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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
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
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
1043	20844765	2010	RRWQWRMKKLG	Lfc8	11	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	110	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=3.8 Î¼M for E.coli
1044	20844765	2010	RRWQWRMKKLG	Lfc8	11	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	110	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=15Î¼M for S. Aureus
1045	20844765	2010	RRWQWRMKKLG	Lfc8	11	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	110	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99 ‰¤ 0.45Î¼M for B. subtilis
1046	20844765	2010	CRRWQWRMKKLGC	Lfc9	13	Free	Amidation	Cyclic (C1-C13)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	110	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9 Î¼M for E.coli
1047	20844765	2010	CRRWQWRMKKLGC	Lfc9	13	Free	Amidation	Cyclic (C1-C13)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	110	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99 ‰¤ 0.45Î¼M for S. Aureus
1048	20844765	2010	CRRWQWRMKKLGC	Lfc9	13	Free	Amidation	Cyclic (C1-C13)	L	None	Synthetic	Antimicrobial	9 hours	5 µM	110	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99 ‰¤ 0.45Î¼M for B. subtilis
1063	12699744	2003	ALCDNPRIDRWYCQFVEG	Peptide 5a	18	Acetylation [(C6H6)-(C6H12)-(C6H6)]	Amidation	Linear	L	None	Synthetic	Anticoagulant	Not reported	2mg/kg	222	Rabbit blood proteases	ELISA	Intravenouly administered into rabbit blood	in vivo	None	None	IC50=90nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin
1065	12699744	2003	ALCDNPRIDRWYCQFVEG	Peptide 5c	18	Acetylation [(C6H6)(CH2)4CH3]	Amidation	Linear	L	None	Synthetic	Anticoagulant	Not reported	2mg/kg	79.1	Rabbit blood proteases	ELISA	Intravenouly administered into rabbit blood	in vivo	None	None	IC50=22nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin
1077	2147696	1990	GVQLDLDEAI	Synthetic peptide	10	Free	Free	Linear	L	None	Synthetic peptide (corresponding to amino acids 605-614 of human protein S)	Anticoagulant	Not reported	Not mentioned	80	Rabbit blood proteases	Spectrofluorometry	Intravenously injected in male New Zealand white rabbits and blood samples withdrawn and plasma sample prepared	in vivo	None	None	34% of 125I protein S bound to C4b-binding protein in presence of 150 µM of peptide
1084	11099487	2000	RQIKIWFQNRRMKWKKNELKRAFAALRDQI	Int-H1-S6A,F8A	30	Free	Free	Linear	L	None	C-Myc derivative	Antiproliferative and proapoptotic	Not reported	Not mentioned	4.62	Fetal calf serum proteases	HPLC	Fetal bovine serum batch3	in vitro	None	None	Not reported
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
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
1116	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=3 µg/ml for M. Luteus ATCC 9341
1117	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=12.5 µg/ml for M. Luteus ATCC 9342
1119	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=3.12 µg/ml for M. Luteus ATCC 9344
1124	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=10 µg/ml for S. Aureus ATCC 6540
1125	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=25 µg/ml for S. Aureus ATCC 6541
1127	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=9 µg/ml for S. Aureus ATCC 6543
1132	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=1.56 µg/ml for S. Epidemidis ATCC 12229
1133	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=3.12 µg/ml for S. Epidemidis ATCC 12228
1135	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=2 µg/ml for S. Epidemidis ATCC 12228
1140	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=50 µg/ml for MRSA SR 1553
1141	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=>100 µg/ml for MRSA SR 1554
1143	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=38 µg/ml for MRSA SR 1556
1148	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=25 µg/ml for M. smegmatis ATCC 607
1149	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=25 µg/ml for M. smegmatis ATCC 607
1151	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=12.5 µg/ml for M. smegmatis ATCC 613
1156	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=12.5 µg/ml for E. coli ATCC 2592
1157	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=31 µg/ml for E. coli ATCC 2592
1159	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=19 µg/ml for E. coli ATCC 2592
1164	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=6.25 µg/ml for P. aeruginosa ATCC 9027
1165	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=25 µg/ml for P. aeruginosa ATCC 9027
1167	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=6.25 µg/ml for P. aeruginosa ATCC 9027
1172	10461747	1998	KKÎ¨[CH2NH]VVFKVKFk	KSL3	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=6.25 µg/ml for C. albicans ATCC 36232
1173	10461747	1998	KÎ¨[CH2NH]KÎ¨[CH2NH]VVFKVKFk	KSL4	10	Free	Free	Linear	Mix	Reduced amide bonds Î¨(CH2NH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	>81	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=31 µg/ml for C. albicans ATCC 36232
1175	10461747	1998	KÎ¨[CH2OCONH]KÎ¨[CH2OCONH]VVFKVKFk	KSL6	10	Free	Free	Linear	Mix	Reduced carbamate Î¨(CH2OCONH)	Synthetic	Antimicrobial	Not reported	100 µg/mL	67	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC=11 µg/ml for C. albicans ATCC 36232
1177	14759771	2004	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Glucagon-like peptide-1(7-36)amide	30	Free	Amidation	Linear	L	None	Glucagon-like peptide-1	Regulate blood glucose	12 hours	2 mM	4.4	Purified DPP IV	ESI-MS	Purified DPP IV	in vitro	None	None	0 ±0% insulin intensity in ARIP cells
1179	14759771	2004	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Glucagon-like peptide-1(7-36)amide	30	Free	Amidation	Linear	L	None	Glucagon-like peptide-1	Regulate blood glucose	12 hours	2 mM	4.7	Serum proteases	ESI-MS	Serum	in vitro	None	None	0 ±0% glucokinase intensity in ARIP cells
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
1204	21244372	2010	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Synthetic version of the 39-amino-acid peptide originally isolated from the saliva of the gila monster lizard	Regulate blood glucose	Not mentioned	5 µg ·mL-1 ·kg-1	1.5 to 4	Rat plasma proteases	ELISA	Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1	in vivo	None	None	EC50 of 2.3nM for stimulation of intracellular cAMP in PC12 cells
1205	21244372	2010	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	PB-105 (ExC39)	39	Free	Amidation	Linear	L	None	Analogue of exenatide	Regulate blood glucose	Not mentioned	5 µg ·mL-1 ·kg-1	2.9 ±0.1	Rat plasma proteases	ELISA	Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1	in vivo	None	None	EC50 of 1.4nM for stimulation of intracellular cAMP in PC12 cells
1212	21114599	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVK-Aib-R	[Aib35]hGLP-1(7-36)NH2	30	Free	Amidation	Linear	L	Aib--Aminoisobutyric acid	Analogue of glucagon like peptide-1	Regulate blood glucose	Not mentioned	Not mentioned	2.0 ±0.3	Rat plasma proteases	HPLC	Rat plasma	in vitro	14759771	None	EC50=0.05 ±0.01nM for cAMP stimulation
1220	20587645	2010	VRRADRAAVPGGGGRG	mPEG-ALD10k-HM-3	16	Methoxy-polyethylene glycolPEG-aldehyde (mPEG-ALD10k )	Free	Linear	L	None	HM-3 analogue	Anti-angiogenetic	Not mentioned	Not mentioned	162.08 ±36.57	Proteases in chorioallantoic membrane of chick embryo	RP-HPLC	Chorioallantoic membrane of chick embryo	in vivo	http://pubs.rsc.org/En/content/articlepdf/2014/tb/	None	Dramatically inhibits angiogenesis on the chorioallantoic membrane of chick embryo
1222	20593470	2010	GGFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 2	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	1.1	None	HPLC	PBS	in vitro	None	None	Not reported
1225	20593470	2010	GVFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 5	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	4.7	None	HPLC	PBS	in vitro	None	None	Not reported
1231	20593470	2010	FGFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 11	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	2.5	None	HPLC	PBS	in vitro	None	None	EC50=0.23 ±0.10nM
1232	20593470	2010	FAFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 12	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	2.8	None	HPLC	PBS	in vitro	None	None	Not reported
1233	20593470	2010	FaFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 13	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	2.4	None	HPLC	PBS	in vitro	None	None	Not reported
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
1243	20631047	2010	MLTKFETKSARVKGLSFHPKRPWIL	Xenin	25	Free	Free	Linear	L	None	Secreted from intestinal K-cells	Regulates insulin	360 minutes	Not mentioned	162 ±6	Mice plasma proteases	HPLC	Mice plasma	in vitro	1429581	None	Stimulated insulin secretion at 5.6 mM In clonal BRIN-BD11 cells
1244	12047915	2002	AEGTFTSDVSSYLEGQAAREFIAWLVK(Oct)GRG	LY315902	35	2-indolyl-propionyl	Free	Linear	L	Oct-octanoic moiety	Glucagon-like peptide-1 analogue	Insulinotropic and glucagonostatic	Not mentioned	Not mentioned	1.1	Canine plasma protease	Radioimmunoassay	Canine plasma after subcutaneous injection of 100 µg/kg	in vivo	9232514	None	Plasma insulin 255 pmol/l on intravenous infusion of 20 pmol/kg/min of LY315902
1245	17292977	2007	HGEGTFTSDLSKQLEEEAVRLFIEWLKNGGPSSGAPPPS	AC3174	39	Free	Amidation	Linear	L	None	Analog of exendin-4	Regulates blood glucose	5 hours	Not mentioned	>5	Human plasma proteases	LC/MS	Human plasma	in vitro	None	None	IC50=0.66 ±0.13nM for binding to GLP-1 receptor
1267	14499707	2003	YADAIFTNSYRKVLGQLSARKLLQDIMSR	GRF-1PEG5000	29	Free	Amidation	Linear	L	PEGylation	Growth hormone-releasing hormone (GRF) analogue	Stimulates release of growth hormone	25 hours	Not mentioned	3.6	Human plasma proteases	Reporter gene assay	Human plasma	in vitro	None	None	EC50=1.06nM
1268	14499707	2003	YADAIFTNSYRKVLGQLSARKLLQDIMSR	GRF-1PEGLys21	29	Free	Amidation	Linear	L	PEGylation on Lys21	Growth hormone-releasing hormone (GRF) analogue	Stimulates release of growth hormone	26 hours	Not mentioned	4	Human plasma proteases	Reporter gene assay	Human plasma	in vitro	None	None	Not reported
1665	2533571	1989	TSEKSQTPLVTL	Des-enkephalin-Î³-endorphin	12	Free	Free	Linear	L	None	Endorphin derivative	Neuropeptide	Not reported	0.1mM	4.5	Proteases in SVK14 keratinocytes	HPLC/liquid scintillation counting	SVK14 keratinocytes	in vitro	3582424	None	Not reported
1666	2533571	1989	TSEKSQTPLVTL	Des-enkephalin-Î³-endorphin	12	Free	Free	Linear	L	None	Endorphin derivative	Neuropeptide	Not reported	0.1mM	4.1	Proteases in fibroblasts	HPLC/liquid scintillation counting	Human fibroblasts	in vitro	3582424	None	Not reported
1667	2533571	1989	TSEKSQTPLVTL	Des-enkephalin-Î³-endorphin	12	Free	Free	Linear	L	None	Endorphin derivative	Neuropeptide	Not reported	0.1mM	4.4	Proteases in human fresh whole skin	HPLC/liquid scintillation counting	Human fresh whole skin	in vitro	3582424	None	Not reported
1668	2533571	1989	TSEKSQTPLVTL	Des-enkephalin-Î³-endorphin	12	Free	Free	Linear	L	None	Endorphin derivative	Neuropeptide	Not reported	0.1mM	4.6	Proteases in human fresh epidermis	HPLC/liquid scintillation counting	Human fresh epidermis	in vitro	3582424	None	Not reported
1669	2533571	1989	TSEKSQTPLVTL	Des-enkephalin-Î³-endorphin	12	Free	Free	Linear	L	None	Endorphin derivative	Neuropeptide	Not reported	0.1mM	4.5	Proteases in human fresh dermis	HPLC/liquid scintillation counting	Human fresh dermis	in vitro	3582424	None	Not reported
1688	3080478	1985	SSLKQYWSSLKQSFS	C0-LAP	15	Free	Free	Linear	L	None	Lipid associated peptide -20	Not mentioned	Not reported	300 µl	~300	Not mentioned	Serum decay experiment	Blood sample of female Sprague-Dawley rat	in vivo	6774331	None	Not mentioned
1697	8222093	1993	VVYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ	Recombinant hirudin	65	Free	Free	Linear	L	None	Not available	Anticoagulant	Not reported	1000ng/ml	2 to 3	Not mentioned	ELISA	Human blood 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
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
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
1709	12119302	2002	RLIEDICLPRWGCLWEDD	SA21	18	Acetylation	Amidation	Linear	L	None	Synthetic (Phage display library)	Not mentioned	Not reported	106 cpm/200Î¼l/mouse	2.3	Blood proteases	ESI-LC ˆ’MS/MS	Rabbit blood sample	in vivo	None	None	Dissociation equilibrium constant of peptide for albumin,Kd=320 ±22
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
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
1755	16472750	2006	TVPVDLASRQEEEEQSPDSTEEEPVTLPR	E2-PEST	29	Free	Free	Linear	L	None	E2 protein from papillomavirus	Gene transcription	Not reported	Not mentioned	63	in aCSF	Pulse chase experiment	pMEP-E2 CV-1 cell lines	in vitro	15014086	None	Not mentioned
1756	16472750	2006	TVPVDLASRQEEEEQSADSTEEEPVTLPR	E2-PESTP299A	29	Free	Free	Linear	L	None	E2 protein from papillomavirus	Gene transcription	Not reported	Not mentioned	94	Not mentioned	Pulse chase experiment	pMEP-E2 CV-1 cell lines	in vitro	15014086	None	Not mentioned
1758	16586064	2006	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	GLP1	30	Free	Amidation	Linear	L	None	Synthetically synthesized Glucagon-like peptide-1	Insulinotropic	Not reported	Not mentioned	114 ±28	Rat plasma proteases	RP-HPLC	Rat plasma	in vitro	16505481	None	380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1762	16586064	2006	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	N-PEG/GLP-1	30	Free	Amidation	Linear	L	Pegylation at N terminus His7	Synthetically synthesized Glucagon-like peptide-1 analogues	Insulinotropic	Not reported	Not mentioned	250 ±117	Rat liver proteases	RP-HPLC	Rat liver homogenate	in vitro	16505481	None	290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1765	16586064	2006	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Lys-PEG/GLP-1	30	Free	Amidation	Linear	L	Pegylation on Lys34	Synthetically synthesized Glucagon-like peptide-1 analogues	Insulinotropic	Not reported	Not mentioned	62 ±23	Rat liver proteases	RP-HPLC	Rat liver homogenate	in vitro	16505481	None	150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1779	17537541	2007	HSDAVFTDNYTRLRKQMAVKKYLNSILN	Vasoactive intestinal peptide (VIP)	28	Free	Free	Linear	L	None	Vasoactive intestinal peptide	Neurotransmitter	Not reported	Ki=2.63 ±0.87 nM	1.38	Not mentioned	Not mentioned	Rat lung alveolar L2 cells	in vitro	None	None	Not given
1780	17537541	2007	HSDAVFTDNYTRLRRQMLVRRYLNSILNGRR	IK312532	31	Free	Free	Linear	L	None	Synthetic peptide	VIP analogue	Not reported	Ki=1.36 ±0.29 nM	4.73	Not mentioned	Not mentioned	Rat lung alveolar L2 cells	in vitro	None	None	Not given
1796	17640899	2007	MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL	T-2410	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.008 µg/ml against IIIB virus
1797	17640899	2007	MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL	T-2410	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.032 µg/ml against 098 virus
1798	17640899	2007	MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL	T-2410	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.039 µg/ml against 098-T20 virus
1799	17640899	2007	MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL	T-2410	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.137 µg/ml against 098-T1249 virus virus
1800	17640899	2007	MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL	T-2410	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=4.975 µg/ml against 098-T651 virus
1801	17640899	2007	TTWEAWDRAIAEYAARIEALIRASQEQQEKNEAELREL	T-290676	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.006 µg/ml against IIIB virus
1802	17640899	2007	TTWEAWDRAIAEYAARIEALIRASQEQQEKNEAELREL	T-290676	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.013 µg/ml against 098 virus
1803	17640899	2007	TTWEAWDRAIAEYAARIEALIRASQEQQEKNEAELREL	T-290676	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.022 µg/ml against 098-T20 virus
