjugation	Linear	L	Substiution of Y amino acid with K	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	2.8 ± 0.1	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 710 ± 100 for hNTS1
5145	32582624	2020	Kψ(CH2NH)KPKI	Entry 12	5	Kψ[CH2NH]K substiuition	TMSAla-OH conjugation	Linear	L	Substiution of Y amino acid with K	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	10 ± 1	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 150 ± 60 for hNTS1
5146	32582624	2020	KKPwI	Entry 13	5	KK amino acid substiuitions	TMSAla-OH conjugation	Linear	Mix	Substiution of Y amino acid with d-W	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	10 ± 2	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 3 600 ± 600 for hNTS1
5147	32582624	2020	Kψ(CH2NH)KPwI	Entry 14	5	Kψ[CH2NH]K substiuition	TMSAla-OH conjugation	Linear	L	Substiution of Y amino acid with d-W	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	19 ± 0.3	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 55 ± 3 for hNTS1
5148	32582624	2020	KKP-Dmt-Tle-L	Entry 15	6	KK amino acid substiuitions	Free	Linear	L	Substiution of Y, I amino acid with Dmt, Tle	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	4.6 ± 0.6	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 57 ± 6 for hNTS1
5149	32582624	2020	Kψ(CH2NH)KP-Dmt-L	Entry 16	5	Kψ[CH2NH]K substiuition	Free	Linear	L	Substiution of Y, I amino acid with Dmt	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	>24	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 110 ± 2 for hNTS1
5150	32512181	2020	LEDGPKFL	[3H]-THF	8	Free	Free	Linear	L	3H labeling at proline5 residue	Isolated from calf thymus	Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment)	Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min	93 nmol/mL	3.7 ± 0.2	Rats blood protease	N.A.	Rats blood sample	In Vitro	None	None	N.A.
5151	32512181	2020	LEDGPKFL	[3H]-THF	8	Free	Free	Linear	L	3H labeling at proline5 residue	Isolated from calf thymus	Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment)	Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min	93 nmol/mL	5.6 ± 0.2	Mouse blood protease	N.A.	Mouse blood sample	In Vitro	None	None	N.A.
5152	32512181	2020	LEDGPKFL	[3H]-THF	8	Free	Free	Linear	L	3H labeling at proline5 residue	Isolated from calf thymus	Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment)	Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min	93 nmol/mL	5.2 ± 0.4	Human blood protease	N.A.	Human blood sample	In Vitro	None	None	N.A.
5160	32464231	2020	KGH	FP-EGCG-NPs	3	Free	Folate peptide (FA-Pep-1) conjugated to EGCG-loaded nanoparticles (EGCG-NPs)	Linear	L	None	Polyphenolic constituent of green tea	Antitumor (Against Mda-Mb-231 Tumor Xenograft)	blood samples were collected at different time intervals (0.5, 1, 2, 4, 6, 8, 12, 24 and 48 h post-administration	0.1 mL	25.13 ± 8.62	Male SD rats plasma protease	HPLC	Male SD rats plasma	In Vivo	None	None	IC50 = 15.56 for FP-EGCG-NPs(µg/mL) in MDA-MB-231
5174	32332143	2020	fQWAVGH	68Ga‐NeoBOMB1	7	68Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1	NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminal	Linear	L	None	Synthetic	DOTA‐coupled GRPR‐antagonist	2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i	50 µg	27.3	Human plasma protease	RP-HPLC	Human plasma	In Vivo	None	None	N.A.
5175	32332143	2020	fQWAVGH	68Ga‐NeoBOMB1	7	68Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1	NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminal	Linear	L	None	Synthetic	DOTA‐coupled GRPR‐antagonist	2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i	50 µg	35	Human blood protease	RP-HPLC	Human blood sample	In Vivo	None	None	N.A.
5201	32141733	2020	INPIYRLRY	TB1-RS6	6	Fluorescein	Amidation	Linear	L	Single atom O toS substitution (X=S)	Thioamide-stabilized version	Stabilization of cancer imaging peptides	37 °C	50 μM	>24	Mouse serum protease	HPLC	Mouse serum	In Vitro	https://sci-hub.se/10.1021/acs.molpharmaceut.6b00464	None	KI = 101 ± 24 nM, The IC50 values determined for TB1 and TB1-RS6 (719 ± 143 nM and 1363 ± 323 nM, respectively
5202	32141733	2020	INPIYRLRY	TB1	6	Fluorescein	Amidation	Linear	L	None	Fluorescein analog of BVD15	Stabilization of cancer imaging peptides	37 °C	50 μM	1.5	Mouse serum protease	HPLC	Mouse serum	In Vitro	https://sci-hub.se/10.1021/acs.molpharmaceut.6b00464	None	KI = 53 ± 10 nM, The IC50 values determined for TB1 and TB1-RS6 (719 ± 143 nM and 1363 ± 323 nM, respectively
5229	32034289	2020	VL-GGGGSGGGGSGGGGS-VH-GGGGS-KPLPEVTDEY	α-GD2 scFv TM	N.A.	Radiolabelled with 64Cu	E5B9	Linear	L	VH and VL joined by linker (GGGGS)3	Synthetic	Antitumor	N.A.	N.A.	1.6	Mice blood protease	PET scanning	Mice blood sample	In Vivo	E5B9 sequence available on this link: https://pmc.ncbi.nlm.nih.gov/articles/PMC6805801/	None	EC50 = 0.7 nM (target cell lysis)
5230	32023048	2020	KEKEKEKE	ICP NPs	8	Free	One 4-carboxy-3-fluorophenylboronic acid (PBA), Three cholic acids (CA)	Linear	L	None	Synthetic	Transcellular Tumor Penetration And Photo−Chemo Combination Therapy	Blood samples (∼0.2 mL each time point) were collected from the jugular vein cannula to centrifuge tubes containing 20 μL of 10 IU heparin at predetermined time points (5, 10, 15, 30, 60, 120, 180, 240, 360, 720, 1440 min)	3 mg/kg	3.34 ± 0.86	Female wistar rats plasma protease	HPLC	Female wistar rats plasma	In Vivo	None	None	Additional phototherapy by treatment with laser further enhanced the antitumor activity of both ICP and hICP NPs, leading to a complete cure rate of 10% and 50%, respectively
5231	32023048	2020	KEKEKEKE	hICP NPs	8	Free	One 4-carboxy-3-fluorophenylboronic acid (PBA), Three cholic acids (CA)	Linear	L	ICP NPs were stacked into nanoparticle clusters upon coating with DA modified HA, Folic acid	Synthetic	Transcellular Tumor Penetration And Photo−Chemo Combination Therapy	Blood samples (∼0.2 mL each time point) were collected from the jugular vein cannula to centrifuge tubes containing 20 μL of 10 IU heparin at predetermined time points (5, 10, 15, 30, 60, 120, 180, 240, 360, 720, 1440 min)	3 mg/kg	7.97 ± 2.38	Female wistar rats plasma protease	HPLC	Female wistar rats plasma	In Vivo	None	None	Additional phototherapy by treatment with laser further enhanced the antitumor activity of both ICP and hICP NPs, leading to a complete cure rate of 10% and 50%, respectively
5241	31866565	2020	YSNSG	YSNSG peptide	5	Free	Free	Cyclic	L	None	Synthetic	Antitumor	Blood samples from blood vessel in the tail were taken at the following time intervals: 15, 30, 60, 90 and 120 min	20 mg/kg	25.8 ± 8.2	B16F1 melanoma mice plasma protease	UPLC-MS/MS	B16F1 melanoma mice plasma	In Vivo	None	None	The relative recoveries of the microdialysis probes of YSNSG peptide in mice using the reverse dialysis method were 79.3 ± 6.6% in the region 1 of the tumor and 79.1 ± 7.4% in the region 2 of the tumor
5252	31765157	2020	XFLFRPRN	CPN-116	7	X = Struture given in paper (6b)	Amidation	Linear	L	None	Synthetic	Antiobesity	At 30 min	50 mg/mL	20% of the initial concentration	Rats serum protease	LC-MS	Rats serum after i.p. pentobarbital sodium	In Vitro	https://sci-hub.se/10.1021/jm500599s	None	CPN exhibits a selective agonistic activity to mouse NMUR2 with an EC50 value of 28 ± 2 nM
5253	31765157	2020	XFLFRPRN	CPN-116	7	X = Struture given in paper (6b)	Amidation	Linear	L	None	Synthetic	Antiobesity	at 30 min	50 mg/mL	90% of initial concentration	Rats CSF protease	LC-MS	Rats CSF after i.p. pentobarbital sodium	In Vitro	https://sci-hub.se/10.1021/jm500599s	None	CPN exhibits a selective agonistic activity to mouse NMUR2 with an EC50 value of 28 ± 2 nM
5254	31765157	2020	XFLFRPRN	CPN-116	7	X = Struture given in paper (6b)	Amidation	Linear	L	None	Synthetic	Antiobesity	4 hours	50 mg/mL	20% of the initial concentration	Rats CSF protease	LC-MS	Rats CSF after i.p. pentobarbital sodium	In Vitro	https://sci-hub.se/10.1021/jm500599s	None	CPN exhibits a selective agonistic activity to mouse NMUR2 with an EC50 value of 28 ± 2 nM
5282	32454120	2020	N.A.	Uox-WT	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment of hyperuricemia	Incubated for 4 h at room temperature	28 μM	1.1 (Enzymatic Activity Half Life)	Mice serum protease	Uric acid degradation assay	Mice serum	In Vivo	None	None	N.A.
5283	32454120	2020	N.A.	Uox-HSA	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment of hyperuricemia	Incubated for 4 h at room temperature	28 μM	17.4 (Enzymatic Activity Half Life)	Mice serum protease	Uric acid degradation assay	Mice serum	In Vivo	None	None	N.A.
5284	32454120	2020	N.A.	PEG-PAEU + Uox-HSA	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment of hyperuricemia	Incubated for 4 h at room temperature	28 μM	43.6 (Enzymatic Activity Half Life)	Mice serum protease	Uric acid degradation assay	Mice serum	In Vivo	None	None	N.A.