1804	17640899	2007	TTWEAWDRAIAEYAARIEALIRASQEQQEKNEAELREL	T-290676	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.072 µg/ml against 098-T1249 virus virus
1805	17640899	2007	TTWEAWDRAIAEYAARIEALIRASQEQQEKNEAELREL	T-290676	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	1.2	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=1.314 µg/ml against 098-T651 virus
1816	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAILREL	T-267209	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	3.4	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.007 µg/ml against IIIB virus
1817	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAILREL	T-267209	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	3.4	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.021 µg/ml against 098 virus
1818	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAILREL	T-267209	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	3.4	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.034 µg/ml against 098-T20 virus virus
1819	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAILREL	T-267209	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	3.4	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.024 µg/ml against 098-T1249 virus
1820	17640899	2007	TTWEAWDRAIAEYAARIEALIRAAQEQQEKNEAILREL	T-267209	38	Free	Free	Linear	L	None	Synthetic peptide	Antiviral peptide	Not reported	~1 €“2mg/kg	3.4	Monkey blood proteases	RP-HPLC and ESI-MS	Male cynomolgus monkey blood plasma (Intravenous)	in vivo	None	None	IC50=0.039 µg/ml against 098-T651 virus
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
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
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
1960	18413862	2008	Chex-RPNKPRPYLPRPRPPRPVR-Dab-RVPRPPRPRPLYPRPKNPR-Chex	A3-APO (Dimer)	38	Chex =Cyclohexane carboxylic acid	Free	Linear	L	Dab =2,4-diamino-butyric acid	Synthetic peptide	Antibacterial	Not reported	5 mg/kg	100	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC= 16 mg/mL
1961	18413862	2008	Chex-RPNKPRPYLPRPRPPRPVR-Dab-RVPRPPRPRPLYPRPKNPR-Chex	A3-APO (Dimer)	38	Chex =Cyclohexane carboxylic acid	Free	Linear	L	Dab =2,4-diamino-butyric acid	Synthetic peptide	Antibacterial	Not reported	5 mg/kg	230	Mouse serum proteases	RP-HPLC	Mouse serum	in vitro	None	None	MIC= 16 mg/mL
1971	18553094	2008	HPLGSPGSASDLETSGLQEQRNHLQGKLSELQVEQTSLEPLQESPRTPGVWKSREVATEGIRGHRKMVLYTLRAPR	NT-proBNP	76	Free	Free	Linear	L	None	Pro-Brain natriuretic peptide	Vasodilator	Not reported	Not mentioned	~120	Human blood proteases	ELISA	Human plasma	in vitro	None	None	Not available
1978	19413309	2009	IRRADRAAVPGGGGRGD	PEG10k-HM-3	17	Methoxypoly(ethylene glycol)-aldehyde (mPEG-ALD)	Free	Linear	L	None	RGD- modified endostatin derived peptide	Antitumor	Not reported	1mg/ml	162.08 ± 36.57	Rat blood proteases	RP-HPLC	Rat blood serum (Intravenous injection)	in vivo	None	None	More active in the inhibition of angiogenesis in the chorioallantoic membrane of chick embryos
1992	19602537	2009	HSQGTFTSDYSKYLDSRRAQDFVQWLMNTKRNRNNIA	DualAG	37	Free	Cholesterol moiety	Linear	L	None	Proglucagon molecule	Protease-resistant dual GLP1R/GCGR agonist	Not reported	3mg/kg	1.7	Mouse blood proteases	RP-HPLC and ESI-MS	Mouse plasma (Subcutaneous injection)	in vivo	None	None	EC 50, cAMP=1.5nM for mGCGR
1994	19715558	2009	LEQYANQLADQIIKEATE	RIAD	18	Free	Free	Linear	L	None	Synthetic peptide	Displaces PKA (protein kinase A) type I from the AKAP (A-kinase-anchoring protein) ezrin	Not reported	Not mentioned	1.5	Human serum proteases	HPLC	Human serum	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
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
2004	11976797	2002	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	GLP-1	30	Free	Amidation	Linear	L	Radiolabelling of GLP-1by [123I]	Proglucagon molecule	Antidiabetic	Not reported	10 MBq of the radiolabelled peptides	110 ±13 for Î² phase	Rat blood proteases	Scintigraphy	NEDH Rats (rat tumour model)	in vivo	None	None	Not mentioned
2006	11976797	2002	HSDGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin 3	39	Free	Free	Linear	L	Radiolabelling of exendin 3 at position 1 (histidine)	Heloderma horridum venom	GLP-1 agonist	Not reported	10 MBq of the radiolabelled peptides	108 ±16	Rat blood proteases	Scintigraphy	NEDH Rats (rat tumour model)	in vivo	None	None	Not mentioned
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
2014	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK	Acetyl-PACAP38	38	Acetylation	Amidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 5.6 ±1.5 nM
2015	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK	Hexanoyl-PACAP38	38	Hexanoylation	Amidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 8.3 ±1.8 nM
2016	18353507	2008	H-Aib-DGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK	[Aib2]PACAP38	38	Free	Amidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	65 ±8	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 7.1 ±1.4 nM
2017	18353507	2008	HsDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK	[D-Ser2]PACAP38	38	Free	Amidation	Linear	Mix	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 9.7 ±2.5 nM
2021	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK	Acetyl-PACAP38-propylamide	38	Acetylation	Propylamidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 2.9 ±0.9 nM
2022	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK	Acetyl-PACAP38-hexylamide	38	Acetylation	Hexylamidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 3.5 ±0.7 nM
2023	18353507	2008	HSDGIFTDSYSRYAKQMAVAKYLAAVLGKRYKQRVKNK	Acetyl-[Ala14, Ala20]PACAP38-propylamide	38	Acetylation	Propylamidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 5.3 ±1.7 nM
2025	18353507	2008	HSDGIFTDSYSRYRAQMAVAKYLAAVLGKRYKQRVKNK	Acetyl-[Ala15, Ala20]PACAP38-propylamide	38	Acetylation	Propylamidation	Linear	L	None	Synthetic analog of PACAP38	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 1.8 ±0.7 nM
2028	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	PACAP27	27	Free	Amidation	Linear	L	None	Synthetically synthesised pituitary adenylate cyclase-activating polypeptide	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-4 M	>120	Human plasma proteases	RP-HPLC and MS-MALDI-TOF	Human plasma	in vitro	None	None	IC50 = 9.6 ±2.4 nM
2029	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	Acetyl-PACAP27	27	Acetylation	Amidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 9.6 ±1.5 nM
2030	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	Hexanoyl-PACAP27	27	Hexanoylation	Amidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 10.6 ±2.4 nM
2031	18353507	2008	H-Aib-DGIFTDSYSRYRKQMAVKKYLAAVL	[Aib2]PACAP27	27	Free	Amidation	Linear	L	Aib	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	145 ±23	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 7.9 ±1.8 nM
2032	18353507	2008	HsDGIFTDSYSRYRKQMAVKKYLAAVL	[D-Ser2]PACAP27	27	Free	Amidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 10.3 ±2.1 nM
2033	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	Acetyl-PACAP27-propylamide	27	Acetylation	Propylamidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 6.7 ±1.2 nM
2034	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	Acetyl-PACAP27-propylamide	27	Acetylation	Propylamidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-4 M	>120	Human plasma proteases	RP-HPLC and MS-MALDI-TOF	Human plasma	in vitro	None	None	IC50 = 6.7 ±1.2 nM
2035	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	Acetyl-PACAP27-hexylamide	27	Acetylation	Hexylamidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-5 M	>240	DPP IV	RP-HPLC and MS-MALDI-TOF	DPP IV	in vitro	None	None	IC50 = 5.6 ±1.3 nM
2036	18353507	2008	HSDGIFTDSYSRYRKQMAVKKYLAAVL	Acetyl-PACAP27-hexylamide	27	Acetylation	Hexylamidation	Linear	L	None	Synthetic analog of PACAP27	Therapeutic Neuropeptide for neurodegenerative diseases.	Not reported	10-4 M	>120	Human plasma proteases	RP-HPLC and MS-MALDI-TOF	Human plasma	in vitro	None	None	IC50 = 5.6 ±1.3 nM
2040	19041716	2009	AGCKNFFWKTFTSC	LCNP/SST (encapsulated within Liquid crystalline nanoparticles)	14	Free	Free	Cyclic (C3-C14)	L	None	Somatostatin encapsulated within Liquid crystalline nanoparticles	Neurotransmitter	Not reported	1.8 mg/ml	1.23 ±0.16	Rat blood proteases	ELISA	Rat plasma (Intravenous injection)	in vivo	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
2057	21334413	2011	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Free	Linear	L	None	Venom of the lizard Heloderma suspectum	Binds and activates the GLP-1 receptor	Not reported	500 Î¼g/kg	2.4	Rat blood proteases	Radioimmunoassay	Rat plasma	in vitro	None	None	Not mentioned
2058	21664938	2011	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	GLP-1	30	Free	Free	Linear	L	None	Proglucagon molecule	Anti-hyperglycemic hormone	Not reported	300 Î¼g/kg	<2	Rat blood proteases	ELISA	Serum of rats (Subcutaneous injection)	in vivo	None	None	Binding constants to the GLP-1 receptor= 27.62 ± 2.13nM
2078	8910426	1996	GCTFRRLKWKCG	LALF-10 (38 €“45)	12	Free	Free	Cyclic (C2-C11)	L	None	Analogue of Limulus anti-lipopolysaccharide factor	Antibacterial	Not reported	2.5 µg/ml	77	Proteases present in fetal calf serum	RP-HPLC	Fetal calf serum	in vitro	None	None	LD50=2.58 mg/ml
2079	8910426	1996	GCKPTFRRLKWKYKCG	LALF-14 (36 €“47)	16	Free	Free	Cyclic (C2-C15)	L	None	Analogue of Limulus anti-lipopolysaccharide factor	Antibacterial	Not reported	2.5 µg/ml	84	Proteases present in fetal calf serum	RP-HPLC	Fetal calf serum	in vitro	None	None	LD50=2.33 mg/ml
2103	N.A.	2009	EACNLPIVRGPCIAFFPRWAFDAVKGKCVLFPYGGCQGNGNKFYSEKECREYCGVP	DX-890	56	Free	Free	Linear	L	None	Kunitz domain peptide	Protease inhibitor	N.A.	Not mentioned	165	Rabbit blood proteases	I-125 radiolabelling method	Rabbit plasma (Intravenous)	in vivo	None	EP2090589A1	Inhibition constt (Ki) 6 ±1 pM
2105	N.A.	2009	EACNLPIVRGPCIAFFPRWAFDAVKGKCVLFPYGGCQGNGNKFYSEKECREYCGVP	DX-890	56	Free	Free	Linear	L	None	Kunitz domain peptide	Protease inhibitor	N.A.	Not mentioned	79.44	Mouse blood proteases	I-125 radiolabelling method	Mouse plasma (Intravenous)	in vivo	None	EP2090589A1	Not mentioned
2174	N.A.	2006	HGDGSFSDEMNTILDNLAARDFINWLIQTLITD	Derivative of Glucagon Like Peptide-2 (GLP-2)	33	Free	Amidation	Linear	L	None	GLP-2	Intestine function modulator	N.A.	500 nM/ Kg	1.5	Rat blood proteases	Radioimmunoassay	Rat plasma (Intravenous)	in vivo	None	US7112567B2	Increase in wet-weight of small intestine >0.5 g
2182	N.A.	2013	VKFNKPFVFLMIEQNTK	SP16	13	Free	Free	Linear	L	None	Human alpha-1-antitrypsin	Anti-inflammatory and immune modulator peptide	N.A.	5 mg/ Kg	1.9	Rat blood proteases	LC-MS/MS	Rat plasma (Intravenous)	in vivo	None	WO2013106273A2	Not mentioned
2183	N.A.	2012	KGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	Intermedin or adrenomedullin peptide	39	Free	Free	Linear	L	None	Preproadrenomedullin	Calcium homeostasis	N.A.	Not mentioned	1.5	Rat blood proteases	ELISA	Rat plasma (Intravenous)	in vivo	None	WO2012138867A2	Not mentioned
2205	N.A.	2009	SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII	Human Corticotropic releasing factor (hCRF)	41	Free	Free	Linear	L	None	Hypothalamus	Inhibitor of edema and inflammation	N.A.	100 micro g/ Kg	62.6	Not mentioned	ELISA	Rat plasma (Subcutaneous)	in vivo	None	WO2009027844	Not mentioned
2206	N.A.	2009	SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII	Human Corticotropic releasing factor (hCRF)	41	Free	Free	Linear	L	None	Hypothalamus	Inhibitor of edema and inflammation	N.A.	1000 micro g/ Kg	72.1	Not mentioned	ELISA	Rat plasma (Subcutaneous)	in vivo	None	WO2009027844	Not mentioned
2207	N.A.	2003	WQEWEQKITALLEQAQIQQEKNEYELQKLDKWASLWEWF	T1249	39	Acetylation	Amidation	Linear	L	None	Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins	Anti-HIV peptide	N.A.	1.2 mg/ Kg	2.02	Not mentioned	HPLC	Rat plasma (Subcutaneous)	in vivo	None	US6656906	Fold fusion-inhibition (CEM cells and Molt-4 cells) with respect to T20 (DP-178) against HIV2-NIH-Z strain 840 Fold
2208	N.A.	2003	WQEWEQKITALLEQAQIQQEKNEYELQKLDKWASLWEWF	T1249	39	Acetylation	Amidation	Linear	L	None	Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins	Anti-HIV peptide	N.A.	1.5 mg/ Kg	2.46	Rat blood proteases	HPLC	Rat plasma (Intravenous)	in vivo	None	US6656906	Not mentioned
2209	N.A.	2003	WQEWEQKITALLEQAQIQQEKNEYELQKLDKWASLWEWF	T1249	39	Acetylation	Amidation	Linear	L	None	Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins	Anti-HIV peptide	N.A.	0.8 mg/ kg	4.83	Not mentioned	HPLC	Monkey plasma (Subcutaneous)	in vivo	None	US6656906	Not mentioned
2212	N.A.	2003	WQEWEQKITALLEQAQIQQEKNEYELQKLDKWASLWEWF	T1249	39	Acetylation	Amidation	Linear	L	None	Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins	Anti-HIV peptide	N.A.	15 mg/ Kg	2	Not mentioned	HPLC	Rat plasma (Subcutaneous)	in vivo	None	US6656906	Not mentioned
2213	N.A.	2003	WQEWEQKITALLEQAQIQQEKNEYELQKLDKWASLWEWF	T1249	39	Acetylation	Amidation	Linear	L	None	Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins	Anti-HIV peptide	N.A.	5 mg/ Kg	1.86	Rat blood proteases	HPLC	Rat plasma (Intravenous)	in vivo	None	US6656906	Not mentioned
2220	12954066	2003	ELYENKP-N3-Hlys-RPYIL	KK1	13	Free	Free	Linear	L	N₃-L-Hlys at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	153 ±4	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2221	12954066	2003	ELYENKP-N3-1d-RPYIL	KK2	13	Free	Free	Linear	L	N₃-1^d= COOH-CH(NH2)CH2-(CH2)3-CH2-NHMe at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	211 ±6	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2222	12954066	2003	ELYENKP-N3-2-RPYIL	KK3	13	Free	Free	Linear	L	N₃-2= COOH-CH(NH2)CH2-(CH2)3-CH2-NMe₂at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	126 ±18	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2223	12954066	2003	ELYENKP-N3-3-RPYIL	KK4	13	Free	Free	Linear	L	N₃-3= COOH-CH(NH2)CH2-(CH2)3-CH2-NMe₂at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	103 ±10	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2224	12954066	2003	ELYENKP-N3-Lys-RPYIL	KK5	13	Free	Free	Linear	L	N₃-L-lys at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	136 ±6	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2225	12954066	2003	ELYENKP-N3-4-RPYIL	KK6	13	Free	Free	Linear	L	N₃-4^d= COOH-CH(NH2)CH2-(CH2)3-CH2-NHMe at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	128 ±6	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2226	12954066	2003	ELYENKP-N3-5-RPYIL	KK7	13	Free	Free	Linear	L	N₃-5^d= COOH-CH(NH2)CH2-(CH2)3-CH2-NMe₂ at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	127 ±2	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2227	12954066	2003	ELYENKP-N3-6-RPYIL	KK8	13	Free	Free	Linear	L	N₃-6^d= COOH-CH(NH2)CH2-(CH2)3-CH2-⁺NMe₃ at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	128 ±30	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2228	12954066	2003	ELYENKP-N3-Orn-RPYIL	KK9	13	Free	Free	Linear	L	N₃-L-Orn at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	134 ±27	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2229	12954066	2003	ELYENKP-N3-7-RPYIL	KK10	13	Free	Free	Linear	L	N₃-7^d= COOH-CH(NH2)CH2-(CH2)3-CH2-⁺NHMe at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	131 ±27	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2230	12954066	2003	ELYENKP-N3-8-RPYIL	KK11	13	Free	Free	Linear	L	N₃-8^d= COOH-CH(NH2)CH2-(CH2)3-CH2-Nme₂ at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	126 ±9	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2231	12954066	2003	ELYENKP-N3-9-RPYIL	KK12	13	Free	Free	Linear	L	N₃-9^d= COOH-CH(NH2)CH2-(CH2)3-CH2-⁺Nme₃ at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	216 ±33	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
2234	12954066	2003	ELYENKP-N3-Arg-RPYIL	KK15	13	Free	Free	Linear	L	N₃-L-Arg at 8th arginine position	Derivative of Bovine hypothalamus	Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis	Not mentioned	1.07mM	174 ±7	Rat serum protease	MALDI-TOF-MS	Rat serum	in vitro	None	None	Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 Î¼g of protein per formed on whole cells.