5285	32454120	2020	N.A.	PEG-PAEU-ABP + Uox-HSA	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Treatment of hyperuricemia	Incubated for 4 h at room temperature	28 μM	96.3 (Enzymatic Activity Half Life)	Mice serum protease	Uric acid degradation assay	Mice serum	In Vivo	None	None	N.A.
5291	33270417	2020	ENGTISRY	Peptide 1a	8	Free	Free	Linear	L	None	From human α-1-acid glycoprotein 1	Used to study glycosylation effects on deamidation	48 hours under 37 C	N.A.	31.08 (Deamidation Half Life)	N.A.	HPLC-MS	N.A.	In Vitro	None	None	N.A.
5292	33270417	2020	SYSRNHTY	Peptide 2a	8	Free	Free	Linear	L	None	From peptidyl-prolyl cis−trans isomerase FKBP10	Used to study glycosylation effects on deamidation	12 days under 37 C	N.A.	6.4 (Deamidation Half Life)	N.A.	HPLC-MS	N.A.	In Vitro	None	None	N.A.
5293	33270417	2020	EPWNSSIT	Peptide 3a	8	Free	Free	Linear	L	None	From deoxyribonuclease-2-alpha	Used to study glycosylation effects on deamidation	15 days under 37 C	N.A.	13 (Deamidation Half Life)	N.A.	HPLC-MS	N.A.	In Vitro	None	None	N.A.
5294	33270417	2020	SEGGNDSR	Peptide 4a	8	Free	Free	Linear	L	None	From protein sidekick-1	Used to study glycosylation effects on deamidation	13 days under 37 C	N.A.	13.2 (Deamidation Half Life)	N.A.	HPLC-MS	N.A.	In Vitro	None	None	N.A.
5295	33270417	2020	ASSGNATG	Peptide 5a	8	Free	Free	Linear	L	None	From the smoothened homologue	Used to study glycosylation effects on deamidation	13 days under 37 C	N.A.	18.78(Deamidation Half Life)	N.A.	HPLC-MS	N.A.	In Vitro	None	None	N.A.
5297	33115231	2020	RGDfK	ASL	5	Bodipy Tr-X Ester Linked Via (Peg)12	Free	Linear	Mix	None	Synthetic	Anticancer	N.A.	N.A.	Stable (Release Half Life)	N.A.	Fluorescent assay	PBS containing 0.05% (w/v) Tween 80	In Vitro	None	None	IC50 = 4.908 ± 0.739 μM for dEx
5315	31594790	2019	RLYE	RLYE	4	Free	Free	Linear	L	None	Synthetic	Antitumor	4 hours at 37°C	2 µg/µl	73	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 = 89.1 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC)
5316	31594790	2019	RLYE	Ac-RLYE	4	Acetylation	Free	Linear	L	None	Synthetic	Antitumor	4 hours at 37°C	2 µg/µl	8.8	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 = 37.1 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC)
5317	31594790	2019	RLYE	RLYE-NH2	4	Free	Amidation	Linear	L	None	Synthetic	Antitumor	4 hours at 37°C	2 µg/µl	1.3	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 = 326.6 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC)
5318	31594790	2019	rLYE	rLYE	4	L-Arg replaced with D-Arg at position 1	Free	Linear	Mix	None	Synthetic	Antitumor	4 hours at 37°C	2 µg/µl	7	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 >1,000 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC)
5319	31594790	2019	RLYE	Ac-RLYE-NH2	4	Acetylation	Amidation	Linear	L	None	Synthetic	Antitumor	4 hours at 37°C	2 µg/µl	9.4	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 = 52.5 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC)
5337	31453257	2019	N.A.	Pept. A	N.A.	Free	Free	Cyclic	L	N.A.	N.A.	Therapeutic agent against a CNS-related disorder	Blood (100 µl) and CSF (100 µl) aliquots for drug concentration assessment were collected pre-dose, on study day 1 at 0.5, 1.5, 3, 6, and 24 h post first dose, and on study day 2 at 1.5 h post the second dose (corresponding to 25.5 h from study start)	4.2 mg/kg	3.5 ± 0.7 (Terminal Half Life)	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	None	None	N.A.
5338	31453257	2019	N.A.	Pept. A	N.A.	Free	Free	Cyclic	L	N.A.	N.A.	Therapeutic agent against a CNS-related disorder	Blood (100 µl) and CSF (100 µl) aliquots for drug concentration assessment were collected pre-dose, on study day 1 at 0.5, 1.5, 3, 6, and 24 h post first dose, and on study day 2 at 1.5 h post the second dose (corresponding to 25.5 h from study start)	4.2 mg/kg	14.3 ± 5.5 (Terminal Half Life)	göttingen Minipig Csf Lumbar Protease	LC-MS/MS	Göttingen minipigs CSF lumbar	In Vivo	None	None	N.A.
5340	31443263	2019	RKDVY	TP5	5	Free	Free	Linear	L	None	Arg32–Tyr36 fragment derived from thymopoietin	Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions)	37 °C	N.A.	1.32 ± 0.24	Rats plasma proteaes	HPLC	10 μg/mL rats plasma	In Vitro	None	None	Among the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL
5362	31194563	2019	CARSKNKDC	Fasudil in CAR-liposome	9	Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys	Amidation	Linear	L	None	Synthetic	Treatment of Pulmonary Arterial Hypertension	N.A.	3 mg/kg	0.7 ± 0.3	Sham rats plasma protease	LC–MS/MS	Sham rats plasma	In Vivo	None	None	N.A.
5363	31194563	2019	CARSKNKDC	Fasudil in CAR-liposome	9	Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys	Amidation	Linear	L	None	Synthetic	Treatment of Pulmonary Arterial Hypertension	N.A.	3 mg/kg	1.1 ± 0.3	PAH rats plasma protease	LC–MS/MS	PAH rats plasma	In Vivo	None	None	N.A.
5364	31194563	2019	CARSKNKDC	Fasudil in CAR-liposome	9	Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys	Amidation	Linear	L	None	Synthetic	Treatment of Pulmonary Arterial Hypertension	N.A.	3 mg/kg	12.9 ± 4.6	Sham rats plasma protease	LC–MS/MS	Sham rats plasma	In Vivo	None	None	N.A.
5365	31194563	2019	CARSKNKDC	Fasudil in CAR-liposome	9	Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys	Amidation	Linear	L	None	Synthetic	Treatment of Pulmonary Arterial Hypertension	N.A.	3 mg/kg	16.1 ± 4.1	PAH rats plasma protease	LC–MS/MS	PAH rats plasma	In Vivo	None	None	N.A.
5398	31079216	2019	KPyIL	NT-5	4	AOPC8 = 1‑(2‑(2‑aminophenyl)‑2‑oxoethyl)‑1H‑pyrrole‑2‑ carboxylic acid (AOPC)	Free	Linear	Mix	Lys9, d-Tyr(Et)11 modification in NT(8–13)	NT analogue	Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue	24 h incubation at 37 °C	160 μM	Higher stability than NT	Human plasma protease	UHPLC	Human plasma	In Vitro	None	None	−LogIC50±SE = 5.63±0.15 in Neurotensin (1–13) for NTS1 receptor
5399	31079216	2019	rPyIL	NT-6	5	AOPC8 = 1‑(2‑(2‑aminophenyl)‑2‑oxoethyl)‑1H‑pyrrole‑2‑ carboxylic acid (AOPC), d-Arg9 modification at N terminal	Free	Linear	Mix	d-Tyr(Et)11 modification in NT(8–13)	NT analogue	Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue	24 h incubation at 37 °C	160 μM	Higher stability than NT	Human plasma protease	UHPLC	Human plasma	In Vitro	None	None	−LogIC50±SE = 5.53±0.31 in Neurotensin (1–13) for NTS1 receptor
5400	31079216	2019	KrPyIL	NT-8	6	AOPC8 = 1‑(2‑(2‑aminophenyl)‑2‑oxoethyl)‑1H‑pyrrole‑2‑ carboxylic acid (AOPC)	Free	Linear	Mix	Lys8, d-Arg9, d-Tyr(Et)11] modification in NT(7–13)	NT analogue	Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue	24 h incubation at 37 °C	160 μM	Higher stability than NT	Human plasma protease	UHPLC	Human plasma	In Vitro	None	None	−LogIC50±SE = 5.28±0.20 in Neurotensin (1–13) for NTS1 receptor
5406	31064153	2019	K-GlyΨ[Trl]-GlyΨ[Trl]-R	Triazolopeptides compounds 3	4	Free	Free	Linear	L	Lys1 linked with Har = Homo-Arginine, GlyΨ[Trl] is a glycyl-1,2,3-triazole unit mimicking glycine (triazole ring substitution instead of peptide bond)	Derived from triazolopeptide	Inhibits the interaction between Neuropilin-1 and Vascular Endothelial Growth Factor-165	37 °C	1.1 µmol/mL	>> 48	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 8.39 μM
5407	31064153	2019	k-GlyΨ[Trl]-GlyΨ[Trl]-R	Triazolopeptides compounds 4	4	D-Lys at the first position which contains Har = Homo-Arginine side chain	Free	Linear	Mix	GlyΨ[Trl] is a glycyl-1,2,3-triazole unit mimicking glycine (triazole ring substitution instead of peptide bond)	Derived from triazolopeptide	Inhibits the interaction between Neuropilin-1 and Vascular Endothelial Growth Factor-165	37 °C	1.1 µmol/mL	>> 48	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 10.22 μM
5408	31064153	2019	K-Dab	Lys(Har)-Dab	2	Lys at the first position contains Har = Homo-Arginine side chain	Dab (2,4-diaminobutyric acid)	Linear	L	None	KPPR analogs	Peptidic inhibitor of the VEGF165/NRP-1 interaction	All samples were incubated at 37 °C and 100 µL of aliquots were withdrawn at different time intervals (for 4 and 5: 0, 10, 20, 30, 40, 50, 60, 70, 80 min, 1.5h, 2h, 2.5h, 3h, 4h, 6h	1.1 µmol/mL	34	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 0.2 μM
5409	31064153	2019	Dap-PR	Peptidotriazoles	3	Dap (2,3-diaminopropionic acid) substiuition at 1st position	Free	Linear	L	None	KPPR analogs	Peptidic inhibitor of the VEGF165/NRP-1 interaction	All samples were incubated at 37 °C and 100 µL of aliquots were withdrawn at different time intervals (for 4 and 5: 0, 10, 20, 30, 40, 50, 60, 70, 80 min, 1.5h, 2h, 2.5h, 3h, 4h, 6h	1.1 µmol/mL	41	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 0.2 μM
5410	31064153	2019	KPA	Lys(Har)-PA	3	Side chain of the Lys residue in the first position was extended by attaching additional homoarginine (Har)	Free	Linear	L	None	KPPR analogs	Peptidic inhibitor of the VEGF165/NRP-1 interaction	100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h)	1.1 µmol/mL	39	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 0.2μM
5411	31064153	2019	Dab-R	Dab-R	2	Dab (2,4-diaminobutyric acid) substiuition at 1st position	Free	Linear	L	None	KPPR analogs	Peptidic inhibitor of the VEGF165/NRP-1 interaction	100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h)	1.1 µmol/mL	44	Human plasma protease	HPLC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 0.3 μM