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.
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
2303	6605972	1984	SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA	Ovine corticotropic releasing factor	41	Free	Free	Linear	L	None	Paraventricular nucleus (PVN) of the hypothalamus	Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis	0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.	76 Î¼g	70.8 (t1/2 slow)	Human blood plasma proteases	Radioimmunoassay and HPLC analysis	Intravenous administration to human plasma	in vivo	http://www.anaspec.com/products/product.asp?id=322	None	Not reported
2305	6605972	1984	SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA	Ovine corticotropic releasing factor	41	Free	Free	Linear	L	None	Paraventricular nucleus (PVN) of the hypothalamus	Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis	0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.	75 Î¼g	95.4 (t1/2 slow)	Human blood plasma proteases	Radioimmunoassay and HPLC analysis	Intravenous administration to human plasma	in vivo	http://www.anaspec.com/products/product.asp?id=322	None	Not reported
2306	6605972	1984	SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA	Ovine corticotropic releasing factor	41	Free	Free	Linear	L	None	Paraventricular nucleus (PVN) of the hypothalamus	Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis	0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.	75 Î¼g	90.8 (t1/2 slow)	Human blood plasma proteases	Radioimmunoassay and HPLC analysis	Intravenous administration to human plasma	in vivo	http://www.anaspec.com/products/product.asp?id=322	None	Not reported
2308	6605972	1984	SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA	Ovine corticotropic releasing factor	41	Free	Free	Linear	L	None	Paraventricular nucleus (PVN) of the hypothalamus	Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis	0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.	80 Î¼g	83.5 (t1/2 slow)	Human blood plasma proteases	Radioimmunoassay and HPLC analysis	Intravenous administration to human plasma	in vivo	http://www.anaspec.com/products/product.asp?id=322	None	Not reported
2309	6605972	1984	SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA	Ovine corticotropic releasing factor	41	Free	Free	Linear	L	None	Paraventricular nucleus (PVN) of the hypothalamus	Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis	0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.	80 Î¼g	73.0 (mean t1/2 slow)	Human blood plasma proteases	Radioimmunoassay and HPLC analysis	Intravenous administration to human plasma	in vivo	http://www.anaspec.com/products/product.asp?id=322	None	Not reported
2313	6658706	1983	ADSGEGDFLAEGGGVR	125I-labeled desamino-tyrosyl (DAT-FPA) FPA	16	Free	Free	Linear	L	DAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-T	Desaminotyrosine Fibrinopeptide derivative	Blood clotting	8 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 min	Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA	180 (radioactivity)	Normal rabbit blood proteases	Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.	Intravenous injection in lateral vein of normal rabbit	in vivo	http://search.anaspec.com/?keywords=fibrinopeptide	None	Not reported
2317	6658706	1983	ADSGEGDFLAEGGGVR	Human Fibrinopeptide A (FPA)	16	Free	Free	Linear	L	None	N terminal end of the A-alpha chain of fibrinogen	Blood clotting	12 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 min	Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA	90	Normal rabbit blood proteases	Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.	Intravenous injection in lateral vein of normal rabbit	in vivo	None	None	Not reported
2326	8839678	1995	HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Glucagon like peptide 1 (GLP( 7-36))	36	Free	Amidation	Linear	L	None	Human intestinal epithelium	Gastric motility	5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min	400 pmol/l	68 ±6 (for final phase)	Dog plasma proteases	Radioimmunoassay and HPLC	Intravenous injection to dogs plasma	in vitro	None	None	Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
2327	8839678	1995	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Glucagon like peptide 1 (GLP( 7-37))	37	Free	Free	Linear	L	None	Human intestinal epithelium	Gastric motility	5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min	400 pmol/l	81 ±3 (for final phase)	Dog plasma proteases	Radioimmunoassay and HPLC	Intravenous injection to dogs plasma	in vitro	http://www.anaspec.com/products/product.asp?id=324	None	Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
2328	8839678	1995	HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Glucagon like peptide 1 (GLP( 7-36))	36	Free	Amidation	Linear	L	None	Human intestinal epithelium	Gastric motility	5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min	400 pmol/l	132 ±16	Dog plasma proteases	Radioimmunoassay and HPLC	Subcutaneous injection into dog plasma	in vitro	None	None	Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
2329	8839678	1995	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Glucagon like peptide 1 (GLP( 7-37))	37	Free	Free	Linear	L	None	Human intestinal epithelium	Gastric motility	5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min	400 pmol/l	61 ±9	Dog plasma proteases	Radioimmunoassay and HPLC	Subcutaneous injection into dog plasma	in vitro	http://www.anaspec.com/products/product.asp?id=324	None	Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
2331	8839678	1995	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Glucagon like peptide 1 (GLP( 7-37))	37	Free	Free	Linear	L	None	Human intestinal epithelium	Gastric motility	5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min	400 pmol/l	238 ±35	Dog plasma proteases	Radioimmunoassay and HPLC	Subcutaneous injection into dog plasma in presence of bacitracin	in vitro	http://www.anaspec.com/products/product.asp?id=324	None	Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
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
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
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
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
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
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
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
2393	11145579	2001	GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA	Insulin like growth factor 1 (IGF-1)	70	Free	Free	Linear	L	I125 radiolabeling	Human IGF-1	Regulate somatic growth and cellular proliferation	1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h	15 Î¼Ci(0.2 ml)	1.22 ±0.237 (t1/2 Î²)	Rat blood proteases	TCA precipitation	Intravenous injection into rat	in vivo	PMID:7758431	None	Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter.
2401	1824807	1991	AELRCMCIKTTSGIHPKNIQSLEVIGKGTHCNQVEVIATLKDGRKICLDPDAPRIKKIVQKKLAGDESAD	naP-2 (Neutrophil-activatingprotein-2)	70	Free	Free	Linear	L	None	beta- thromboglobulin	Inflammatory peptide	48 hours	20 pmol/site	65-75	Rabbit blood proteases	Not mentioned	Intradermal injection in rabbit	in vivo	None	None	P- 2 elicited inflammatory responses (neutrophil emigration, edema formation at 20 pmol/l
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.
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
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
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
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
2422	18937214	2009	SVTLFGESAGAASVSLHLLSPGSHSLFTR	Carbofuran (methylcarbamyl-)-labeled tryptic peptide	29	Free	Free	Linear	L	Methylcarbamylated at serine (position 8)	Human Bche protein	Pesticide	Not mentioned	Not mentioned	2	Human blood proteases	HPLC	Human serum	in vivo	None	None	BChE activity was 88% inhibited at time zero, but became less inhibited with time as carbofuran was released from the active site Ser 198.
2441	7522585	1994	rPKPfQwFwLLRPKPQQFFGLM	Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP	22	Free	Free	Linear	Mix	None	Substance P (SP) analogue	Anticancer drugs	1, 2, 5 and 24 hours	10 Î¼g/ml	4.6	Mouse liver proteases	RP-HPLC and Electrochemical Detection	Mouse liver homogenate	in vitro	None	None	Act as growth factors
2446	7522585	1994	RwFWLMRPKPQQFFGLM	Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11)	17	Free	Free	Linear	Mix	Methylation of phenylalanine at 3rd position	Substance P (SP) analogue	Anticancer drugs	1, 2, 5 and 24 hours	0.1 Î¼g/ml	4.4	Human plasma proteases	RP-HPLC and Electrochemical Detection	Human plasma	in vitro	None	None	Act as growth factors
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
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
2476	8353526	1993	YDPAPPPPPP	Trypsin modulating oostatic factor (TMOF)	10	Acetylation	Free	Linear	L	None	A. aegypti ovary	Growth regulatory peptide	Not mentioned	Not mentioned	1.6	Mosquito ovary endopeptidases	Radioimmunoassay	Ovaries of A. aegypti, Culex quinquefasciatus and Anopheles quadrimaculatus	in vivo	None	None	At concentrations of 3 x 10-9 M and 6.8 x 10-6 M, TMOF inhibited 50 and 90% of trypsin-like enzyme biosynthesis, respectively.
2482	8545241	1995	YGGFLRRIRPKLKWDN	Dynorphin A (DYN A) analog-2	17	Free	Free	Linear	L	The reduced bond psi [CH,-NH] was introduced at position 1-2	Opoid	Physiological effect regulating peptide	0-60 minutes	100 Î¼M peptide solution to 0.18-ml portions of brain membranes	67	Endopeptidase 24-11 (enkephalinase), mouse brain proteases	HPLC	Mouse brain homogenates	in vitro	None	None	Not reported
2484	8545241	1995	YGGFLRRIRPKLKWDN	Dynorphin A (DYN A) analog-4	17	Free	Free	Linear	L	The reduced bond psi [CH,-NH] was introduced at position 4-5	Opoid	Physiological effect regulating peptide	0-60 minutes	100 Î¼M peptide solution to 0.18-ml portions of brain membranes	100	Endopeptidase 24-11 (enkephalinase), mouse brain proteases	HPLC	Mouse brain homogenates	in vitro	None	None	Not reported
2486	8545241	1995	YGGFLRRIRPKLKWDN	Dynorphin A (DYN A) analog-6	17	Free	Free	Linear	L	The reduced bond psi [CH,-NH] was introduced at position 6-7	Opoid	Physiological effect regulating peptide	0-60 minutes	100 Î¼M peptide solution to 0.18-ml portions of brain membranes	80	Endopeptidase 24-11 (enkephalinase), mouse brain proteases	HPLC	Mouse brain homogenates	in vitro	None	None	Not reported
2487	8545241	1995	YGGFLRRIRPKLKWDN	Dynorphin A (DYN A) analog-7	17	Free	Free	Linear	L	The reduced bond psi [CH,-NH] was introduced at position 7-8	Opoid	Physiological effect regulating peptide	0-60 minutes	100 Î¼M peptide solution to 0.18-ml portions of brain membranes	192	Endopeptidase 24-11 (enkephalinase), mouse brain proteases	HPLC	Mouse brain homogenates	in vitro	None	None	Not reported
2488	8545241	1995	YGGFLRRIRPKLKWDN	Dynorphin A (DYN A) analog-8	17	Free	Free	Linear	L	The reduced bond psi [CH,-NH] was introduced at position 8-9	Opoid	Physiological effect regulating peptide	0-60 minutes	100 Î¼M peptide solution to 0.18-ml portions of brain membranes	191	Endopeptidase 24-11 (enkephalinase), mouse brain proteases	HPLC	Mouse brain homogenates	in vitro	None	None	Not reported
2489	8545241	1995	YGGFLRRIRPKLKWDN	Dynorphin A (DYN A) analog-9	17	Free	Free	Linear	L	The reduced bond psi [CH,-NH] was introduced at position 9-10	Opoid	Physiological effect regulating peptide	0-60 minutes	100 Î¼M peptide solution to 0.18-ml portions of brain membranes	93	Endopeptidase 24-11 (enkephalinase), mouse brain proteases	HPLC	Mouse brain homogenates	in vitro	None	None	Not reported
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
2496	19165353	2009	HPLGSPGSASDLETSGLQEQRNHLQGKLSELQVEQTSLEPLQESPRTPGVWKSREVATEGIRGHRKMVLYTLRAPR	NT pro-BNP (N-terminal Pro-Brain natriuretic Peptide)	76	Free	Free	Linear	L	None	Brain Natriuretic Peptide	Diuretic,natriuretic and vasodilatory peptide	Not mentioned	Not mentioned	60-120	Human plasma proteases	Not mentioned	Human plasma	in vitro	http://www.phoenixpeptide.com/catalog/product_info	None	NT-pro-BNP is an independent predictor of postoperative myocardial injury in patients undergoing vascular surgery
2509	19805567	2010	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	Enfuvirtide	36	Acetylation	Free	Linear	L	19 residue is N15 labelled, also have 13C carbon	Enfuvirtide	Antiretroviral fusion inhibitor	5, 15, and 30 min and 1, 2, 4, 8, 24, and 48 h after drug injection	dose, 4 mg/kg of body weight	2.8	Wistar rats blood protease	LC-MS/MS	Female Wistar rats	in vivo	None	None	Showed an EC50 of about 275 nM
2517	17583927	2007	RXRRXRRXRRXRXB	Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO)	34	Free	PMO (5'-ACGTTGAIIIGCATCGTCGC-3')	Linear	L	X = 6-aminohexanoic acid, B = beta-alanine, I = inosine	Cell penetrating peptides-Phosphorodiamidate morpholino oligomers	Cell penetrating peptide	24 hours	150 mg/kg	1.56 ±0.10 (t1/2 Î±)	Rat plasma proteases	MALDI-TOF-MS	Intravenous administration in Rat	in vitro	None	None	LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg
2521	17682073	2007	NQEEVSPYTLLKG	NC100668	13	Acetylation	Tc chelator (NC100194)	Linear	L	Tyr residue at 8 position is Iodionated	Cell penetrating peptides-Phosphorodiamidate morpholino oligomers	Tracer tested for nuclear medical imaging	1, 1.5, 3, 6, 12, and 24 hours	20, 100, 500, 1000, and 2000 Î¼g	1.2	Human plasma proteases	LC-MS	Injected in human plasma	in vivo	None	None	Not reported
2523	17704241	2007	EDYELMDLLAYLK	FROPDOTA	13	Free	lys coupled to the chelator DOTA (DOTA is 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid)	Linear	L	111In radiolabeling	Somatostatin receptor-binding octreotide	Tumor-Targeting Peptide	1, 2, 5, 15, 30, 60, and 120 min	200 Î¼l	71	Human serum proteases	Radioimmunoassay and RP-HPLC	Human serum	in vitro	None	None	The inhibition constant was 494 nM.
2525	3871610	1985	PSSSLHLHRRITHHRRLGCFRSSGSLLNNAMKGGVDDEITLSAYITMALLESSLPDTDP	Rat Î±1- proteinase inhibitor	60	Free	Free	Linear	L	Glycosylation	Rat serum	Protelytic activities regulating peptide	5 minutes, 30 minutes, 1 hour, 4 hour and 7 hour	Not mentioned	170 (for glycosylated Î±1- proteinase inhibitor)	Rat serum proteases	Radioimmunoassay	Wistar rats	in vivo	http://www.uniprot.org/uniprot/Q9JMK6	None	Protect tissue against proteolytic attack by leukocyte elastase
2528	6433008	1984	pGlu-HYSTlLAP-des-Gly	TAP-144	10	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid, des-Gly	LHRH derivative	Gonadotrophins secreting hormone	10 days	1Î¼g/100g body wt	90.6 (t1/2 terminal phase)	Rat serum proteases	Not mentioned	Vaginal administration to Sprague-Dawley rats	in vivo	None	None	Serum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration
2529	6433008	1984	pGlu-HYSTlLAP-des-Gly	TAP-144	10	Free	Ethylamide	Linear	Mix	pGlu=pyroglutamic acid, des-Gly	LHRH derivative	Gonadotrophins secreting hormone	10 days	10Î¼g/100g body wt	109.8 (t1/2 terminal phase)	Rat serum proteases	Not mentioned	Vaginal administration to Sprague-Dawley rats	in vivo	None	None	Serum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration
2532	18586440	2008	HPLGSPGSASDLETSGLQEQRNHLQGKLSELQVEQTSLEPLQESPRTPGVWKSREVATEGIRGHRKMVLYTLRAPR	NT pro-BNP (N-terminal pro B-type natriuretic peptide)	76	Free	Free	Linear	L	None	B-type Natriuretic peptide	Diuretic, Natriuretic and vasodilatory peptide	Not mentioned	Not mentioned	120	Human serum proteases	Not mentioned	Humans	in vivo	http://www.phoenixpeptide.com/catalog/product_info	None	NT-pro-BNP (using a cutoff value of >308 pg/mL) is an independent predictor of postoperative myocardial injury in patients undergoing vascular surgery
2537	10607940	2000	GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA	Insulin-like growth factor-I (IGF-I)	70	Free	Free	Linear	L	I125 labeling	Human IGF-1	Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow	5, 30, 120 and 240 min	100 Î¼l	203 ±10.2 (t1/2Î²)	Rat blood proteases	Radioimmunoassay and bi-exponential equation that describes a two-compartment model	Intravenous bolus administration in Rat	in vivo	632300	None	infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid.
2538	10607940	2000	GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA	Insulin-like growth factor-I (IGF-I)	70	Free	Free	Linear	L	I125 labeling	Human IGF-1	Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow	5, 30, 120 and 240 min	100 Î¼l	185.4 ±4.7 (t1/2Î²)	Rat blood proteases	Radioimmunoassay and bi-exponential equation that describes a two-compartment model	Intravenous bolus administration in Rat	in vivo	632300	None	infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid.
2539	10607940	2000	MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA	LR(3) insulin-like growth factor-I (IGF-I)	83	Free	Free	Linear	L	I125 labeling	Analogue of IGF-I	Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow	5, 30, 120 and 240 min	100 Î¼l	111.1 ±3.9 (t1/2Î²)	Rat blood proteases	Radioimmunoassay and bi-exponential equation that describes a two-compartment model	Intravenous bolus administration in Rat	in vivo	http://www.cellsciences.com/content/p-detail.asp?r	None	At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid.
2540	10607940	2000	MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA	LR(3) insulin-like growth factor-I (IGF-I)	83	Free	Free	Linear	L	I125 labeling	Analogue of IGF-I	Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow	5, 30, 120 and 240 min	100 Î¼l	140.2 ±2.5 (t1/2Î²)	Rat blood proteases	Radioimmunoassay and bi-exponential equation that describes a two-compartment model	Intravenous bolus administration in Rat	in vivo	http://www.cellsciences.com/content/p-detail.asp?r	None	At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid.
2556	4327730	1971	Î²Ala-YSMEHFRYGKPVGKKR-Orn	ACTH analogue- 6	18	Free	Amidation	Linear	L	Î²Ala = Beta alanine, Orn = Ornithine	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	Not mentioned	76.2 (lipolytic activity t1/2)	Rat plasma proteases	Not mentioned	Rat plasma	in vitro	4286483	None	Similar or higher activity in rat than in rabbit (rat = 0.410-6mg/50mg tissue and rabbit = 0.110-6mg/50mg tissue
2557	4327730	1971	Ibu-YSMEHFRYGKPVGKKR-Orn	ACTH analogue- 7	18	Free	Amidation	Linear	L	Ibu = Î±-aminoisobutyric acid	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	Not mentioned	80.63 (lipolytic activity t1/2)	Rat plasma proteases	Not mentioned	Rat plasma	in vitro	4286483	None	Similar or higher activity in rat than in rabbit (rat = 0.0610-6mg/50mg tissue and rabbit = 0.510-6mg/50mg tissue
2558	4327730	1971	Î²Ala-YSMEHfRYGKPVGKKR-Orn	ACTH analogue- 8	18	Free	Amidation	Linear	Mix	Î²Ala = Beta alanine, Orn = Ornithine	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	Not mentioned	88.12 (lipolytic activity t1/2)	Rat plasma proteases	Not mentioned	Rat plasma	in vitro	4286483	None	Similar or higher activity in rat than in rabbit (rat = 0.0710-6mg/50mg tissue and rabbit = 0.210-6mg/50mg tissue
2559	4327730	1971	SYSMEHFRWGKPVGKKRRPVKVYPAGEDDEASEAFPLEF	Purified Sheep Adrenocorticotropic Hormone (ACTH)	39	Free	Free	Linear	L	None	Sheep Adrenocorticotropic Hormone (ACTH)	Steroidogenic peptides	1,2,3 and 4 hours	200 mU	250.87 (lipolytic activity t1/2)	Rat muscle proteases	Not mentioned	Rat muscle slices	in vitro	http://www.genscript.com/peptide/RP11304-ACTH_1-39	None	Not mentionedtive ACTH shows similar activity to rat and rabbit fats when compared in terms of the minimal effective dose (rat = 610-6mg/50mg tissue and rabbit = 510-6mg/50mg tissue)
2561	4327730	1971	Î²Ala-YSMEHFRYGKPVGKKRR	ACTH analogue- 4	18	Free	Amidation	Linear	L	Î²Ala = Beta alanine	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	20 Î¼g	88.2 (lipolytic activity t1/2)	Rat muscle proteases	Not mentioned	Rat muscle slices	in vitro	4286483	None	Showed much higher activity in rabbit fat than in rat fat (rat = 0.610-6mg/50mg tissue and rabbit = 0.0710-6mg/50mg tissue)
2562	4327730	1971	Ibu-YSMEHFRYGKPVGKKRR	ACTH analogue- 5	18	Free	Amidation	Linear	L	Ibu = Î±-aminoisobutyric acid	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	20 Î¼g	122.88 (lipolytic activity t1/2)	Rat muscle proteases	Not mentioned	Rat muscle slices	in vitro	4286483	None	Showed much higher activity in rabbit fat than in rat fat (rat = 0.210-6mg/50mg tissue and rabbit = 0.00210-6mg/50mg tissue)
2563	4327730	1971	Î²Ala-YSMEHFRYGKPVGKKR-Orn	ACTH analogue- 6	18	Free	Amidation	Linear	L	Î²Ala = Beta alanine, Orn = Ornithine	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	Not mentioned	102.62 (lipolytic activity t1/2)	Rat muscle proteases	Not mentioned	Rat muscle slices	in vitro	4286483	None	Similar or higher activity in rat than in rabbit (rat = 0.410-6mg/50mg tissue and rabbit = 0.110-6mg/50mg tissue
2564	4327730	1971	Ibu-YSMEHFRYGKPVGKKR-Orn	ACTH analogue- 7	18	Free	Amidation	Linear	L	Ibu = Î±-aminoisobutyric acid	Octadecapeptide analogues of ACTH	Steroidogenic peptides	1,2,3 and 4 hours	Not mentioned	261.78 (lipolytic activity t1/2)	Rat muscle proteases	Not mentioned	Rat muscle slices	in vitro	4286483	None	Similar or higher activity in rat than in rabbit (rat = 0.0610-6mg/50mg tissue and rabbit = 0.510-6mg/50mg tissue
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.