5418	30986342	2019	NLLMAAS	T4-Cy5.5	7	Free	Conjugated with Cy5.5	Linear	L	None	Synthetic	Antitumor	N.A.	N.A.	1	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	Free T4 or P-T4 slowed tumor regrowth after chemotherapy, whereas the P-T4 treatment group exhibited a better suppressive effect
5433	30900390	2019	SDKP	Ac-SDKP	4	Acetylation	Free	Linear	L	None	Synthetic	Antifibrotic effects on Hepatic Fibrosis	At 2, 4, 6, 8, 10, 18, 30, 120, 360, 480, and 540 min after the injection, 50 μL of blood was sampled from each animal through the caudal vein	1 mg/kg	9.65 ± 1.78	Rats serum protease	RP-HPLC	Rats serum	In Vivo	None	None	Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro
5434	30900390	2019	SdkP	Ac-SD(d)K(d)P	4	Acetylation	Free	Linear	Mix	Asp2 and Lys3 were replaced with their D-isomers	Synthetic	Antifibrotic effects on Hepatic Fibrosis	At 2, 4, 6, 8, 10, 18, 30, 120, 360, 480, and 540 min after the injection, 50 μL of blood was sampled from each animal through the caudal vein	1 mg/kg	176.5 ± 6.45	Rats serum protease	RP-HPLC	Rats serum	In Vivo	None	None	Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro
5435	30900390	2019	SDKP	Ac-SDKP	4	Acetylation	Free	Linear	L	None	synthetic	Antifibrotic Effects On Hepatic Fibrosis	9 h at 37 C	100 μM	6.47 ± 1.53	Human Serum Protease	HPLC	human serum	In Vitro	None	None	Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro
5436	30900390	2019	SdkP	Ac-SD(d)K(d)P	4	Acetylation	Free	Linear	Mix	Asp2 and Lys3 were replaced with their D-isomers	synthetic	Antifibrotic Effects On Hepatic Fibrosis	9 h at 37 C	100 μM	161.5 ± 5.79	Human Serum Protease	HPLC	human serum	In Vitro	None	None	Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro
5444	30809901	2019	DNIXWK	FITC-AAR029b	6	FITC labelled	Free	Macrocyclic	L	X=Structure given in paper	Derived from a class of peptides known as cyclic peptide triazoles (cPTs)	Antiviral	N.A.	0.01 mg/kg	2.92 ± 0.93 (T1/2b-Elimination Half Life)	Rats plasma protease	Fluorescence assay	Rats plasma	In Vivo	None	None	EC50(nM) = 210±16 for AAR029b in Bal.01 virus
5445	30809901	2019	DNIXWK	FITC-AAR029b in Liposome	6	FITC labelled	Free	Macrocyclic	L	X=Structure given in paper	Derived from a class of peptides known as cyclic peptide triazoles (cPTs)	Antiviral	N.A.	0.01 mg/kg	8.87 ± 3.17(T1/2b-Elimination Half Life)	Rats plasma protease	Fluorescence assay	Rats plasma	In Vivo	None	None	EC50(nM) = 210±16 for AAR029b in Bal.01 virus
5453	30709867	2019	DRVYIHS	PNA5	7	Free	Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus	Linear	L	None	Ang-(1-7) analogs	Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction	N.A.	100 µM	1.0 ± 0.2	Rats serum protease	Tandem mass spectrometry (MS)	Rats serum	In Vitro	None	None	Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition)
5454	30709867	2019	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Ang-(1-7)	Decrease Brain ROS production and Inflammation in Preclinical models of HF	N.A.	100 µM	0.25 ± 0.05	Rats serum protease	Tandem mass spectrometry (MS)	Rats serum	In Vitro	None	None	Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition)
5455	30709867	2019	DRVYIHS	PNA5	7	Free	Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus	Linear	L	None	Ang-(1-7) analogs	Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction	N.A.	10 mg/kg	18.2 ± 3	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition)
5456	30709867	2019	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Ang-(1-7)	Decrease Brain ROS production and Inflammation in Preclinical models of HF	N.A.	10 mg/kg	20.9 ± 0.7	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition)
5457	30709867	2019	DRVYIHS	PNA5	7	Free	Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus	Linear	L	None	Ang-(1-7) analogs	Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction	N.A.	10 mg/kg	26.6 ± 3.6	CSF protease	LC-MS	CSF	In Vivo	None	None	Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition)
5458	30709867	2019	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Ang-(1-7)	Decrease Brain ROS production and Inflammation in Preclinical models of HF	N.A.	10 mg/kg	24.7 ± 5	CSF protease	LC-MS	CSF	In Vivo	None	None	Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition)
5488	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-F	Compound 7	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated-Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated DAsp	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	115 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.35 (In Vitro CCK-1R Potency)
5489	30624060	2019	D-Phe(4sm)-Nle-GW-Nle-MeAsp-MePhe	Compound 8	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	L	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, MeAsp = N-methylated Asp	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	145 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.97 (In Vitro CCK-1R Potency)
5490	30624060	2019	D-Phe(4sm)-Nle-GW-Nle-DMeAsp-MePhe	Compound 9	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	113 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.60 (In Vitro CCK-1R Potency)
5491	30624060	2019	D-Phe(4sm)-LGW-Nle-DMeAsp-MePhe	Compound 14	9	yGlu-(OEG)2 linker between C14 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	2 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.74 (In Vitro CCK-1R Potency)
5492	30624060	2019	D-Phe(4sm)-LGW-Nle-DMeAsp-MePhe	Compound 15	9	yGlu-(OEG)2 linker between C16 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	37 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.72 (In Vitro CCK-1R Potency)
5493	30624060	2019	D-Phe(4sm)-LGW-Nle-DMeAsp-MePhe	Compound 16	9	yGlu-(OEG)2 linker between C20 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	153 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.43 (In Vitro CCK-1R Potency)
5494	30624060	2019	D-sTyr-Nle-GW-Nle-DMeAsp-MePhe	Compound 17	9	yGlu-PEG10-PEG10 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	103 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.54 (In Vitro CCK-1R Potency)
5495	30624060	2019	D-sTyr-Nle-GW-Nle-DMeAsp-MePhe	Compound 18	9	yGlu-PEG10-PEG10 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Phe(4sm) = 4-sulfomethylphenylalanine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	161 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.50 (In Vitro CCK-1R Potency)
5497	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-MePhe	Compound 20	8	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	2.6 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.14 (In Vitro CCK-1R Potency)
5498	30624060	2019	DYLGW-Nle-DMeAsp-MePhe	Compound 25	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	45 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.81 (In Vitro CCK-1R Potency)
5499	30624060	2019	GW-Nle-DMeAsp-MePhe	Compound 27	6	Lys(C18d-yGlu-(OEG)2) linker between hydroxyphenylacetic acid and peptide	Amidation	Linear	Mix	Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	7.1 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.80 (In Vitro CCK-1R Potency)
5500	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-MePhe	Compound 30	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	112 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.44 (In Vitro CCK-1R Potency)
5501	30624060	2019	D-sTyr-LGW-Nle-DMeAsp-Me1Nal	Compound 48	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Me1Nal = N-methyl-1-naphthylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	147 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.39 (In Vitro CCK-1R Potency)
5502	30624060	2019	D-sTyr-Nle-GW-Nle-DMeAsp-1Nal	Compound 49	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Me1Nal = N-methyl-1-naphthylalanine	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	140 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.44 (In Vitro CCK-1R Potency)
5503	30624060	2019	βAsp-Phe(4sm)-Nle-GW-Nle-DMeAsp-MePhe	Compound 56	9	yGlu-(OEG)2 linker between C18 fatty acid and peptide	Amidation	Linear	Mix	sTyr = Sulfated Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine, Phe(4sm) = 4-sulfomethylphenylalanine, βAsp at position 1	CCK-8 analogue	Role in the regulation of energy balance	The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h	5 nmol/kg	106 (Terminal Half Life)	Female göttingen minipigs plasma protease	LC-MS	Female göttingen minipigs plasma	In Vivo	None	None	pEC50 = 9.50 (In Vitro CCK-1R Potency)
5581	30684538	2019	LVIWINGDK	Tryptic peptide	9	Free	Free	Linear	L	N23G24	MBP analog	Model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 µM	400 ± 100 (Deamidation Half Life)	Trypsin	LC-MS	WT - MBP	In Vitro	None	None	N.A.
5584	30684538	2019	YENGKYDIK	Tryptic peptide	9	Free	Free	Linear	L	N184G185	MBP analog	Model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 µM	12 ± 1 (Deamidation Half Life)	Trypsin	LC-MS	WT - MBP	In Vitro	None	None	N.A.
5588	30684538	2019	LVIWINGDK	Peptic peptide	9	Free	Free	Linear	L	N23G24	MBP analog	model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 µM	200 ± 40 (Deamidation Half Life)	Pepsin	LC-MS	Mutant MBP	In Vitro	None	None	N.A.
5591	30684538	2019	YENGKYDIK	Peptic peptide	9	Free	Free	Linear	L	N184G185	MBP analog	model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 µM	2.0 ± 0.5 (Deamidation Half Life)	Pepsin	LC-MS	Mutant MBP	In Vitro	None	None	N.A.
5595	30676716	2019	IAVEEEE	APA1	7	SATHA-FBA	Free	Linear	L	R=OMe	Synthetic	Increase half life of H2S	N.A.	0.1 mg/mL	31 ± 8 (H2S Release Half Life)	Dilute APA solution protease	Methylene blue method	Dilute APA solution	In Vitro	None	None	N.A.
5596	30676716	2019	IAVEEEE	APA2	7	SATHA-FBA	Free	Linear	L	R=Me	Synthetic	Increase half life of H2S	N.A.	0.1 mg/mL	22±4 (H2S Release Half Life)	Dilute APA solution protease	Methylene blue method	Dilute APA solution	In Vitro	None	None	N.A.
5597	30676716	2019	IAVEEEE	APA3	7	SATHA-FBA	Free	Linear	L	None	Synthetic	Increase half life of H2S	N.A.	0.1 mg/mL	19±8 (H2S Release Half Life)	Dilute APA solution protease	Methylene blue method	Dilute APA solution	In Vitro	None	None	N.A.
5598	30676716	2019	IAVEEEE	APA4	7	SATHA-FBA	Free	Linear	L	R=F	Synthetic	Increase half life of H2S	N.A.	0.1 mg/mL	14±2 (H2S Release Half Life)	Dilute APA solution protease	Methylene blue method	Dilute APA solution	In Vitro	None	None	N.A.
5599	30676716	2019	IAVEEEE	APA5	7	SATHA-FBA	Free	Linear	L	R=Cl	Synthetic	Increase half life of H2S	N.A.	0.1 mg/mL	13±4 (H2S Release Half Life)	Dilute APA solution protease	Methylene blue method	Dilute APA solution	In Vitro	None	None	N.A.
5601	30344018	2019	N.A.	ASN	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	B. cereus BDRD-ST26 (P43-amyE-BcA)	Production of acrylamide-free food	50 C	N.A.	17.35 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	Km = 9.38 mM
5602	30344018	2019	N.A.	ASN	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	B. cereus BDRD-ST26 (P43-BcA)	Production of acrylamide-free food	50 C	N.A.	17.57 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	km = 9.41 mM
5603	30344018	2019	N.A.	ASN	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	B. subtilis 168	Production of acrylamide-free food	65 C	N.A.	61 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	km = 5.3 mM
5604	30344018	2019	N.A.	ASN	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	T. kodakaraensis 1656	Production of acrylamide-free food	85 C	N.A.	130 (Activity Half Life)	N.A.	N.A.	N.A.	N.A.	None	None	km = 5.5 mM
5613	30684538	2019	VRYNGKL	Tryptic peptide	7	Free	Free	Linear	L	N111G112	MBP analog	Model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 μM	150 ± 10 (Hx Half Life)	Trypsin	Hydrogen Exchange Mass Spectrometry (HX-MS)	WT - MBP	In Vitro	None	None	N.A.
5614	30684538	2019	FKYENGKY	Tryptic peptide	8	Free	Free	Linear	L	N184G185	MBP analog	Model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 μM	<30 (Hx Half Life)	Trypsin	Hydrogen Exchange Mass Spectrometry (HX-MS)	WT - MBP	In Vitro	None	None	N.A.
5623	30684538	2019	VRYNGKL	Peptic peptide	7	Free	Free	Linear	L	N111G112	MBP analog	Model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 μM	130 ± 5 (Hx Half Life)	Pepsin	Hydrogen Exchange Mass Spectrometry (HX-MS)	Mutant MBP	In Vitro	None	None	N.A.
5624	30684538	2019	FKYENGKY	Peptic peptide	8	Free	Free	Linear	L	N184G185	MBP analog	Model protein	Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C	20 μM	<30 (Hx Half Life)	Pepsin	Hydrogen Exchange Mass Spectrometry (HX-MS)	Mutant MBP	In Vitro	None	None	N.A.
5631	30809901	2019	N.A.	FITC-AAR029b	N.A.	Fluorescein isothiocynate labeled	Free	Macrocyclic	L	None	Derived from a class of peptides known as cyclic peptide triazoles (cPTs)	Antiviral	N.A.	0.01 mg/kg	0.029 ± 0.01 (T1/2Α-Distribution Half Life)	Rats plasma protease	Fluorescence assay	Rats plasma	In Vivo	None	None	EC50(nM) = 210±16 for AAR029b in Bal.01 virus
5632	30809901	2019	N.A.	FITC-AAR029b in Liposome	N.A.	Fluorescein isothiocynate labeled	Free	Macrocyclic	L	None	Derived from a class of peptides known as cyclic peptide triazoles (cPTs)	Antiviral	N.A.	0.01 mg/kg	0.032 ± 0.005 (T1/2Α-Distribution Half Life)	Rats plasma protease	Fluorescence assay	Rats plasma	In Vivo	None	None	EC50(nM) = 210±16 for AAR029b in Bal.01 virus
5633	30565900	2018	RGD	DOX@PLEPMPss-cRGD	3	PCL-PEG	Free	Cyclic (N-C terminal end)	L	None	Synthetic	Anticancer	The plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h)	2 mg/kg	11.81 ± 0.67 (T1/2b)	Mice plasma protease	fluorescence spectrometry	mice plasma	In Vivo	None	None	The IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1
5634	30565900	2018	RGD	DOX@Cu-PLEPMPss-cRGD	3	PCL-PEG	Free	Cyclic (N-C terminal end)	L	None	Synthetic	Anticancer	The plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h)	2 mg/kg	12.20 ± 0.73 (T1/2b)	Mice plasma protease	fluorescence spectrometry	mice plasma	In Vivo	None	None	The IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1
5642	30314880	2018	RK	SA-5K	2	Stearic acid conjugation	Substituition of Phe with Lys at C terminal	Linear	L	chemical group (S)-3-amino-3-(1-naphthyl)-propionic acid- conjugated between R1 and Lys2	Synthetic	Anticancer	0, 15, 30, min, 1, 2, 6, 12, 24 h	2 mM	5	Human serum protease	HPLC, MS	Human serum	In Vitro	None	None	IC50 μM = 1.0 ± 0.05 for SA-5 in BT-474
5643	30314880	2018	RF	Compound 5	2	Free	Free	Linear	L	chemical group (S)-3-amino-3-(1-naphthyl)-propionic acid- conjugated between R1 and F2	Synthetic	Anticancer, Antiproliferative	0, 15, 30, min, 1, 2, 6, 12, 24 h	2 mM	2	Human serum protease	HPLC, MS	Human serum	In Vitro	None	None	IC50 μM = 0.895 ±0.029 for compound 5 in BT-474
5652	30175919	2018	GRP-MeArg-AFTF-MeAla	Electroporation peptide	9	6FAM labelled	Free	Linear	L	MeAla, MeArg	Synthetic	Substrate reporter for PKB	RT	35 µM	53 ± 15	N.A.	N.A.	Axenic D. discoideum K-AX3 SorCM buffer after electroporation	In Vitro	None	None	N.A.
5653	30175919	2018	GRP-MeArg-AFTF-MeAla	Pinocystosis peptide	9	6FAM labelled	Free	Linear	L	MeAla, MeArg	Synthetic	Substrate reporter for PKB	RT	150 µM	19 ± 2	N.A.	N.A.	Axenic D. discoideum K-AX3 DB after pinocytosis	In Vitro	None	None	N.A.
5725	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	27 ± 1	NEP (5.687 Nm)	RP-HPLC	Tris–HCl buffer (50 mM, pH 7.4)	In Vitro	None	None	N.A.
5726	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	78 ± 2	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM Sialorphin inhibitor	In Vitro	None	None	N.A.
5727	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	94 ± 2	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM Opiorphin inhibitor	In Vitro	None	None	N.A.
5728	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	47 ± 1	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Ala1]sialorphin inhibitor	In Vitro	None	None	N.A.
5729	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	74 ± 2	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Ala2]sialorphin inhibitor	In Vitro	None	None	N.A.
5730	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	109 ± 8	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Ala3]sialorphin inhibitor	In Vitro	None	None	N.A.
5731	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	42 ± 2	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM[Ala4]sialorphin inhibitor	In Vitro	None	None	N.A.
5732	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	52 ± 2	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Ala5]sialorphin inhibitor	In Vitro	None	None	N.A.
5733	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	116 ± 1	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [His2]opiorphin inhibitor	In Vitro	None	None	N.A.
5734	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	53 ± 1	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Ser4]sialorphin inhibitor	In Vitro	None	None	N.A.
5735	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	114 ± 2	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Arg2]sialorphin inhibitor	In Vitro	None	None	N.A.
5736	29752565	2018	YGGFM	Met-enkephalin	5	Free	Met substituition at C terminal	Linear	L	None	Synthetic	Involved in the pain modulating mechanism in the spinal cord	Incubated over 0, 30, 60, 90, 120 min at 37 °C	0.0413 mM	139 ± 3	NEP (5.687 Nm)	RP-HPLC	Tris HCl buffer with 0.156 mM [Pro4]opiorphin inhibitor	In Vitro	None	None	N.A.