2572	8403527	1993	ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF	Calcitonin gene-related peptide (CGRP)	37	Free	Free	Linear	L	None	Human Vasopressin	Vasoactive peptide	2,4,6,8, 10, 15,20,25,30,40,50,60 and 90 min.	Not mentioned	63.9 ±4.5	Rat kidney proteases	Not mentioned	Isolated perfused rat kidney	in vivo	http://www.uniprot.org/blast/?about=P06881[83-119]	None	Not reported
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
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
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
2595	16287259	2005	HHLGGAKQAGDV	H12 (Fibrinogen Î³ chain dodecapeptide)	12	Free	Free	Linear	L	conjugated with PEG	Derived from Fibrinogen gamma chain	Induce Thrombosis	Not mentioned	40mg/kg peptide infused	200 ±23	Proteases from (thrombocytopenic rats)plasma	Spectrofluorometer	Rat(thrombocytopenic)plasma	in vivo	None	None	10 mg/kg slightly reduced the Bleeding time to 573 ± 127 seconds in comparison control group 618 ± 51 seconds
2608	17408666	2007	PPPPPARPYSFGL	Cydiastatin 4-alpha	13	Free	Amidation	Linear	L	None	Synthetic	Neuropeptides	30 °C for 20 minutes	1nmol	71	M. sexta larval midgut tissue extract proteases	RP-HPLC	Midgut tissues of M. sexta	in vitro	None	None	Not reported
2611	17408666	2007	PPPPPARPYSF-(Acpc)	Cydiastatin 4-alpha	12	Free	Amidation	Linear	L	Acpc=cyclopropylalanine	Synthetic	Neuropeptides	30 °C for 20 minutes	1nmol	116	M. sexta larval midgut tissue proteases	RP-HPLC	Midgut tissue	in vitro	None	None	Not reported
2625	17532097	2007	FGGFTGARKSARKLANQ	N/OFQ (Nociceptin/Orphanin FQ peptide receptor)	17	Free	Free	Linear	L	None	Derived from the prepronociceptin protein	NOP-Receptor ligands	37 °C for 240 min	6 Î¼g/Î¼l	64 ±1	Mouse plasma proteases	RP-HPLC	Mouse Plasma	in vitro	None	None	Hypotensive and bradycardic effects evoked by N/OFQ after i.v. administration in rats, was lasting (about 10 min)
2628	17532097	2007	FGG-(pF)F-TG-Aib-RKSARKRKNQ	UFP-112 (Nociceptin/Orphanin FQ receptor antagonist)	17	Free	Amidation	Linear	L	(pF)F = p-flouro Phenylalanine; Aib= 2-Aminoisobutyric acid	Synthetic	NOP-Receptor ligands	37 °C for 240 min	6 Î¼g/Î¼l	167 ±9	Mouse plasma proteases	RP-HPLC	Mouse Plasma	in vitro	20497197	None	Hypotensive and bradycardic effects evoked by UFP-112 after i.v. administration in rats wast lasting for (i.e. 80 min
2629	17766836	2003	Pyr-Glu-LYENKPRRPYIL	Neurotensin (NT)	13	Free	Free	Linear	L	Pyr-Glu= pyro-glutamate	Neurotransmitter-like hypothalamic peptide	Regulates luteinizing hormone and prolactinrelease	37 °C for 2-24 hours	Not mentioned	<2	Human plasma proteases	HPLC-MS	Human plasma	in vivo	None	None	Tetra-branched NT(8-13)-methotrexate cause 60% reduction in tumor growth was observed with respect to mice treated with free drug
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
2638	21185160	2011	VDKPPYLPRPRPPRRIYNR	O-1(Oncocin)	19	Free	Amidation	Linear	L	None	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	68 ±15	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 8 Î¼g/mL M.luteus
2640	21185160	2011	VDKPPYLPRPRPPRRIYN	O-2 (Oncocin)	18	Free	Free	Linear	L	None	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	120	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 64 Î¼g/mL in E.coli BL21A1 and 128 Î¼g/mL M.luteus
2641	21185160	2011	VDKPPYLPRPRPPRRIYNN	O-4 (Oncocin)	19	Free	Amidation	Linear	L	None	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	120	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC =16Î¼g/mL in E.coli BL21A1 and 64 Î¼g/mL M.luteus
2642	21185160	2011	VDKPPYLPRPRPPRRIYNH	O-5 (Oncocin)	19	Free	Amidation	Linear	L	None	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	90 ±1	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 16 Î¼g/mL in E.coli BL21A1 and 16 Î¼g/mL M.luteus
2643	21185160	2011	VDKPPYLPRPRPPRRIYN-Orn	O-6 (Oncocin)	19	Free	Amidation	Linear	L	Orn=Ornithine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	210 ±60	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and 16 Î¼g/mL M.luteus
2644	21185160	2011	VDKPPYLPRPRPPRRIYN-Agp	O-7 (Oncocin)	19	Free	Amidation	Linear	L	Agp = Î±-amino-3-guanidinopropionic acid	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	98 ±6	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and 8Î¼g/mL M.luteus
2645	21185160	2011	VDKPPYLPRPRPPRRIYN-Nir	O-8 (Oncocin)	19	Free	Amidation	Linear	L	Nir=Nitro-arginine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	78 ±2	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and 16 Î¼g/mL M.luteus
2646	21185160	2011	VDKPPYLPRPRPPRRIYN-Nmr	O-9 (Oncocin)	19	Free	Amidation	Linear	L	Nmr =N-methylarginine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	79 ±3	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and 4 Î¼g/mL M.luteus
2647	21185160	2011	VDKPPYLPRPRPPRRIYN-Har	O-10 (Oncocin)	19	Free	Amidation	Linear	L	Har=Homoarginine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	94 ±1	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and8 Î¼g/mL M.luteus
2648	21185160	2011	VDKPPYLPRPRPPRRIYNr	O-11 (Oncocin)	19	Free	Amidation	Linear	Mix	D-Arg at 19th position	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	160 ±5	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 4Î¼g/mL in E.coli BL21A1
2649	21185160	2011	VDKPPYLPRPRPPRRIYNR-NHpr	O-12 (Oncocin)	19	Free	Propylamidation	Linear	L	None	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	>120	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 8 Î¼g/mL M.luteus
2650	21185160	2011	VDKPPYLPRPRPPR-Orn-IYNR	O-14 (Oncocin)	19	Free	Amidation	Linear	L	orn =Ornithine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	90	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and 16 Î¼g/mL M.luteus
2651	21185160	2011	VDKPPYLPRPRPPR-beta-Hr-IYNR	O-15 (Oncocin)	19	Free	Amidation	Linear	L	Beta-Hr =Î²-homoarginine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	150	Mouse serum proteases	MALDI-TOF-MS	25% mouse serum	in vivo	None	None	MIC = 4Î¼g/mL in E.coli BL21A1 and 16 Î¼g/mL M.luteus
2654	21185160	2011	VDKPPYLPRPRPPR-Har-IYN-Agp	O-18 (Oncocin)	19	Free	Amidation	Linear	L	Har=Homoarginine, Agp = Î±-amino-3-guanidinopropionic acid	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	62 ±4	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 4 Î¼g/mL M.luteus
2655	21185160	2011	VDKPPYLPRPRPPR-Agp-IYN-Har	O-19 (Oncocin)	19	Free	Amidation	Linear	L	Har=Homoarginine, Agp = Î±-amino-3-guanidinopropionic acid	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	111 ±6	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 2 Î¼g/mL M.luteus
2656	21185160	2011	VDKPPYLPRPRPPR-Agp-IYN-Agp	O-20 (Oncocin)	19	Free	Amidation	Linear	L	Agp = Î±-amino-3-guanidinopropionic acid	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	171 ±20	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC =8 Î¼g/mL in E.coli BL21A1 and 4 Î¼g/mL M.luteus
2657	21185160	2011	VDKPPYLPRPRPPR-Orn-IYN-Har	O-21 (Oncocin)	19	Free	Amidation	Linear	L	Har=homoarginine, Orn=Ornithine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	75 ±1	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 4 Î¼g/mL M.luteus
2658	21185160	2011	VDKPPYLPRPRPPR-Orn-IYN-Agp	O-22 (Oncocin)	19	Free	Amidation	Linear	L	Agp = Î±-amino-3-guanidinopropionic acid, Orn=Ornithine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	103 ±5	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 4 Î¼g/mL M.luteus
2659	21185160	2011	VDKPPYLPRPRPPR-Orn-IYN-Orn	O-23(Oncocin)	19	Free	Amidation	Linear	L	Orn=Ornithine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	176 ±8	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC = 8 Î¼g/mL in E.coli BL21A1 and 8 Î¼g/mL M.luteus
2661	21185160	2011	VDKPPYLPRPRPPR-Orn-IYNR	O-25 (Oncocin)	19	Free	Propylamidation	Linear	L	Orn=Ornithine	2kDa Oncopeltus peptide derivatives	Antimicrobial	30-480 Minutes	7.5 Î¼g/100Î¼l	102 ±2	Mouse serum proteases	MALDI-TOF-MS	Full mouse serum	in vivo	None	None	MIC = 4 Î¼g/mL in E.coli BL21A1 and 8 Î¼g/mL M.luteus
2671	22263969	2012	SLRRSSCFGGRMDRIGAQSGLGCNSFRY(GGS)3GG-Fc region	2m (monomer Atrial natriuretic peptide- Fc )	39	Free	Fc region	Cyclic (C7-C23 & C-residues of Fc region)	L	None	Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation.	Natriuretic and vasodilator	4-72 hours	0.5mg/kg of protein	3.9	Rat plasma proteases	ELISA	Female Wistar rats Plasma	in vivo	None	None	Not reported
2672	22263969	2012	SLRRSSCFGGRMDRIGAQSGLGCNSFRYGS(GGS)4GG-Fc region	3m (monomer Atrial natriuretic peptide- Fc )	42	Free	Fc region	Cyclic (C7-C23 & C-residues of Fc region)	L	None	Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation.	Natriuretic and vasodilator	4-72 hours	0.5mg/kg of protein	4.5	Rat plasma proteases	ELISA	Female Wistar rats Plasma	in vivo	None	None	Not reported
2673	22263969	2012	{[SLRRSSCFGGRMDRIGAQSGLGCNSFRY(GGS)3GG]2}-Fc region	2d (Atrial natriuretic peptide- Fc dimer)	78	Free	Fc region	Cyclic (C7-C23 & C-residues of Fc region)	L	None	Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation.	Natriuretic and vasodilator	4-72 hours	0.5mg/kg of protein	2.8	Rat plasma proteases	ELISA	Female Wistar rats Plasma	in vivo	None	None	Not reported
2681	24588343	2014	EGTFTSDVSSYLEGQAAKEFIAWLVKGR	GLP-1(9-36)(Glucagon Like protein-1)	28	Free	Amidation	Linear	L	None	Glucagon Like protein-1 (GLP-1)	Vasodialator	5-120 minutes	10mg/ml	>240	Serum and plasma proteases	LC-MS	Male beagle dog plasma	in vitro	None	None	Not reported
2682	24588343	2014	EGTFTSDVSSYLEGQAAKEFIAWLVKGR	GLP-1(9-36)(Glucagon Like protein-1)	28	Free	Amidation	Linear	L	None	Glucagon Like protein-1 (GLP-1)	Vasodialator	4 hours at 37C	1 µM	>110	Dog hepatocyte proteases	LC-MS	Male beagle dog hepatocyte	in vitro	None	None	Not reported
2689	25039358	2014	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	Derived from Saliva of Gila monster	GLP-1 receptor agonist	37 °C for 2-72 hours	1000ng/ml	4.8	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vitro	None	None	GLP-1 receptor Activation potency with EC50 =1.6 ± 0.4 pM in HEK-293 cells
2699	25039358	2014	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	Derived from Saliva of Gila monster	GLP-1 receptor agonist	37 °C for 2-72 hours	1000ng/ml	2.5 ±1.2	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vivo	None	None	GLP-1 receptor Activation potency with EC50 =1.6 ± 0.4 pM in HEK-293 cells
2702	25243635	2014	HAEGTFTSDVSCYLEGQAACEFIAWLVKGRG	VGLP1 (Glucagon like peptide 1 derivative)	31	Free	Free	Cyclic (C18-C26)	L	None	Glucagon Like protein-1 (GLP-1)	Antihyperglycemic	37 °C for 0.1-24 hours	500Î¼g	<5	DPP IV	ELISA	DPP IV	in vitro	None	None	Not reported
2706	25243635	2014	HAEGTFTSDVSCYLEGQAACEFIAWLVKGRGVVVVVV	VGLP1V6 (Glucagon like peptide 1 derivative)	37	Free	Free	Cyclic (C12-C20)	L	None	Glucagon Like protein-1 (GLP-1)	Antihyperglycemic	37 °C for 0.1-24 hours	500Î¼g	~ 5	DPP IV	ELISA	DPP IV	in vitro	None	None	Not reported
2709	25324697	2014	MIFVKTLTGKTIL	SHSMP(Sadat-Habdan Mesenchymal stimulating Peptide)	13	Free	Free	Linear	L	None	SHSMP(Sadat-Habdan Mesenchymal stimulating Peptide)	Angiogenesis Factor	Blood sample collected after 30-480 minutes after the infusion of peptide	5mg/kg	90	Rat plasma proteases	HPLC	Sprague Dawley rats (Dose i/m injected)	in vivo	Patent US7399826 B1	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
2712	25594223	2015	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	ENF(Enfuvirtide)	36	Acetylation	Amidation	Linear	L	None	Enfuvirtide	Anti-viral (Anti-HIV activity)	0.5-24 hours	1.7Î¼M/Kg	1.5	Rat plasma proteases	HPLC	Sprague-Dawey (SD) rats Plasma	in vivo	None	None	EC50 = 3nM for Anti-viral potency
2714	25594223	2015	CYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	Lac-ENF (Lactic acid Enfuvirtide)	37	Lactic acid	Amidation	Linear	L	None	Synthetic derived from glycosylated ENFs	Anti-viral	0.5-24 hours	1.7Î¼M/Kg	4.2	Rat plasma proteases	HPLC	Sprague-Dawey (SD) rats Plasma	in vivo	None	None	EC50 = 2nM for Anti-viral potency
2723	25771000	2015	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Free	Linear	L	None	GLP-1 derived peptide	Regulate blood glucose	0.5-24 hours	0.5 mg/kg	3.03	db/db mice plasma proteases	LC-MS/MS	db/db Mice plasma (Dose i/v injected)	in vivo	None	None	AUC for glucose -stimulated 1st phase insulin secretion in Exendin-4 -treated mice (20nmol/kg) is 1.62 fold higher than control
2724	25771000	2015	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Free	Linear	L	None	GLP-1 derived peptide	Regulate blood glucose	0.5-24 hours	0.5 mg/kg	>3	Rabbit plasma proteases	LC-MS/MS	New Zealand White Rabbit plasma (Dose i/v injected)	in vivo	None	None	AUC for glucose -stimulated 1st phase insulin secretion in Exendin-4 -treated mice (20nmol/kg) is 1.62 fold higher than control
2725	25900863	2015	TTWEAWDRAIAEYAARIEALLRALQEQQEKNEAALREL	TRI-1144	38	Acetylation	Amidation	Linear	L	None	Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus.	HIV-fusion inhibitor	Blood sample collected after 1-168 hours after the infusion of peptide	800nmol/Kg dose injected	4.2	Rat plasma proteases	LC-MS/MS	Intravenously administered to Sprague €“Dawley rats	in vivo	None	None	Not reported
2731	26197931	2015	YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	Porcine-PYY(1-36)	36	Free	Free	Linear	L	None	Synthetic peptide hormone released from enteroendocrine cells	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	37 °C for 24 hours	Not mentioned	3.4 ±0.2	Pig blood proteases	Radioimmunoassay and HPLC	Female pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide)	in vitro	None	None	Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L
2738	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR	G36A or [GLP-1(7-36A)]	30	Free	Amidation	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp	0.4 µM	4 ±0.2	Human plasma proteases + DPP IV	MS	Citrate + Human plasma	in vitro	None	None	Not reported
2739	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR	G36A or [GLP-1(7-36A)]	30	Free	Amidation	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp	0.4 µM	4 ±0.2	Human serum proteases + DPP IV	MS	Serum	in vitro	None	None	Not reported
2744	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR	G36A or [GLP-1(7-36A)]	30	Free	Amidation	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	Room Temp	0.4 µM	2 ±0.4	Human blood proteases + DPP IV	MS	EDTA whole blood	in vitro	None	None	Not reported
2752	26222180	2015	HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGRG	G 37 or [GLP-1(7 €“37)]	31	Free	Free	Linear	L	None	Glucagon-like peptide 1 (GLP-1)	Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)	On ice	0.4 µM	5 ±1.0	Human blood proteases + DPP IV	MS	EDTA whole blood	in vitro	None	None	Not reported
2762	26308095	2015	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Saliva of Gila monster	Regulates blood glucose by upregulating the insulin secretion	Blood sample collected after7-288 hours after the injection of peptide	5nmol/Kg	02-Mar	Proteases from mini-pig plasma	ELISA, LC/MS	Mini-pigs plasma (Dose s/c injected)	in vivo	None	None	Not reported
2769	26325323	2015	p-Gln-HWSYwLRPG	Compound 1(lactose [Q1][w6]LHRH )	10	Lactose	Amidation	Linear	L	Lactose at N-ter, pyro-Glutamine at n-ter, D-Trp at 6 pos	Hypothalamus	Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH)	Blood sample collected after0.5-24 hours after the injection of peptide	2.5mg/Kg	2.9 ±0.63	Rat plasma proteases	LC/MS	Rat Plasma (Dose i/v injected)	in vivo	None	None	Increase in the level of LH was observed i.e. nAUC = 11.33 ± 1.65 ng/24 hafter oral administration of 20 mg/kg of compound 1 compared to the control nAUC = 4.45 ± 1.028 ng/24 h
2770	26325323	2015	p-Gln-HWSYwLRPG	Compound 1(lactose [Q1][w6]LHRH )	10	Lactose	Amidation	Linear	L	Lactose at N-ter, pyro-Glutamine at n-ter, D-Trp at 6 pos	Hypothalamus	Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH)	Blood sample collected after0.5-24 hours after the injection of peptide	10mg/Kg	2.6 ±0.84	Rat plasma proteases	LC/MS	Rat Plasma (Dose i/p injected)	in vivo	None	None	Increase in the level of LH was observed i.e. nAUC = 11.33 ± 1.65 ng/24 hafter oral administration of 20 mg/kg of compound 1 compared to the control nAUC = 4.45 ± 1.028 ng/24 h
2776	26400022	2015	fPRPGGGGQGDFEPIPEDAYDE	Peptide S2 (Hirudin mimetic peptide)	22	Free	Amidation	Linear	Mix	Stearic acid at Lys	Hirudin derived	Anti-coagulant	Not mentioned	1.0Î¼M/Kg	212.2 ±58.4	Rat plasma proteases	HPLC, MS-MS	Sprague-Dawley (SD) rats plasma (Dose i/v injected)	in vivo	None	None	Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 15.24 ± 0.18 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.75 ± 0.46nM