5739	29732120	2018	RGDfV	Analogue 6	5	Free	Free	Macrocyclic (N-C terminal end)	Mix	D-Phe	Synthetic	Inhibits pro-angiogenic integrins	At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h)	1 mg/ml	9	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50(μM) = 140 ± 95 against αvβ3
5740	29732120	2018	RGDFV	Analogue 12	5	Free	Free	Macrocyclic (N-C terminal end)	L	None	Synthetic	Inhibits pro-angiogenic integrins	At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h)	1 mg/ml	7	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50(μM) = 166 ± 98 against αvβ3
5741	29732120	2018	RGDfV, RGDfV	Analogue 11 and 9b	5	Free	Free	Macrocyclic (N-C terminal end)	Mix	Thio substiuition in Asp (analogue 11) and Phe (analogue 9b)	Synthetic	Inhibits pro-angiogenic integrins	At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h)	1 mg/ml	36	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 value of 11 shows that 11 is poorer than Cilen
5742	29732120	2018	RGDfV	Cilen	5	Free	Free	Macrocyclic (N-C terminal end)	Mix	Methylation at Phenylalanine (D-form)	Synthetic	Glioblastoma therapy	At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h)	1 mg/ml	12	Human serum protease	HPLC	Human serum	In Vitro	None	None	IC50 value of 11 shows that 11 is poorer than Cilen
5749	29685037	2018	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Ang-(1-7)	Decrease brain ROS production and inflammation in preclinical models of HF	15 h at 37°C	100 µM	13.8 ± 5.7	Rats serum protease	HPLC	Rats serum	In Vitro	None	None	Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5750	29685037	2018	DRYVIHP	Ang-AA	7	Acetylation	Amidation	Linear	L	None	Ang-(1-7) analogs	Antifibrosis, Antihypertension, Antihypertrophic and Antiarrhythmia Activities	15 h at 37°C	100 µM	171.1 ± 40.7	Rats serum protease	HPLC	Rats serum	In Vitro	None	None	Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5751	29685037	2018	DRYVIHP	Ang-AA	7	Acetylation	Amidation	Linear	L	None	Ang-(1-7) analogs	Antifibrosis, Antihypertension, Antihypertrophic and Antiarrhythmia Activities	After a 30 min incubation at 37°C	0.1 mM	135.7 ± 37.7	ACE, LAP and NEP	HPLC	PBS solution containing all three hydrolytic enzymes (0.5 IU/mL), ACE, LAP and NEP	In Vitro	None	None	Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5752	29685037	2018	DRVYIHP	Ang-(1-7)	7	Free	Free	Linear	L	None	Ang-(1-7)	Decrease brain ROS production and inflammation in preclinical models of HF	After a 30 min incubation at 37°C	0.1 mM	9.2 ± 0.5	ACE, LAP and NEP	HPLC	PBS solution containing all three hydrolytic enzymes (0.5 IU/mL), ACE, LAP and NEP	In Vitro	None	None	Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5753	29685037	2018	DRYVIHP	Ang-AA	7	Acetylation	Amidation	Linear	L	None	Ang-(1-7) analogs	Antifibrosis, Antihypertension, Antihypertrophic and Antiarrhythmia Activities	At 2, 4, 6, 8, 10, 15, 50, 120, 240, 480, 720 and 960 min after the injection, 100 µL of blood were sampled from each animal through the caudal vein	400 µg/kg	238.7 ± 61.3	Rats serum protease	RP-HPLC	Rats serum	In Vivo	None	None	Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5773	29602308	2018	HSTPSSP	P4-Chlorambucil	7	Free	Chlorambucil	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	21.5	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5774	29602308	2018	HSTPSSP	P4-Chlorambucil	7	Free	Chlorambucil	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	12.4	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5775	29602308	2018	HSTPSSP	P4-Melphalan	7	Free	Melphalan	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	24.6	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5776	29602308	2018	HSTPSSP	P4-Melphalan	7	Free	Melphalan	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	10.6	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5777	29602308	2018	HSTPSSP	P4-Bendamustine	7	Free	Bendamustine	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	19.3	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5778	29602308	2018	HSTPSSP	P4-Bendamustine	7	Free	Bendamustine	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	15.4	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5779	29602308	2018	HSTPSSP	P4-Chlorambucil-PEG-AuNP	7	Free	Chlorambucil	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	21	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5780	29602308	2018	HSTPSSP	P4-Chlorambucil-PEG-AuNP	7	Free	Chlorambucil	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	20	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5781	29602308	2018	HSTPSSP	P4-Melphalan-PEG-AuNP	7	Free	Melphalan	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	22	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5782	29602308	2018	HSTPSSP	P4-Melphalan-PEG-AuNP	7	Free	Melphalan	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	18.3	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5783	29602308	2018	HSTPSSP	P4-Bendamustine-PEG-AuNP	7	Free	Bendamustine	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	22.3	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5784	29602308	2018	HSTPSSP	P4-Bendamustine-PEG-AuNP	7	Free	Bendamustine	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	18.3	Mouse liver homogenate protease	BCA protein assay	Mouse liver homogenate	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5794	29531858	2018	KCRGDCFC	[68Ga]Ga-DOTA-RGD	8	CH2CO chemical group attached, DOTA conjugated with Lys1	CCPEG	Cyclic (C2-C6 Disulfide Bond)	L	68Ga labelling	Synthetic	PET imaging agent to visualize and quantify angiogenesis	Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection	N.A.	24.6 (Slow Phase)	NHP plasma protease	UV-HPLC and LC-ESI-MS	NHP uterus plasma without NC-100717	N.A.	None	None	N.A.
5795	29531858	2018	KCRGDCFC	[68Ga]Ga-DOTA-RGD	8	CH2CO chemical group attached, DOTA conjugated with Lys1	CCPEG	Cyclic (C2-C6 Disulfide Bond)	L	68Ga labelling	Synthetic	PET imaging agent to visualize and quantify angiogenesis	Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection	N.A.	1.1 (Fast Phase)	NHP plasma protease	UV-HPLC and LC-ESI-MS	NHP uterus plasma without NC-100717	N.A.	None	None	N.A.
5796	29531858	2018	KCRGDCFC	[68Ga]Ga-DOTA-RGD	8	CH2CO chemical group attached, DOTA conjugated with Lys1	CCPEG	Cyclic (C2-C6 Disulfide Bond)	L	68Ga labelling	Synthetic	PET imaging agent to visualize and quantify angiogenesis	Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection	1 mg/kg	26.4 (Slow Phase)	NHP plasma protease	UV-HPLC and LC-ESI-MS	NHP uterus plasma after administration of NC-100717 (1 mg/kg)	In Vivo	None	None	N.A.
5797	29531858	2018	KCRGDCFC	[68Ga]Ga-DOTA-RGD	8	CH2CO chemical group attached, DOTA conjugated with Lys1	CCPEG	Cyclic (C2-C6 Disulfide Bond)	L	68Ga labelling	Synthetic	PET imaging agent to visualize and quantify angiogenesis	Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection	1 mg/kg	1.9 (Fast Phase)	NHP plasma protease	UV-HPLC and LC-ESI-MS	NHP uterus plasma after administration of NC-100717 (1 mg/kg)	In Vivo	None	None	N.A.
5875	29335522	2018	N.A.	PAK2	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Role in PDAC cancer invasion and metastasis	N.A.	N.A.	4.5	Miapaca-2 cell lysate protease	Western blotting	Miapaca-2 cells lysate after PKM2 depletion (treated with 20 μg/ml cycloheximide (CHX))	In Vitro	None	None	N.A.
5876	29335522	2018	N.A.	PAK2	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Role in PDAC cancer invasion and metastasis	N.A.	N.A.	>24	Miapaca-2 cell lysate protease	Western blotting	Miapaca-2 cells lysate with PKM2 expression (treated with 20 μg/ml cycloheximide (CHX))	In Vitro	None	None	N.A.
5877	29329072	2018	YFLFRPRN	Compound 1	8	Free	Amidation	Linear	L	None	NMU-analogs	Regulation of Feeding Behavior, the stress response and nociception	37 °C	112 µM	4.3 ± 0.2	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 38.9, IC50(nM) = 0.78 for hNMUR1 and EC50(nM) = 30.8, IC50(nM) = 1.7 for hNMUR2
5878	29329072	2018	YFLFRPRN	Compound 2	8	Acetylation	Amidation	Linear	L	None	NMU-analogs	Regulation of Feeding Behavior, the stress response and nociception	37 °C	112 µM	117.8 ± 0.7	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	N.A.
5879	29329072	2018	FLFRPRN	Compound 16	7	Acetylation, 7-OH-Tic = 7-hydroxy-L-1,2,3,4- tetrahydroisoquinoline-3-carboxylic acid at position 1	Amidation	Linear	L	None	NMU-analogs	Regulation of Feeding Behavior, the stress response and nociception	37 °C	112 µM	109.8 ± 3.1	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 5.1, IC50(nM) = 0.037 for hNMUR1 and EC50(nM) = 13.4, IC50(nM) = 12.3 for hNMUR2
5880	29329072	2018	FLFRPRN	Compound 18	8	Ac-2'NaI = 2’-naphtylalanine at position 1	Amidation	Linear	L	None	NMU-analogs	Regulation of Feeding Behavior, the stress response and nociception	37 °C	112 µM	128.8 ± 1.7	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 1.6, IC50(nM) = 0.88 for hNMUR1 and EC50(nM) = 1.6, IC50(nM) = 5.6 for hNMUR2
5881	29329072	2018	YFL-Dmt-RPRN	Compound 28	8	Acetylation	Amidation	Linear	L	Dmt = 2',6'-dimethyltyrosine at position 4	NMU-analogs	Regulation Of Feeding Behavior, The Stress Response And Nociception	37 °C	112 µM	253.5 ± 6	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 7.7, IC50(nM) = 0.36 for hNMUR1 and EC50(nM) = 3675, IC50(nM) = 1857 for hNMUR2
5882	29329072	2018	YFLNGRPRN	Compound 32	8	Acetylation	Amidation	Linear	L	N(benzyl)Gly modfication at position 4	NMU-analogs	Regulation Of Feeding Behavior, The Stress Response And Nociception	37 °C	112 µM	837.4 ± 27.8	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 172.2, IC50(nM) = 83.1 for hNMUR1 and EC50(nM) = 1278, IC50(nM) = 1019 for hNMUR2
5883	29329072	2018	YFLNGRPRN	Compound 38	8	Acetylation	Amidation	Linear	L	N(4-OH-Phenethyl)Gly at position 4	NMU-analogs	Regulation Of Feeding Behavior, The Stress Response And Nociception	37 °C	112 µM	1096.1 ± 56.1	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 216.6, IC50(nM) = 3.9 for hNMUR1 and EC50(nM) = 339.2, IC50(nM) = 206.9 for hNMUR2
5884	29329072	2018	YFLFRRN	Compound 42	7	Acetylation	Amidation	Linear	L	Oic = octahydroindole carboxylic acid modification between R5 and R6	NMU-analogs	Regulation Of Feeding Behavior, The Stress Response And Nociception	37 °C	112 µM	1426.1 ± 67.4	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 28.8, IC50(nM) = 11.2 for hNMUR1 and EC50(nM) = 1.8, IC50(nM) = 13.9 for hNMUR2
5885	29282303	2018	SIINFEKL	SCRAP-mCherry	N.A.	DD	mCherry	N.A.	L	None	Synthetic	Affects Antigen Presentation	N.A.	N.A.	41 ± 5	El4 cells protease	BD cytoflex flow cytometry	EL4 cells after Shield-1 removal	N.A.	None	None	N.A.
5894	29104145	2018	ATWLPPR	AS16-Fc	7	Free	Fc	Linear	L	None	Fusion protein of AS16 and Fc	Antitumor	Blood samples were taken at 0 min, 5min,30 min, 2 h, 4 h, 6 h, 8 h, 10 h and 24h from orbit	45 mg/kg	231	Rats serum protease	ELISA	Rats serum	In Vivo	https://sci-hub.st/10.1016/j.peptides.2010.01.007	None	The activity value of AS16-Fc, as observed in vivo, is its significant inhibition of tumor growth and reduction in M2-polarized macrophages and vessel density in the MCA-205 tumor model
5895	29104145	2018	ATWLPPR	AS16	7	Free	Free	Linear	L	None	Synthetic	Antitumor	Blood samples were taken at 0 min, 5min,30 min, 2 h, 4 h, 6 h, 8 h, 10 h and 24h from orbit	45 mg/kg	1	Rats serum protease	ELISA	Rats serum	In Vivo	None	None	The activity value of AS16-Fc, as observed in vivo, is its significant inhibition of tumor growth and reduction in M2-polarized macrophages and vessel density in the MCA-205 tumor model
5916	29633613	2018	N.A.	ThXylC	N.A.	Free	Free	Linear	L	None	Obtained from the soluble fractions of the recombinant E. coli BL21(DE3) cells	β-xylosidase	65 °C	N.A.	8.9 (Activity Half Life)	N.A.	N.A.	ThXylC	In Vitro	None	None	N.A.
5917	29633613	2018	N.A.	ThXylC-ELK	N.A.	Free	ELK16 short peptide was introduced to the C-terminus of ThXylC	Linear	L	None	Obtained from the soluble fractions of the recombinant E. coli BL21(DE3) cells	β-xylosidase	65 °C	N.A.	54.8 (Activity Half Life)	N.A.	N.A.	ThXylC-ELK	In Vitro	None	None	N.A.
5922	29373818	2018	N.A.	fibrinolytic enzyme	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	From the marine Serratia marcescens subsp sakuensis	Clot lysis	37 °C	N.A.	19 (Activity Half Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
5923	29373818	2018	N.A.	fibrinolytic enzyme	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	From the marine Serratia marcescens subsp sakuensis	Clot lysis	50°C	N.A.	29 (Activity Half Life)	N.A.	N.A.	N.A.	In Vitro	None	None	N.A.
5977	28714475	2017	EYEKEYE	Tag	7	Fluorescein (F)	Amidation	Linear	L	Lys4 linked with Palm fatty acid	Synthetic	Increases Half Life	N.A.	0.25 mg/kg	1.5 ± 0.4 (T1/2a)	Rats plasma protease	RP-HPLC using a fluorescence detector	Rats plasma	In Vivo	None	None	Albumin binding (Kd) (nM) = 220±30 for rat albumin
5978	28714475	2017	EYEKEYE	Tag	7	Fluorescein (F)	Amidation	Linear	L	Lys4 linked with Palm fatty acid	Synthetic	Increases Half Life	N.A.	0.25 mg/kg	12.3 ± 0.4 (T1/2b)	Rats plasma protease	RP-HPLC using a fluorescence detector	Rats plasma	In Vivo	None	None	Albumin binding (Kd) (nM) = 220±30 for rat albumin
5979	28714475	2017	EYEK(C14)EYE-(PEG24)3-XCFRLPCRQLRC	tag-3xPEG24-FXIIa inhibitor	N.A.	Tag-3xPEG24	Amidation	Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor)	L	None	Synthetic	FXIIa Inhibitor	N.A.	5 mg/kg	1.0 ± 0.2 (T1/2a)	Rabbit plasma protease	RP-HPLC using fluorescence detector	Rabbit plasma	In Vivo	None	None	(EC5x) at 4.2±0.5 mM
5980	28714475	2017	EYEK(C14)EYE-(PEG24)3-XCFRLPCRQLRC	tag-3xPEG24-FXIIa inhibitor	N.A.	Tag-3xPEG24	Amidation	Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor)	L	None	Synthetic	FXIIa Inhibitor	N.A.	5 mg/kg	5.2 ± 0.4 (T1/2b)	Rabbit plasma protease	RP-HPLC using fluorescence detector	Rabbit plasma	In Vivo	None	None	(EC5x) at 4.2±0.5 mM
5981	28714475	2017	XCFRLPCRQLRC	FXIIa inhibitor	N.A.	Fluorescein (F)	Amidation	Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor)	L	None	Synthetic	FXIIa Inhibitor	N.A.	3.7 mg/kg	0.21 ± 0.04 (T1/2b)	Rabbit plasma protease	A single quadrupole liquid chromatography mass spectrometer	Rabbit plasma	In Vivo	None	None	Ki FXIIa = 4±0.9 nM in presence of albumin
5986	28691076	2017	wLwReQeR	Cyclic D,L-α-Peptides	8	Free	free	Cyclic	Mix	D-amino acid substituitons	Synthetic	Antiatherosclerotic	Blood was drawn (30–60 μL) from the retro-orbital sinus into a heparinized capillary tube before dosing (0 min) and at different intervals from 30 min to 8 h after dosing	20 g	6	BALB/c mouse plasma protease	LC-MS/SIM	BALB/c mouse plasma	In Vivo	None	None	cytotoxicity LD50 (μM) = 36 for NCI
5990	28623878	2017	FEFKFEFKK	FITC-F9 hydrogel	9	Fluoresceinisothiocyanate labelled	Free	Linear	L	None	F9 analogue	Therapeutic drug delivery	5 days	0.01 M	1 to 4	Mice plasma protease	fluorescence assay	Mice plasma	In Vivo	None	None	N.A.
6022	28416744	2017	RGDyK	cRGD-ZW800-1	5	Free	ZW800-1 fluorophore	Cyclic (RGDyK)	Mix	y = D-Tyr	Synthetic	Generic tracer for Intraoperative Near-Infrared Fluorescence Imaging of Solid Tumors	Time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection	10 nmol	25.3 ± 6.4	Mice serum protease	Fluorescence assay	Mice serum	In Vivo	None	None	In vitro competition for binding cRGD-ZW800-1 (500 nM) with a 1:1 molar ratio of unlabeled cRGD (500 nM) resulted in a reduction of 32% on the HT-29 cells and 36% on the high integrin-expressing U-87 MG cells compared to cells treated without unlabeled cRGD
6023	28416744	2017	RGDyK	cRGD-ZW800-1	5	Free	ZW800-1 fluorophore	Cyclic (RGDyK)	Mix	y = D-Tyr	Synthetic	Generic tracer for Intraoperative Near-Infrared Fluorescence Imaging of Solid Tumors	Time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection	10 nmol	71.1 ± 9.4 (Terminal Half Life)	Mice serum protease	Fluorescence assay	Mice serum	In Vivo	None	None	In vitro competition for binding cRGD-ZW800-1 (500 nM) with a 1:1 molar ratio of unlabeled cRGD (500 nM) resulted in a reduction of 32% on the HT-29 cells and 36% on the high integrin-expressing U-87 MG cells compared to cells treated without unlabeled cRGD
6047	28068664	2017	N.A.	scFv57R	N.A.	Free	Free	Linear	L	None	Synthetic	Antiviral (against Rabies Virus)	37o C for 0-72 hours	0.5 mg/ml	14.1	N.A.	ELISA	PBS	In Vitro	None	None	Neutralizing potency (IU/ml) = 83.8 ± 9.4 for monomer
6048	28068664	2017	DPDNEAYEMPSEEGYQDYEPEA	scFv57R-ATS	N.A.	Free	(ATS) was fused to the C-terminus of the anti-RV scFv57R	Linear	L	None	scFv57R-ATS fusion protein	Antiviral (against Rabies Virus)	37o C for 0-72 hours	0.5 mg/ml	33.9	N.A.	ELISA	PBS	In Vitro	None	None	Neutralizing potency (IU/ml) = 2.9 ± 0.5 for polymer
6049	28068664	2017	DPDNEAYEMPSEEGYQDYEPEA	scFv57R-ATS	N.A.	Free	(ATS) was fused to the C-terminus of the anti-RV scFv57R	Linear	L	None	scFv57R-ATS fusion protein	Antiviral (against Rabies Virus)	37o C	0.5 mg/ml	15.6	Mouse serum protease	ELISA	Mouse serum	In Vitro	None	None	Neutralizing potency (IU/ml) = 2.9 ± 0.5 for polymer
6050	28065871	2017	RGDyK	DOX-cRGD30-RCCMs	5	Free	RCCMs	Cyclic (RGDyK)	Mix	y = D-Tyr	Synthetic	Antitumor	-4 C for 10 h	10 mg DOX equiv./kg	4.7 (T1/2,b)	Kunming mice retro-orbital sinus protease	Fluorescence assay	Kunming mice retro-orbital sinus	In Vivo	None	None	IC50 value for DOX-cRGD30-RCCMs is 1.9 µg/mL
6051	28065871	2017	RGDyK	DOX-cRGD30-PEG-PCL	5	Free	PEG-PLC	Cyclic (RGDyK)	Mix	y = D-Tyr	Synthetic	Antitumor	-4 C for 10 h	10 mg DOX equiv./kg	1.2 (T1/2,b)	Kunming mice retro-orbital sinus protease	Fluorescence assay	Kunming mice retro-orbital sinus	In Vivo	None	None	N.A.