2781	21459096	2011	EVKYDPCFGHKIDRINHVSNLGCPSLRDPRPNAPSTSA	DNP (Dendroaspis natriuretic peptide)	39	Free	Free	Cyclic (C7-C23)	L	None	Dendroaspis natriuretic peptide	Natriuretic and hypotensive activities	37 °C for 0-125 minutes	Not mentioned	159	Human kidney proteases	Not mentioned	Human kidney membrane extract	in vitro	19395584	None	Not reported
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
2801	24874704	2014	YRQSMNNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY	PEGylated AM	52	Pegylation	Amidation	Cyclic (Ringed structure formed by C16-C21)	L	None	Isolated from Human pheochromocytoma	Vasodilator and cardiovascular protection	Not mentioned	3nmol/kg Dose	108 ±12 min (2nd plasma half life)	Rat plasma proteases	ELISA	Male Wistar rats plasma	in vivo	http://www.genscript.com/peptide/RP11288-Adrenomed	None	PEGylated AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.519 ± 0.10 and9.44 ± 0.30 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
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
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
2828	1346149	1992	SANSNPAMAPRERKAGCKNFFWKTFTSC	SS-28 (Somatostatin-28)	28	Free	Free	Cyclic (C17-C28)	L	None	Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus.	Inhibitor of growth hormone release	37 °C for 30-180 minutes	50Î¼M	228.1 ±76.5 (Metabolic half life)	Brodmann Area tissues proteases	Radioimmunoassay	Brodmann Area tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY)	in vitro	None	None	Not reported
2829	1346149	1992	SANSNPAMAPRERKAGCKNFFWKTFTSC	SS-28 (Somatostatin-28)	28	Free	Free	Cyclic (C17-C28)	L	None	Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus.	Inhibitor of growth hormone release	37 °C for 30-180 minutes	50Î¼M	257.81 ±86.2(Metabolic half life)	Brodmann Area tissues proteases	Radioimmunoassay	Brodmann Area tissues of brain of SDAT(Medical Research Council Brain Bank, Cambridge, England)	in vitro	None	None	Not reported
2830	1346149	1992	SANSNPAMAPRERKAGCKNFFWKTFTSC	SS-28 (Somatostatin-28)	28	Free	Free	Cyclic (C17-C28)	L	None	Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus.	Inhibitor of growth hormone release	37 °C for 30-180 minutes	50Î¼M	260.4 ±129.8 (Metabolic half life)	Hippucampal tissues proteases	Radioimmunoassay	Hippocampus tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY)	in vitro	None	None	Not reported
2832	1346149	1992	AGCKNFFWKTFTSC	SS-14 (Somatostatin-14)	14	Free	Free	Cyclic (C3-C14)	L	None	Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus.	Inhibitor of growth hormone release	37 °C for 30-180 minutes	50Î¼M	140.1 ±36.5 (Metabolic half life)	Brodmann Area tissues proteases	Radioimmunoassay	Brodmann Area tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY)	in vitro	None	None	Not reported
2833	1346149	1992	AGCKNFFWKTFTSC	SS-14 (Somatostatin-14)	14	Free	Free	Cyclic (C3-C14)	L	None	Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus.	Inhibitor of growth hormone release	37 °C for 30-180 minutes	50Î¼M	129.8 ±53.2(Metabolic half life)	Hippucampul tissues proteases	Radioimmunoassay	Hippucampus tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY)	in vitro	None	None	Not reported
2834	1346149	1992	AGCKNFFWKTFTSC	SS-14 (Somatostatin-14)	14	Free	Free	Cyclic (C3-C14)	L	None	Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus.	Inhibitor of growth hormone release	37 °C for 30-180 minutes	50Î¼M	79.8 ±11.1(Metabolic half life)	Hippucampul tissues proteases	Radioimmunoassay	Posterior Hippucampus tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY)	in vitro	None	None	Not reported
2842	1723638	1991	GWTLNSAGYLLGPHAIDNHRvSFHDKYGLA	Galanin(1-29)	29	Free	Amidation	Linear	L	None	Neuropeptide	Neuroendocrine activities, stimulates growth hormone secretion	37 °C	1 Î¼M	100	Hypothalamic membrane protaeses	HPLC	Hypothalamic membranes of Male Sprague-Dawley rats	in vitro	None	None	Not reported
2850	1826667	1991	YADAIFT-(cyclo-D)-SYR-(cyclo-K)-VLAQLSARKLLQDIMSR	[Asp8,Ala15]Cyclo(Asp8-Lys12)GRF(1-29)-NH2	29	Free	Amidation	Linear	L	None	Synthetic(GRF-1 analogs)	Release growth hormone	Not mentioned	100 µg/ml	~ 4	Porcine plasma proteases	HPLC	Porcine plasma	in vitro	None	None	Not reported
2851	1826667	1991	YADAIFT-(cyclo-D)-SYR-(cyclo-K)-VLAQLSARKLLQDIMSR	[D-Ala2,Asp8,Ala15]Cyclo(Asp8-Lys12)GRF(1-29)-NH2	29	Free	Amidation	Linear	Mix	Cyclo-Asp at 8th position, cyclo-Lys at 12 position	Synthetic(GRF-1 analogs)	Release growth hormone	Not mentioned	100 µg/ml	>4	Porcine plasma proteases	HPLC	Porcine plasma	in vitro	None	None	Not reported
2852	1826667	1991	YADAIFTNSYRVLAQLSAR-(cyclo-K)LLQ-(cyclo-D)-IMSR	[Ala15 ]Cyclo(Lys21 -Asp 25)GRF(1 -29)-NH2	29	Free	Amidation	Linear	L	None	Synthetic(GRF-1 analogs)	Release growth hormone	Not mentioned	100 µg/ml	>4	Porcine plasma proteases	HPLC	Porcine plasma	in vitro	None	None	Not reported
2853	1826667	1991	YaDAIFTNSYRKVLAQLSAR-(cyclo-K)LLQ-(cyclo-D)-IMSR	[D-Ala2,Ala15]Cyclo(Lys21-Asp25)GRF(1-29)-NH2	29	Free	Amidation	Linear	Mix	None	Synthetic(GRF-1 analogs)	Release growth hormone	Not mentioned	100 µg/ml	>4	Porcine plasma proteases	HPLC	Porcine plasma	in vitro	None	None	Not reported
2854	1826667	1991	YADAIFT-(cyclo-D)-SYR-(cyclo-K)-VLAQLSAR-(cyclo-K)LLQ-(cyclo-D)IMSR	[Asp8,Ala15]Cyclo(Asp8-Lys12)(Lys21-Asp25)GRF(1-29)-NH2	29	Free	Amidation	Linear	L	None	Synthetic(GRF-1 analogs)	Release growth hormone	Not mentioned	100 µg/ml	>4	Porcine plasma proteases	HPLC	Porcine plasma	in vitro	None	None	Not reported
2856	1889124	1991	AQKVNSGEPRAHLGALLARYIQQARKAPSGRMSVIKNLQNLDPSHRISDRDYMGWMDF	CCK58 (Cholecystokinin 58)	58	Free	Amidation	Linear	L	None	Peptide hormone of the gastrointestinal system	Stimulates digestion of fat & protein	37 °C for 30-180 minutes	1.6pmol	69 ±8	Normal Human blood proteases	Radioimmunoassay and HPLC	Normal Human blood	in vitro	None	None	Not reported
2873	2940625	1986	pyr-EHWSYwLRPG	[D-Trp6]-LHRH (Luteinizing hormone-releasing hormone)	10	Free	Amidation	Linear	Mix	Pyr=Pyro-glutamic acid	LHRH (Luteinizing hormone-releasing hormone) derivative	Release Luteinizing hormone	Blood collected 1-240 minutes after peptide infused	100 µg/ml	>84 (beta t1/2)	Dog plasma proteases	HPLC	Two male Beagle dogs plasma (Dose s/c injected)	in vivo	None	None	Not reported
2889	2970910	1988	pEHWSY{nnr:Nal}{d}LRPG{ct:Amid}	Naferlin	10	Free	Amidation	Linear	L	pE=Pyro-glutamate, D-alanin= 3-(2Naphthyl)-D-alanine	GnRH (Gonadotropin releasing hormone) agonist	It decreases pituitary secretion of the gonadotropins	Not mentioned	400 µg	2.3 ±0.2	Human serum proteases	Radioimmunoassay	Subcutaneous route of injection in human serum	in vivo	None	None	Not reported
2890	2970910	1988	pEHWSY-(D-Nal(2))LRPG	Naferlin	10	Free	Amidation	Linear	L	pE=Pyro-glutamate, D-alanin= 3-(2Naphthyl)-D-alanine	GnRH (Gonadotropin releasing hormone) agonist	It decreases pituitary secretion of the gonadotropins	Not mentioned	304 ± 2.2 µg	2.7 ±0.2	Human serum proteases	Radioimmunoassay	Nasal route of injection in human serum	in vivo	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
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
2938	2454805	1988	GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA	[125I]IGF-I	70	Free	Free	Linear	L	None	Human Recombinant peptide	Stmulates glycogen synthesis	Blood collected 10 minutes to 6 hours after peptide injection	1 µCi peptide injected to rhesus monkey	100	Proteases from Rat serum	Radioimmunoassay	Rat Serum	in vivo	None	None	Stimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm
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
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
2961	2524034	1989	GGFMTSEKSQTPLVTL	DE-gamma-E (Des-enkephalin-gamma-endorphin)	18	Free	Free	Linear	L	None	Neuroleptic peptide	Neuroregulator	Not mentioned	Peptide 0.04 w/v in 154mM KCl + 0.25% w/v Na2EDTA co-administeration	93 ±45	Proteases from rat rectal proteases	HPLC	Rat rectal lumen	in vitro	None	None	Not mentioned
2964	2556215	1989	DRVYIHPFHL	Angiotensin I (AI)	10	Free	Free	Linear	L	None	Derived from angiotensin	Precusor of angiotensin- II (AII)	37 °C	100 - 2000 ng/ml	4	Fetal calf serum proteases	Radioimmunoassay	Primary endothelial cells + Fetal calf Serum (5%)	in vitro	None	None	Not mentioned
2965	2556215	1989	DRVYIHPFHL	Angiotensin I (AI)	10	Free	Free	Linear	L	None	Derived from angiotensin	Precusor of angiotensin- II (AII)	37 °C	100 - 2000 ng/ml	1.9	Fetal calf serum proteases	Radioimmunoassay	Primary endothelial cells + Fetal calf Serum (10%)	in vitro	None	None	Not mentioned
2969	2556215	1989	DRVYIHPFHL	Angiotensin I (AI)	10	Free	Free	Linear	L	None	Derived from angiotensin	Precusor of angiotensin- II (AII)	37 °C	100 - 2000 ng/ml	4	Fetal calf serum proteases	Radioimmunoassay	Primary endothelial cells + Fetal calf Serum(10%) + converting enzyme inhibitor (MK422) with conc 10-6 M	in vitro	None	None	Not mentioned
2970	2556215	1989	DRVYIHPFHL	Angiotensin I (AI)	10	Free	Free	Linear	L	None	Derived from angiotensin	Precusor of angiotensin- II (AII)	37 °C	100 - 2000 ng/ml	1.2	Fetal calf serum proteases	Radioimmunoassay	Primary endothelial cells + Fetal calf Serum (20%) + converting enzyme inhibitor (MK422) with conc 10-6 M	in vitro	None	None	Not mentioned
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
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
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
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
2997	8353526	1993	YDPAPPPPPP	TMOF (Trypsin modulatinf oostatic factor)	10	Free	Free	Linear	L	None	Hormone is secreted from the ovary of Mosquitoes	Inhibitor of trypsin and chymotrypsin biosynthesis	Not mentioned	30ng/group	1.6	Proteases from A. aegypti blood	RP-HPLC	A. aegypti blood	in vivo	None	None	Not reported
2998	8403527	1993	ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF	CGRP(Calcitonin gene related peptide)	37	Free	Amidation	Cyclic (C2-C7)	L	None	Neuropeptide and alernative spliced product of calcitonon produced by thyroid gland	Vasodilator	Blood sample collected after 2-90 minutes	1.0 pmol/ml of peptide	63.9 ±4.5	Rat plasma proteases and isolated perfused rat kidney	Not mentioned	Rat plasma (+IPRK (isolated perfused rat kidney)filtering)	in vitro	None	None	Not reported
3001	8545241	1995	YGGFLRRIRPK	Dynorphin A(1-11)-NH2 analogue 2 (DYN A analogue)	11	Free	Amidation	Linear	L	None	Human placenta Dynorphin A derivative	Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.	37 °C	100 µM	67	Proteases from mouse brain tissues	HPLC	Mouse brain homogenate	in vitro	None	None	Not reported
3003	8545241	1995	YGGFLRRIRPK	Dynorphin A(1-11)-NH2 analogue 4 (DYN A analogue)	11	Free	Amidation	Linear	L	None	Human placenta Dynorphin A derivative	Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.	37 °C	100 µM	100	Proteases from mouse brain tissues	HPLC	Mouse brain homogenate	in vitro	None	None	Not reported
3005	8545241	1995	YGGFLRRIRPK	Dynorphin A(1-11)-NH2 analogue 6 (DYN A analogue)	11	Free	Amidation	Linear	L	None	Human placenta Dynorphin A derivative	Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.	37 °C	100 µM	80	Proteases from mouse brain tissues	HPLC	Mouse brain homogenate	in vitro	None	None	Not reported
3006	8545241	1995	YGGFLRRIRPK	Dynorphin A(1-11)-NH2 analogue 7 (DYN A analogue)	11	Free	Amidation	Linear	L	None	Human placenta Dynorphin A derivative	Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.	37 °C	100 µM	192	Proteases from mouse brain tissues	HPLC	Mouse brain homogenate	in vitro	None	None	Not reported
3007	8545241	1995	YGGFLRRIRPK	Dynorphin A(1-11)-NH2 analogue 8 (DYN A analogue)	11	Free	Amidation	Linear	L	None	Human placenta Dynorphin A derivative	Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.	37 °C	100 µM	191	Proteases from mouse brain tissues	HPLC	Mouse brain homogenate	in vitro	None	None	Not reported
3008	8545241	1995	YGGFLRRIRPK	Dynorphin A(1-11)-NH2 analogue 9 (DYN A analogue)	11	Free	Amidation	Linear	L	None	Human placenta Dynorphin A derivative	Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.	37 °C	100 µM	93	Proteases from mouse brain tissues	HPLC	Mouse brain homogenate	in vitro	None	None	Not reported
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
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
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
3026	18424366	2008	HAEGTFTSDVSSYLEGQAAKEFIAWLVK	GLP(7-34) (Glucagon like peptide)	28	Acetylation	Amidation	Linear	L	None	GLP-1 (Glucagon like peptide-1) analogue	Antihyperglycemic or incretin effect (Stimulate Insulin release in glucose dependent manner)	37C for 2 hours	200 µg/ml	>2	DPP IV	MALDI-TOF-MS	Peptide in 0.01 M Na2HPO4 buffer	in vitro	None	None	In the DPP-IV-free rat pancreatic beta cell line RINm5F GLP-1-(7-34)-amide elevated cAMP production with an EC50 of about 40 nM
3035	24361089	2014	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF	Teriparatide	34	Free	Free	Linear	L	None	Parathyroid Hormone derivative	Increase the concentration of ionic calcium (Ca2+) in the blood	Not mentioned	Not available	5 (Elimination half life)	Proteases from human plasma(Severe renal impairment patients)	Not mentioned	Human plasma (Severe renal impairment patients)	in vivo	None	None	Not reported
3036	24361089	2014	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF	Teriparatide	34	Free	Free	Linear	L	None	Parathyroid Hormone derivative	Increase the concentration of ionic calcium (Ca2+) in the blood	Not mentioned	Not available	1.5 (Elimination half life)	Proteases from human plasma(Normal)	Not mentioned	Human plasma (Normal)	in vivo	None	None	Not reported
3046	7994807	1994	ANTFLEEVRKGNLERECVEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHVNITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQECSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASAQAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETGDGLDEDSDRAIEGRTA	Prothrombin fragment 1.2	273	Free	Free	Linear	L	None	Prothrombin	Not mentioned	Not reported	Not reported	90	Human blood proteases in presence of Hirudin (anti-coagulant)	Radioimmunoassay ,ELISA	Human blood plasma sample	in vivo	3759958, 2824564	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
3087	15656696	2005	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	Enfuvirtide	36	Acetylation	Amidation	Linear	L	None	Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein.	Inhibits de novo infection and cell-to-cell HIV-1 virus transmission	Not mentioned	90mg	3.16(t1/2Î²)	Human blood proteases	liquid chromatography-tandem mass spectrometry method	Intravenous injection in 12 HIV patients,blood samples	in vivo	http://www.drugbank.ca/drugs/DB00109	None	Not mentioned
3088	15656696	2005	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	Enfuvirtide	36	Acetylation	Amidation	Linear	L	None	Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein.	Inhibits de novo infection and cell-to-cell HIV-1 virus transmission	Not mentioned	45mg	3.46(t1/2Î²)	Human blood proteases	liquid chromatography-tandem mass spectrometry method	Subcutaneous injection in 12 HIV patients,blood samples	in vivo	http://www.drugbank.ca/drugs/DB00109	None	Not mentioned
3089	15656696	2005	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	Enfuvirtide	36	Acetylation	Amidation	Linear	L	None	Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein.	Inhibits de novo infection and cell-to-cell HIV-1 virus transmission	Not mentioned	90mg	3.8(t1/2Î²)	Human blood proteases	liquid chromatography-tandem mass spectrometry method	Subcutaneous injection in 12 HIV patients,blood samples	in vivo	http://www.drugbank.ca/drugs/DB00109	None	Not mentioned
3090	15656696	2005	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	Enfuvirtide	36	Acetylation	Amidation	Linear	L	None	Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein.	Inhibits de novo infection and cell-to-cell HIV-1 virus transmission	Not mentioned	180mg	4.35(t1/2Î²)	Human blood proteases	liquid chromatography-tandem mass spectrometry method	Subcutaneous injection in 12 HIV patients,blood samples	in vivo	http://www.drugbank.ca/drugs/DB00109	None	Not mentioned
3091	19023544	2008	SDAAVDTSSEITTKDLKEKKEVVEEAENRKDVY	TÎ±1-TP5 (Thymosin Î±1-thymopentin)	33	Acetylation	Free	Linear	L	None	Synthetic	Immunoregulatory	Not mentioned	Not mentioned	140 ±14	Rabbit plasma proteases	HPLC	Heparinized rabbit plasma	in vitro	http://www.drugbank.ca/drugs/DB00110	None	IL2 concentration in mouse serum:0.75pg/ml,macrophage clearance index(K value)=0.0206 ±0.0010,phagocytic index(Î± value=3.95 ±0.19(compared to TP5).
3092	19023544	2008	SDAAVDTSSEITTKDLKEKKEVVEEAEN	TÎ±1 (Thymosin Î±1)	28	Acetylation	Free	Linear	L	None	Component of thymosin fraction	Immunomodulator	Not mentioned	Not mentioned	127 ±11	Rabbit plasma proteases	HPLC	Heparinized rabbit plasma	in vitro	http://www.drugbank.ca/drugs/DB00111	None	IL2 concentration in mouse serum:0.7pg/ml,macrophage clearance index(K value)=0.0165 ±0.0007,phagocytic index(Î± value=3.73 ±0.56.
3096	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	GLP-1 (glucagon like peptide-1)	30	Free	Free	Linear	L	None	Incretin released by intestinal L cells	Glucose dependent insulin secretion,promotion of insulin gene transcription,stimulation of Î²-cell proliferation and neogenesis, inhibition of Î²-cell apoptosis, and suppression of glucagon secretion.	24 hours	100Î¼M	2.0 ±0.2	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00115	None	EC50=4.6nM,pEC50=8.3 ±0.08
3097	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E16,K20]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16 and K20)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	1.8 ±0.3	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00116	None	EC50=3.8nM,pEC50=8.4 ±0.06
3098	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E18,K22]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E18 and K22)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	2.1 ±0.4	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00117	None	EC50=0.6nM,pEC50=9.2 ±0.11
3099	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E22,K26]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E22 and K26)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	2.9 ±0.8	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00118	None	EC50=2.8nM,pEC50=8.3 ±0.03
3100	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E30 and K34)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	3.3 ±0.4	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00119	None	EC50=5.3nM,pEC50=8.6 ±0.13
3101	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E16,K20]-c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20 and E30-K34)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	3.1 ±0.1	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00120	None	EC50=3.3nM,pEC50=8.5 ±0.04
3102	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[K16,E20]-c[K30,E34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between K16-E20 and K30-E34)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	2.9 ±0.1	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00121	None	EC50=7.0nM,pEC50=8.2 ±0.11
3103	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E18,K22]-c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E18-K22 and E30-K34)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	3.6 ±0.2	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00122	None	EC50=1.9nM,pEC50=8.7 ±0.14
3104	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[K18,E22]-c[K30,E34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between K18-E22 and K30-E34)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	4.1 ±0.2	Dipeptidyl peptidase-IV	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00123	None	EC50=1.0nM,pEC50=9.0 ±0.09
3108	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E16,K20]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K35)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	4.6 ±0.7	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00127	None	EC50=3.8nM,pEC50=8.4 ±0.06
3109	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E18,K22]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K36)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	3.2 ±0.4	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00128	None	EC50=0.6nM,pEC50=9.2 ±0.11
3113	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[K16,E20]-c[K30,E34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K40)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	1.7 ±5.0	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00132	None	EC50=7.0nM,pEC50=8.2 ±0.11
3116	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K43)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	3.5 ±0.9	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00135	None	EC50=1.6nM,pEC50=8.8 ±0.11
3117	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[K22,E26]-c[K30,E34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K44)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	1.2 ±0.3	Neutral endopeptidase 24.11	HPLC	GLP-1 analogue (100 Î¼M) was incubated with the recombinant human NEP 24.11 enzyme (1.0 Î¼g/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C	in vitro	http://www.drugbank.ca/drugs/DB00136	None	EC50=2.2nM,pEC50=8.7 ±0.14
3129	22770564	2012	CEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLW	N-terminus-PEG2000 of HR2	42	Pegylation-PEG2000	Free	Linear	L	None	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	79.3	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00148	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=11.2 ± 1.9nM
3132	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW	R4C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at 4th position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	67.4	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00151	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=8.7 ± 1.3nM
3135	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW	S11C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at 11th position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	91	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00154	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.9 ± 0.5nM
3138	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW	S15C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at 15th position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	82.4	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00157	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.0 ± 0.5nM
3141	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW	E18C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at 18th position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	81.3	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00160	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.9 ± 0.6nM
3144	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW	N22C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at22nd position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	80.7	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00163	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.1 ± 0.5nM
3147	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW	Q29C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at 29th position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	84.1	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00166	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.5 ± 0.5nM
3149	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWC	C terminus-PEG750 derivative of HR2	42	Free	Free	Linear	L	None	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	81.2	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00168	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=10.9 ± 2.2nM
3150	22770564	2012	EWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWC	C terminus-PEG2000 derivative of HR2	42	Free	Pegylation (PEG750)	Linear	L	None	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	126	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00169	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=43.3 ± 14.8nM
3153	22770564	2012	EWDREINNYTSLIHSLIEECQNQQEKNEQELLELDKWASLW	S20C-PEG2000 derivative of HR2	41	Free	Free	Linear	L	Pegylation-PEG2000 of cysteine at 20th position	Modified HR2 wild type peptide	Inhibitor to prevent virus ˆ’host cell membrane fusion	Not mentioned	20Î¼M	76.3	Bovine Trypsin	Trypsin degradation assay, Analytical reverse phase HPLC	Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)	in vitro	http://www.drugbank.ca/drugs/DB00172	None	Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)>401
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
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
3159	23099431	2012	HwAWfK	GHRP-6 (Growth Hormone-Releasing Peptide-6)	11	Free	Amidation	Linear	Mix	None	Synthetic molecule structurally related to Met-enkephalin	Cytoprotective,antioxidant in nature	Not mentioned	400 Î¼g/kg of the body weight	1.15 ±0.17(t1/2Î²)	human plasma proteases	LC-MS	Intravenous bolus administartion in 9 healthy male subjects	in vivo	http://www.drugbank.ca/drugs/DB00178	None	Not mentioned
3162	23696181	2013	VDCFLSRPTEKT	Cx43MP (Connexin43 mimetic peptides)	12	Free	Free	Linear	L	None	Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43	Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia	Aliquots were collected at 0, 5, 30, 60, 120, and 240 min	500Î¼M	145.57 ±14.57	Bovine vitreous proteases	RP-HPLC	500 Î¼L of freshly collected bovine vitreous	in vitro	http://www.drugbank.ca/drugs/DB00181	None	Cell viability of NT2/ D1 cells at 100Î¼M of peptide= 90% approx. after 48 hours
3191	19422857	2009	FNAPFDVGIKLSGAQYQQHGRAL	Mouse Obestatin	23	Free	Amidation	Linear	L	None	Proghrelin from mouse	Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion	37 °C for 0 - 120 minutes	90 Î¼g	75.5	Proteases from Membrane brain Homogenate	HPLC	Membrane brain Homogenate + P8340 protease inhibitor cocktail	in vitro	http://www.sigmaaldrich.com/catalog/product/sigma/	None	No suppressive effects of obestatin on food or water intake were observed
3192	19422857	2009	FNAPFDVGIKLSGAQYQQHGRAL	Mouse Obestatin	23	Free	Amidation	Linear	L	None	Proghrelin from mouse	Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion	37 °C for 0 - 120 minutes	90 Î¼g	62	Proteases from Membrane brain Homogenate	HPLC	Membrane brain Homogenate + EDTA	in vitro	http://www.sigmaaldrich.com/catalog/product/sigma/	None	No suppressive effects of obestatin on food or water intake were observed
3201	18602197	2008	FNAPFDVGIKLSGAQYQQHGRAL	Mouse Obestatin	23	Free	Amidation	Linear	L	None	Proghrelin from mouse	Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion	37 °C for 0 - 60 minutes, pH 7.7	90 Î¼g	138.0 [114.8, 172.9]	Proteases from Mouse kidney membrane homogenate	HPLC, LC-UV/MS	Mouse kidney membrane homogenate	in vitro	http://www.sigmaaldrich.com/catalog/product/sigma/	None	Not reported
3202	18602197	2008	FNAPFDVGIKLSGVQYQQHSQAL	Human Obestatin	23	Free	Amidation	Linear	L	None	Proghrelin frpm human	Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion	37 °C for 0 - 60 minutes, pH 7.8	90 Î¼g	65.1 [59.6, 71.7]	Proteases from mouse plasma	HPLC, LC-UV/MS	Mouse plasma	in vitro	http://www.sigmaaldrich.com/catalog/product/sigma/	None	Not reported
3203	18602197	2008	FNAPFDVGIKLSGVQYQQHSQAL	Human Obestatin	23	Free	Amidation	Linear	L	None	Proghrelin frpm human	Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion	37 °C for 0 - 60 minutes, pH 7.9	90 Î¼g	95.8 [89.4, 103.3]	Proteases from mouse plasma + protease inhibitor cocktai	HPLC, LC-UV/MS	Mouse plasma with protease inhibitor cocktail	in vitro	http://www.sigmaaldrich.com/catalog/product/sigma/	None	Not reported
3206	18602197	2008	FNAPFDVGIKLSGVQYQQHSQAL	Human Obestatin	23	Free	Amidation	Linear	L	None	Proghrelin frpm human	Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion	37 °C for 0 - 60 minutes, pH 7.12	90 Î¼g	67.7 [61.7, 75.1]	Proteases from mouse membrane homogenate	HPLC, LC-UV/MS	Mouse kidney membrane homogenate	in vitro	http://www.sigmaaldrich.com/catalog/product/sigma/	None	Not reported
4008	38789061	2024	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Exendin-4 analogs	Antidiabetes	Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr	1 mg/kg	1.03 ± 0.10	Male SD rats plasma protease	UHPLC	Male SD rats plasma	In Vivo	PDB id: 7MLL	None	N.A.