6052	28010844	2017	fCFwKTCT	Octreotide	8	D-amino acid Phe	Free	Cyclic (C2-C7 Disulfide Linkage)	Mix	D-amino acid substituitons Trp	SST analog	Anticancer and treatment of Endocrine Diseases	The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min	50 mg/kg	28	Mouse stomach tissue lysate protease	HPLC-MS	Mouse stomach tissue lysate	In Vivo	https://sci-hub.st/10.1177/106002808802201001	None	N.A.
6053	28010844	2017	fCFwKTCT	Octreotide	8	D-amino acid Phe	Free	Cyclic (C2-C7 Disulfide Linkage)	Mix	D-amino acid substituitons Trp	SST analog	Anticancer and treatment of Endocrine Diseases	The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min	50 mg/kg	37.7	Mouse intestine tissue lysate protease	MALDI-TOF-MSI and LC-MS/MS	Mouse intestine tissue lysate	In Vivo	None	None	N.A.
6054	28005375	2017	PHSCN	DOX-ATN/SCID-Ps	5	Acetylation	PEG-P(TMC-DTC)	Linear	Mix	None	Synthetic	Anticancer	N.A.	150 μL	4.13 (Elimination Half Life)	Kunming mice retro-orbital sinus protease	Fluorescence assay	Kunming mice retro-orbital sinus blood	In Vivo	None	None	DOX-ATN56/SCID-Ps revealed a low IC50 of 5.2 μg/mL to B16F10 cells
6055	27990643	2017	VSRRR	CN-105	5	Acetylation	Amidation	Linear	L	None	APOE-derived peptide	Treatment of Spontaneous Intracranial Hemorrhage (Ich)	Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing	0.01 mg/kg	2.3 ± 0.5	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC5054364/	None	N.A.
6056	27990643	2017	VSRRR	CN-105	5	Acetylation	Amidation	Linear	L	None	APOE-derived peptide	Treatment of Spontaneous Intracranial Hemorrhage (Ich)	Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing	0.03 mg/kg	2.4 ± 0.5	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	None	None	N.A.
6057	27990643	2017	VSRRR	CN-105	5	Acetylation	Amidation	Linear	L	None	APOE-derived peptide	Treatment Of Spontaneous Intracranial Hemorrhage (Ich)	Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing	0.1 mg/kg	3.3 ± 0.6	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	None	None	N.A.
6058	27990643	2017	VSRRR	CN-105	5	Acetylation	Amidation	Linear	L	None	APOE-derived peptide	Treatment Of Spontaneous Intracranial Hemorrhage (Ich)	Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing	0.3 mg/kg	3.6 ± .4	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	None	None	N.A.
6059	27990643	2017	VSRRR	CN-105	5	Acetylation	Amidation	Linear	L	None	APOE-derived peptide	Treatment Of Spontaneous Intracranial Hemorrhage (Ich)	Blood samples were taken at 15 minutes prior to start of dosing and at 0.083, 0.167, 0.5, 1, 2, 4, 8, 12, and 24 hours from the start of dosing	1 mg/kg	3.5 ± 0.3	Human plasma protease	LC-MS/MS	Human plasma	In Vivo	None	None	N.A.
6078	27689406	2017	N.A.	X1	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Antiobesity	N.A.	N.A.	3.9	Surgical rats plasma protease (Wistar Rat)	RIA	Surgical rats plasma (Wistar rat)	In Vivo	None	None	N.A.
6079	27689406	2017	N.A.	X2	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Antiobesity	N.A.	N.A.	16.1	Surgical rats plasma protease (Wistar Rat)	RIA	Surgical rats plasma (Wistar rat)	In Vivo	None	None	N.A.
6080	27689406	2017	N.A.	X3	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Antiobesity	N.A.	N.A.	21.3	Surgical rats plasma protease (Wistar Rat)	RIA	Surgical rats plasma (Wistar rat)	In Vivo	None	None	N.A.
6096	28416744	2017	RGDyK	cRGD-ZW800-1	5	Free	Zw800-1	Cyclic (RGDyK)	Mix	y = D-Tyr, cyclic peptide linked with ZW800-1	Synthetic	Generic tracer for intraoperative near-infrared fluorescence imaging of solid tumors	time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection	10 nmol	14.6 ± 1.7 (Distribution Half Life)	Mice serum protease	Fluorescence assay	Mice serum	In Vivo	None	None	N.A.
6104	27656777	2016	CMPRLRGC	VH434	8	Acetylation	Amidation	Cyclic (C1-C8 Disulfide Bond)	L	None	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	1.16	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	KD = 196 nM
6105	27656777	2016	cMPRLRGC	VH445	8	Acetylation	Amidation	Cyclic (C1-C8 Disulfide Bond)	Mix	c = D-Cys at position 1	VH445	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	3.03	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	KD = 76 nM
6106	27656777	2016	(D-Pen)-M-Thz-RLRGC	VH4106	8	Acetylation	Amidation	Cyclic	Mix	Pen, Thz = Penicillamine, Thiazolidine	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	1.89	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	KD = 9 nM
6107	27656777	2016	cM-Thz-RLRG-Pen	VH4127	8	Pr = propionylation, c = D-Cys at N terminal	Amidation	Cyclic	Mix	Pen, Thz = non-natural amino acid	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	4.27	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	KD = 18 nM
6108	27656777	2016	cM-Thz-RLR-Sar-Pen	VH4128	8	Pr = propionylation, c = D-Cys at N terminal	Amidation	Cyclic	Mix	c = D-Cys and Pen, Thz, Sar = non-natural amino acid	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	4.35	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130
6109	27656777	2016	cM-Pip-RLR-Sar-C	VH4129	8	Pr = propionylation, c = D-Cys at N terminal	Amidation	Cyclic (C1-C8 Disulfide Bond)	Mix	c = D-Cys and Sar modification , Pip = Pipecolic acid	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	6.66	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	N.A.
6110	27656777	2016	cM-Pip-RLRG-Pen	VH4130	8	Pr = propionylation, c = D-Cys at N terminal	Amidation	Cyclic	Mix	c = D-Cys and Pen, Pip = non-natural amino acid	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	4.03	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130
6111	27656777	2016	cM-Pip-RLR-Sar-Pen	VH4131	8	Pr = propionylation, c = D-Cys at N terminal	Amidation	Cyclic	Mix	c = D-Cys and Sar,Pen, Pip = non-natural amino acid	VH445 analogues	Vectors targeting the LDL receptor	Incubated at 4°C or 37°C	2 µM	10	Mouse plasma protease	LC-MS/MS	(CD-1) mouse plasma	In Vitro	None	None	Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130
6129	27217590	2016	CYIQNCPLG	OT (oxytocin)	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	None	Produced in the hypothalamus and released by the posterior pituitary gland	Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia	Time points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours	0.1 mg/kg	0.12	Wistar rats plasma protease	LC-MS/MS	Wistar rats plasma	In Vivo	https://sci-hub.st/10.1016/s0079-6123(08)00417-2	None	EC50(nM) = 0.039 (OTR agonist)
6130	27217590	2016	CYIQNCGKG	PF1	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid	OT analog	Non–brain-penetrant OT receptor agonist	Time points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours	0.1 mg/kg	8.5	Wistar rats plasma protease	LC-MS/MS	Wistar rats plasma	In Vivo	None	None	EC50(nM) = 0.025 (OTR agonist)
6131	27217590	2016	CYIQNCGKG	PF1	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid	OT analog	Non–brain-penetrant OT receptor agonist	Time points postdose: 0.25 (OT only), 0.5, 1, 2, 4, 6, and 24 hours (6- and 24-hour sampling limited to PF1 only)	4 ml/kg	3.2	C57Bl/6J mice plasma protease	LC-MS/MS	C57BL/6J mice plasma	In Vivo	None	None	EC50(nM) = 0.025 (OTR agonist)
6132	27217590	2016	CYIQNCPLG	OT (oxytocin)	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	None	Produced in the hypothalamus and released by the posterior pituitary gland	Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia	Time points postdose: 0.25 (OT only), 0.5, 1, 2, 4, 6, and 24 hours (6- and 24-hour sampling limited to PF1 only	10 ml/kg	0.5	C57Bl/6J mice plasma protease	LC-MS/MS	C57BL/6J mice plasma	In Vivo	PDB id: 2MGO	None	EC50(nM) = 0.039 (OTR agonist)
6133	27217590	2016	CYIQNCGKG	PF1	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid	OT analog	Non–brain-penetrant OT receptor agonist	Serial blood samples were collected from each mouse via the retro-orbital sinus at the following time points postdose: 0.5, 1, 2, 4, 6, and 24 hours	20 mg/kg	309	C57Bl/6J mice plasma protease	LC-MS/MS	C57BL/6J mice plasma	In Vivo	None	None	EC50(nM) = 0.025 (OTR agonist)
6134	27217590	2016	CYIQNCPLG	OT (oxytocin)	9	Free	Amidation	Cyclic (C1-C6 Disulfide Linkage)	L	None	Produced in the hypothalamus and released by the posterior pituitary gland	Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia	Serial blood samples were collected from each mouse via the retro-orbital sinus at the following time points postdose: 0.5, 1, 2, 4, 6, and 24 hours	20 mg/kg	7.3	C57Bl/6J mice plasma protease	LC-MS/MS	C57BL/6J mice plasma	In Vivo	None	None	EC50(nM) = 0.039 (OTR agonist)
6148	32263229	2016	RGDfC	iT-P/PTX NPs	5	Free	TPGS(D-a-tocopherol polyethylene glycol succinate) linked with poly(lactide) using disulfide linkage, cRGD further conjugated to NP surface	Cyclic (RGDfC)	Mix	D-Phe at position 4	Synthetic	Anticancer	Blood samples were collected in EP tubes containing 20 mL of 1000 U heparin per mL at 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h for each group.	10 mg/ kg	12.68 ± 0.81	SD rats plasma protease	HPLC	SD rats plasma	In Vivo	None	None	IC50 = 1.90 ± 0.28 mg/mL incubated with A2780 cell
6149	26982623	2016	KKWWKKW-Dip-K	Peptide -5 (LTX-315)	9	Free	Amidation	Linear	L	Replacing Trp8 with the more bulky unnatural Dip = Diphenyalanine	Synthetic	Anticancer	100 µl samples were taken after 0, 10, 20, 45 and 90 min	1 µM	71	Cryopreserved rats hepatocyte protease	LC-MS/MS	Cryopreserved rats hepatocytes at a cell density of 0.5 million cells/ml	In Vitro	None	None	IC50 ± SD in µM = 34.3 ± 2.3 for MRC-5 cells
6150	26982623	2016	KKWWKKW-Dip-K	Peptide -5 (LTX-315)	9	Free	Amidation	Linear	L	Replacing Trp8 with the more bulky unnatural Dip = Diphenyalanine	Synthetic	Anticancer	100 µl samples were taken after 0, 10, 20, 45 and 90 min	1 µM	64	Cryopreserved rats hepatocyte protease	LC-MS/MS	Cryopreserved rats hepatocytes at a cell density of 0.5 million cells/ml	In Vitro	None	None	IC50 ± SD in µM = 34.3 ± 2.3 for MRC-5 cells
6183	26741458	2016	FEFQFK	Peptide 1	6	Free	Free	Linear	L	None	Synthetic	Hydrogelators	Degradation was monitored after 0, 1, 2, 3, 4, 5, and 10 min	34 μM	3.43 ± 0.06	Human blood plasma protease	HPLC	Human blood plasma	In Vitro	None	None	N.A.
6184	26741458	2016	FE-β3hF-FQ-β3hF-FK	Peptide 2	8	Free	Free	Linear	L	β3-homophenylalanine (β3-hPhe) at position 3 and 6	Synthetic	Hydrogelators	During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min.	33 μM	19.53 ± 0.55	Human blood plasma protease	HPLC	Human blood plasma	In Vitro	None	None	N.A.
6185	26741458	2016	FE-β3hF-FQ-β3hF-FK	Peptide 3	8	Free	Amidation	Linear	L	β3-homophenylalanine (β3-hPhe) at position 3 and 6	Synthetic	Hydrogelators	During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min.	33 μM	40.00 ± 1.28	Human blood plasma protease	HPLC	Human blood plasma	In Vitro	None	None	N.A.
6186	26741458	2016	FE-β3hF-YQ-β3hF-YK	Peptide 4	8	Free	Amidation	Linear	L	β3-homophenylalanine (β3-hPhe) at position 3 and 6, substitution of Phe with Tyr at positions 4 and 7	Synthetic	Hydrogelators	During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min.	33 μM	18.71 ± 0.44	Human blood plasma protease	HPLC	Human blood plasma	In Vitro	None	None	N.A.
6223	26628555	2016	TGENHR	HLDF-6-NH2	6	3H labeling at N terminal	Amidation	Linear	L	None	Isolated from the culture medium of retinoic acid-treated HL-60 cells	Neuroprotective And Nootropic Activities	N.A.	N.A.	8	Wistar rats blood plasma protease	N.A.	Wistar rats blood plasma	In Vivo	None	None	ChAT activity, dpm/mg of tissue = 5.61±0.40 in (βA + HLDF-6-NH2,250 µg/kg)
6224	26628555	2016	TGENHR	HLDF-6-OH	6	3H labeling at N terminal	Free	Linear	L	None	Isolated from the culture medium of retinoic acid-treated HL-60 cells	Neuroprotective And Nootropic Activities	N.A.	N.A.	2	Wistar rats blood plasma protease	N.A.	Wistar rats blood plasma	In Vivo	None	None	ChAT activity, dpm/mg of tissue = 5.29±0.34 in (βA + HLDF-6-OH,250 µg/kg)
6259	076-262-596-914-468	2016	NA	GLP-1 ELP1-120	NA	His7 of GLP1	Free	Linear	L	Fusion with ELP	preproglucagon	N.A.	N.A.	10mg/kg	12.9	Tev protease	Bioassay	Rat	in vivo	https://www.lens.org/lens/patent/076-262-596-914-468	US 9,458,218 B2	N.A.
6260	076-262-596-914-468	2016	NA	GLP-1 ELP1-120	NA	His7 of GLP1	Free	Linear	L	Fusion with ELP	preproglucagon	N.A.	N.A.	1 mg/kg	20	Tev protease	Bioassay	Rabbit	in vivo	https://www.lens.org/lens/patent/076-262-596-914-468	US 9,458,218 B2	N.A.
6266	059-320-765-410-102	2016	MGSHHHHHHSSGENLYFQGHPCPDSSPLLQFGGQVRQRYLYTDDAQQTEAHLEIREDGTVGGAADQSPESLLQLKALKPGVIQILGVKTSRFLCQRPDGALYGSLHFDPEACSFRELLLEDGYNVYQSEAHGLPLHLPGNKSPHRDPAPRGPARFLPLPGLPPALPEPPGILAPQPPDVGSSDPLSMVEPSQGRSPSYASP	FGF21	NA	6-his tag, free cysteine	182P	Linear	L	Vitamin D3-PEG-maleimide	E. coli	Therapeutic	NA	0.1 mg/kg	675-fold increase	NA	ELISA	Rats	in vivo	https://www.lens.org/lens/patent/059-320-765-410-102	US 9,289,507 B2	N.A.
6267	059-320-765-410-102	2016	GS(n-octanoyl-S)FLSPEHQKAQQRKESKKPPAKLQPRC	rGhrelin-carrier conjugate	NA	Free	cysteine	Linear	L	Vitamin D3-PEG-maleimide	E. coli	Therapeutic	NA	0.1 mg/kg	8	NA	ELISA	Rats	in vivo	https://www.lens.org/lens/patent/059-320-765-410-102	US 9,289,507 B2	N.A.
6271	191-672-090-004-249	2016	DAHKSEVAHRFKDLGEENFKALVLIAFAQYLQQCPFEDHVKLVNEVTEFAKTCVADESAENCDKSLHTLFGDKLCTVATLRETYGEMADCCAKQEPERNE CFLQHKDDNPNLPRLVRPEVDVMCTAFHDNEETFLKKYLYEIARRHPYFY APELLFFAKRYKAAFTECCQAADKAACLLPKLDELRDEGKASSAKQRLKC ASLQKFGERAFKAWAVARLSQRFPKAEFAEVSKLVTDLTKVHTECCHGDL LECADDRADLAKYICENQDSISSKLKECCEKPLLEKSHCIAEVENDEMPA DLPSLAADFVESKDVCKNYAEAKDVFLGMFLYEYARRHPDYSVVLLLRLA KTYETTLEKCCAAADPHECYAKVFDEFKPLVEEPQNLIKQNCELFEQLGE YKFQNALLVRYTKKVPQVSTPTLVEVSRNLGKVGSKCCKHPEAKRMPCAE DYLSVVLNQLCVLHEKTPVSDRVTKCCTESLVNRRPCFSALEVDETYVPK EFNAETFTFHADICTLSEKERQIKKQTALVELVKHKPKATKEQLKAVMDD FAAFVEKCCKADDKETCFAEEGKKLVAASQAALGL	human albumin	NA	Free	Free	Linear	L	None	Human	NA	NA	NA	NA	NA	NA	NA	in vivo	https://lens.org/191-672-090-004-249	US 9352016 B2	NA
6272	023-486-744-040-716	2016	ANSFLEEMKKGHLERECMEETCSYEEAREVFEDSDKTNEFWNKYKDGDQC ETSPCQNQGKCKDGLGEYTCTCLEGFEGKNCELFTRKLCSLDNGDCDQFC HEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLER	Factor Xa variant	NA	Free	Free	Linear	L	None	Human	NA	NA	NA	1	intracellular protease	aPTT-based assay	CHO cells	in vivo	https://lens.org/023-486-744-040-716	US 9371522 B2	NA
6280	179-033-965-606-598	2017	NA	20K-PEG-insulin	NA	20K-PEG	Free	Linear	L	None	Human	NA	15 min	NA	improved	NA	enzyme immunoassay	Rat Blood	in vivo	https://lens.org/179-033-965-606-599	US 9616109 B2	EC50 =26.3ng/ml
6281	179-033-965-606-598	2017	NA	VitD-(25)-PEG2K-insulin	NA	VitD-(25)-PEG2K	Free	Linear	L	None	Human	NA	2-16 hours	NA	improved	NA	enzyme immunoassay	Rat Blood	in vivo	https://lens.org/179-033-965-606-600	US 9616109 B2	EC50 =15.8ng/ml
6282	179-033-965-606-598	2017	NA	VitD-(3)-PEG1.2K-insulin	NA	VitD-(3)-PEG1.2K	Free	Linear	L	None	Human	NA	20 min	NA	Drastically Improved	NA	enzyme immunoassay	Rat Blood	in vivo	https://lens.org/179-033-965-606-601	US 9616109 B2	EC50= 282.2ng/ml
6295	034-343-155-162-302	2017	NA	singly stapled SAH-Ex(A)	NA	SAH	Free	Linear	L	None	NA	NA	NA	NA	94	chymotrypsin	ELISA	NA	in vitro	https://lens.org/034-343-155-162-302	US 9695224 B2	NA
6296	034-343-155-162-302	2017	NA	singly stapled SAH-Ex(B)	NA	SAH	Free	Linear	L	None	NA	NA	NA	NA	128	chymotrypsin	ELISA	NA	in vitro	https://lens.org/034-343-155-162-302	US 9695224 B2	NA
6297	034-343-155-162-302	2017	NA	doubly stapled SAH-Ex(A, B)	NA	SAH	Free	Linear	L	None	NA	NA	NA	NA	295	chymotrypsin	ELISA	NA	in vitro	https://lens.org/034-343-155-162-302	US 9695224 B2	NA
6299	034-343-155-162-302	2017	NA	singly stapled SAH-Ex(A)	NA	Free	SAH	Linear	L	None	NA	NA	NA	NA	81	pepsin	ELISA	NA	in vitro	https://lens.org/034-343-155-162-302	US 9695224 B2	NA
6300	034-343-155-162-302	2017	NA	SAH-Ex(A, B)	NA	Free	SAH	Linear	L	None	NA	NA	NA	NA	172	pepsin	ELISA	NA	in vitro	https://lens.org/034-343-155-162-302	US 9695224 B2	NA