4032	38613996	2024	WRRRYRRWRRRRRWRRRPRR	vCPP2319	20	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	280.40 ± 59.20	Human serum protease	RP-HPLC	Human serum	In Vitro	None	None	IC50 = 4.00±1.03 for TNBC MDA-MB-231 Monolayer
4033	38613996	2024	AGILKRW-Ahx-WRRRYRRWRRRRRQRRRPRR	PepH3-vCPP2319 5	27	Free	Amidation	Linear	L	Ahx links two peptide	Synthetic chimeric peptide of PepH3 and vCPP2319	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	125.20 ± 34.21	Human serum protease	RP-HPLC	Human serum	In Vitro	None	None	IC50 = 5.20±1.04 for TNBC MDA-MB-231 Monolayer
4036	38601038	2024	YSEGTFTSDKSKYLDSQAAQDFVQWLLAGGPSSGAPPPS	DR10627	39	Free	Amidation	Linear	L	A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position	GLP-1 analogs	Antiobesity, Antidiabetes	Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration	26 nmol/kg	4.19 ± 0.957	Cynomolgus monkeys serum protease	LC-MS/MS	Cynomolgus monkeys serum	In Vivo	None	None	The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action
4037	38555444	2024	CGSNKGAIIGLM	Aβ11/T80@CSs-TGC	12	Free	Linked with Chol using PEG2k linker	Linear	L	None	Synthetic	Treating intracranial infections caused by multidrug resistant Acinetobacter Baumannii	Blood samples were collected at predetermined time points (0.25, 0.5, 1, 2, 4, 6, and 8 h),	12.5 mg/kg	1.26 ± 0.21	SD rats plasma protease	HPLC	SD rats plasma	In Vivo	None	None	Both free TGC and Aβ11/T80@CSs-TGC displayed potent antimicrobial activity with a minimum inhibitory concentration of 2 μg/mL
4052	38340726	2024	IEEQAKTFLDKFNHEAEDLFYQSSLGGSKGDFRGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSDVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQ	A1L35HR2m	114	Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker,	Free	Linear	L	None	fusion protein of A1 and HR2m	Antiviral (Inhibits Coronaviruses)	Sera were collected from these mice before (0 h) and 2, 4, 8, 12, 24, 48, 72, 120, 168, 240 and 336 h after injection	5 mg/kg	2.64	Balb/c mice serum protease	N.A.	BALB/c mice serum	In Vivo	None	None	A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM
4063	37818589	2024	RCLPAGKPCAGVTQKIPCCGKCSRNKCT	ΔTRTX-Ac1	28	Free	Free	Cyclic (C2-C9-C18-C19-C22-C27 form LCK Loop)	L	None	From venom of the Mexican Blond tarantula spider Aphonopelma chalcodes	Antidiabetes	Blood withdrawn by cardiac puncture at0, 2, 4, 6, 8 and 12 h post-administration	10 mg/kg	2.17	C57Bl/6 Male Mice Plasma Protease	Mass spectrometry	C57BL/6 male mice plasma	In Vivo	https://dom-pubs.pericles-prod.literatumonline.com/doi/10.1111/dom.15319	None	The activity value of ΔTRTX-Ac1 alone shows minimal influence on reducing circulating glucose levels, with glucose levels remaining at 23.7 ± 3.1 mmol/L in high-fat-fed/streptozotocin (HFF/STZ) mice
4064	37818589	2024	RCLPAGKPCAGVTQKIPCCGKCSRNKCT	ΔTRTX-Ac1	28	Free	Free	Cyclic (C2-C9-C18-C19-C22-C27 form LCK Loop)	L	None	From venom of the Mexican Blond tarantula spider Aphonopelma chalcodes	Antidiabetes	Blood withdrawn by cardiac puncture at 0, 2, 4, 6, 8 and 12 h post-administration	10 mg/kg	2.16	C57Bl/6 Male Mice Pancreas Protease	Mass spectrometry	C57BL/6 male mice pancreas	In Vivo	https://dom-pubs.pericles-prod.literatumonline.com/doi/10.1111/dom.15319	None	The activity value of ΔTRTX-Ac1 alone shows minimal influence on reducing circulating glucose levels, with glucose levels remaining at 23.7 ± 3.1 mmol/L in high-fat-fed/streptozotocin (HFF/STZ) mice
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.
4170	38092894	2023	MPRPRLLAALCGALLCAPSLLVALDICSKNPCHNGGLCEEISQEVRGDVFPSYTCTCLKGYAGNHCETKCVEPLGLENGNIANSQIAASSVRVTFLGLQHWVPELARLNRAGMVNAWTPSSNDDNPWIQVNLLRRMWVTGVVTQGASRLASHEYLKAFKVAYSLNGHEFDFIHDVNKKHKEFVGNWNKNAVHVNLFETPVEAQYVRLYPTSCHTACTLRFELLGCELNGCANPLGLKNNSIPDKQITASSSYKTWGLHLFSWNPSYARLDKQGNFNAWVAGSYGNDQWLQVDLGSSKEVTGIITQGARNFGSVQFVASYKVAYSNDSANWTEYQDPRTGSSKIFPGNWDNHSHKKNLFETPILARYVRILPVAWHNRIALRLELLGC	Tag-free rhMFG-E8	387	23 amino acid leader sequence of cystatin S introduced at N terminal	Free	Linear	L	None	Expressed in Expi293F cells	Antiinflammatory (Including Radiation Injury)	Blood samples (100 μl per time point) were collected starting from 2 to 6 hours	50 µg	1.45 (Terminal Elimination Half Life)	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The tag-free rhMFG-E8 demonstrated markedly higher cell adhesion binding activity (to SVEC4-10 cells) compared to E. coli-expressed His-tagged rhMFG-E8, which binds to αVβ3 integrin on the membrane of phagocytes
4171	38092894	2023	MPRPRLLAALCGALLCAPSLLVALDICSKNPCHNGGLCEEISQEVRGDVFPSYTCTCLKGYAGNHCETKCVEPLGLENGNIANSQIAASSVRVTFLGLQHWVPELARLNRAGMVNAWTPSSNDDNPWIQVNLLRRMWVTGVVTQGASRLASHEYLKAFKVAYSLNGHEFDFIHDVNKKHKEFVGNWNKNAVHVNLFETPVEAQYVRLYPTSCHTACTLRFELLGCELNGCANPLGLKNNSIPDKQITASSSYKTWGLHLFSWNPSYARLDKQGNFNAWVAGSYGNDQWLQVDLGSSKEVTGIITQGARNFGSVQFVASYKVAYSNDSANWTEYQDPRTGSSKIFPGNWDNHSHKKNLFETPILARYVRILPVAWHNRIALRLELLGC	Tag-free rhMFG-E8	387	23 amino acid leader sequence of cystatin S introduced at N terminal	Free	Linear	L	None	Expressed in Expi293F cells	Antiinflammatory (Including Radiation Injury)	Blood samples (100 μl per time point) were collected starting from 2 to 12 hours	50 µg	2.33 (Terminal Elimination Half Life)	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The tag-free rhMFG-E8 demonstrated markedly higher cell adhesion binding activity (to SVEC4-10 cells) compared to E. coli-expressed His-tagged rhMFG-E8, which binds to αVβ3 integrin on the membrane of phagocytes
4172	38027063	2023	QVTLKESGPGILQPSQTLSLTCSFSGFSLNTFGMGVSWIRQPSGKGLEWLAHIFWDDDKHYNPSLKSRLTISKDTSNNQVFLKITTVDTADTATYYCVRYGFDGFPYWGQGTGGGGSGGGGSGGGGSDVVMTQTPLSLPVSLGDQASISCRSNQSLVHSNGNTYLHWYLQKPGQSPKLLIYKVSNRFSGVPDRPSGSGSGTDFTLKISRVEAEDLGFYFCSQSTRVPWTFGGGTKLEIKR -METDTLLLWVLLLWVPGSTGDEFMGYQGPPGPPGPPGIPGNHGNNGNNGATGHEGAKGEKGDKGDLGPRGERGQHGPKGEKGYPGIPGYCGPPGPPGPPGIPGNHGNNGNNGATGHEGAKGEKGDKGDLGPRGERGQHGPKGEKGYPGIPDYKDDDDKLQGGRHHHHHH	ScFv9-CD	466	Free	Fusion of CD	Linear	L	Biotinylation	CD sequence originates from the C1qTNF3 protein and scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ)	Treatment of AD and Parkinson disease	Plasma was collected at 0, 2, 4, 8, and 24 h after injection	250 μg	1.82	TgCRND8 mice plasma protease	Direct ELISA	TgCRND8 mice plasma	In Vivo	None	None	N.A.
4174	37880318	2023	VAIALKAAHYHTHKE	L1	15	Acetylation	Free	Linear	L	None	Derived from calcitermin	Antimicrobial	37 °C	0.0001 M	>2	Human plasma protease	HPLC	Human plasma with 1 ml of ammonium acetate buffer (pH 7.4)	In Vitro	None	None	CFU = 40 ± 10 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation)
4175	37880318	2023	VAIALKAAHYHTHKE	L2	15	Acetylation	Amidation	Linear	L	None	Derived from calcitermin	Antimicrobial	37 °C	0.0001 M	68	Human plasma protease	HPLC	Human plasma with 1 ml of ammonium acetate buffer (pH 7.4)	In Vitro	None	None	CFU = 211 ± 25 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation)
4183	37835489	2023	QQTNWSLGGGSC	QQT*-IRDye800	12	QQT* conjugated with IRDye800 at C terminus using linker	Free	Linear	L	None	Synthetic	Used for in vivo imaging to identify premalignant Colorectal Lesions	RP-HPLC was performed at 0, 0.5, 1, 2, 4, 8, and 24 h	30 μM	3.6	APC mice serum protease	RP-HPLC	APC mice serum	In Vivo	None	None	Not mentioned
4194	37373203	2023	LRKLRKRLLRLVGRQLEEFL	HM-10/10	20	Free	Free	Linear	L	None	Chimeric high-density lipoprotein mimetic peptide	Anticancer	Timepoints of 0, 10, 20, 30, 60, and 120 min	2 μM	164	Human plasma protease	Triple Quadrupole Mass spectrometry	Human plasma	In Vitro	None	None	Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4195	37373203	2023	LRKLRKRLLRLVGRQLEEFL	HM-10/10	20	Free	Free	Linear	L	None	Chimeric high-density lipoprotein mimetic peptide	Anticancer	Timepoints of 0, 10, 20, 30, 60, and 120 min	2 μM	82.5	SD rats plasma protease	Triple Quadrupole Mass spectrometry	SD rats plasma	In Vitro	None	None	Not mentioned
4201	37373203	2023	LRKLRKRLLRLVGRQLEEFL	HM-10/10	20	Free	Free	Linear	L	None	Chimeric high-density lipoprotein mimetic peptide	Anticancer	120 minutes	2 μM	>120	N.A.	Triple Quadrupole Mass spectrometry	potassium phosphate buffers of pH 1.3 (acidic)	In Vitro	None	None	Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4202	37373203	2023	LRKLRKRLLRLVGRQLEEFL	HM-10/10	20	Free	Free	Linear	L	None	Chimeric high-density lipoprotein mimetic peptide	Anticancer	120 minutes	2 μM	>120	N.A.	Triple Quadrupole Mass spectrometry	potassium phosphate buffers of pH 5.5 (slightly acidic)	In Vitro	None	None	Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086)
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
4254	36631971	2023	LVPRVDKPPYLPRPRPPROIYNO	5k-prodrug	23	Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs	Amidation, Orn at position 23	Linear	L	Orn at postion 19	Oncocins	Antimicrobial	Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration	4.34 mmol/kg	66	CD-1 mice plasma protease	cELISA	CD-1 mice plasma	In Vivo	None	None	(Prodrugs of Onc72) MIC values >50 μmol L−1 on E.coli BW25113
4255	36631971	2023	LVPRVDKPPYLPRPRPPROIYNO	5k-prodrug	23	Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs	Amidation, Orn at position 23	Linear	L	Orn at postion 19	Oncocins	Antimicrobial	Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration	4.34 mmol/kg	66	CD-1 mice plasma protease	cELISA	CD-1 mice plasma	In Vivo	None	None	Prodrugs Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS)
4256	36631971	2023	LVPRVDKPPYLPRPRPPROIYNO	5k-prodrug	23	Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs	Amidation, Orn at position 23	Linear	L	Orn at postion 19	Oncocins	Antimicrobial	Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration	4.34 mmol/kg	66	CD-1 mice plasma protease	cELISA	CD-1 mice plasma	In Vivo	None	None	5 kDa thiol-PEG: Reduced cell viability to ≈89% for both HepG2 and HEK293 cell lines
4260	36631971	2023	VDKPPYLPRPRPPROIYNO	Onc72	19	Free	Amidation, Orn=Ornithine at position 19	Linear	L	Orn=Ornithine at position 15	Synthetic	Antimicrobial	Aliquots weretaken in triplicates after 0, 1, 2, 4, and 8 h for Onc72 and 0, 4, 8, and 24 hfor both prodrugs	31.5 μmol/L	≈80	Cell lysate protease (Obtained From An E. Coli Bw25113 Culture)	RP-HPLC	E. coli BW25113 cell lysate	In Vitro	None	None	(Onc72 in 19% MHB2 medium) MIC = 12.5 μmol L−1 (29 mg L−1) on E.coli BW25113
4263	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	Fluorescently labeled	Isolated from the saliva of the Gila monster lizard (Heloderma suspectum)	Antidiabetes	Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h	1000 nmol kg−1	2.12 ± 0.3 (T1/2 Elimination)	Naïve mice plasma protease	Fluorescence assay	Naïve mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.04 ± 0.01 nM for exendin
4267	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	Fluorescently labeled	Isolated from the saliva of the Gila monster lizard (Heloderma suspectum)	Antidiabetes	Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h	1000 nmol kg−1	1.88 ± 0.2(T1/2 Elimination)	Naïve mice plasma protease	Fluorescence assay	Naïve mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.04 ± 0.01 nM for exendin
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
4275	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin	39	Fluorescently labelled	Amidation	Linear	L	None	Derived from Gila monster	Antidiabetes	Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h.	1000 nmol/kg	2.12 ± 0.3 (T1/2 Elimination)	Naïve mice plasma protease	fluorescence assay	Naïve mice plasma	In Vivo	PDB id: 7MLL	None	EC50 (nM) = 0.04 ± 0.01
4279	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin	39	Fluorescently labelled	Amidation	Linear	L	None	Derived from Gila monster	Antidiabetes	Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h.	1000 nmol/kg	1.88 ± 0.2 (T1/2 Elimination)	Immunized mice plasma protease	fluorescence assay	Immunized mice plasma	In Vivo	PDB id: 7MLL	None	EC50 (nM) = 0.04 ± 0.01
4384	36997003	2023	HsQGTFTSDLSKQKDSRRAQDFIEWLKNGGPSSGAPPPS	Compound 14	40	Free	Amidation	Linear	Mix	D-Ser2 substiuition, Lys14 side chain linked to C16 fatty acid via linker yE-C16	GLP-1 analogs	Dual GLP-1/Glucagon receptor agonist	The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application	1 mg/kg	3.2	C57/B16 female mice plasma protease	LC−MS/MS	C57/B16 female mice plasma	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	GLP-1 receptor : EC50 = 3.9 pM
4385	36997003	2023	HsQGTFTSDLSKQMDSRRAQDFIEWLKNGGPSSGAPPPSK	Compound 15	41	Free	Terminal Lys side chain linked to C16 fatty acid via linker yE-C16 at C terminal	Linear	Mix	D-Ser2 substiuition	GLP-1 analogs	Dual GLP-1/Glucagon receptor agonist	The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application	1 mg/kg	2.2	C57/B16 female mice plasma protease	LC−MS/MS	C57/B16 female mice plasma	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	GLP-1 receptor : EC50 = 5.2 pM
4386	36997003	2023	HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Liraglutide	32	Free	Free	Linear	L	Lys20 side chain linked to C16 fatty acid via linker yE-C16	GLP-1 analogs	Dual GLP-1/Glucagon receptor agonist	The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application	1 mg/kg	3.6	C57/B16 female mice plasma protease	LC−MS/MS	C57/B16 female mice plasma	In Vivo	https://www.nature.com/articles/s41598-022-21251-y	None	GLP-1 receptor : EC50 = 6.4 pM
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.
4435	36443381	2022	LEGREKVRAKI-Aib-Aib-EG-Nle-STWS-Aib-RKKK	SA10SC-RLX	25	Acetylation	Amidation	Linear	L	Attachment of a lipid moiety (C18-γ-Glu-PEG2) at K25 position, Aib, Nle,acetylation of Lys10	Synthetic	Treatment for Chronic Fibrotic and Cardiovascular Diseases	Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48 and 72 h (IV route) and 0.25, 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h (SC route)	1 mg/kg	4 (Terminal Half Life)	Rats plasma protease	LC-HRMS	Rats plasma	In Vivo	None	None	EC50 (nM) = 0.8 for EA.hy926_hRXFP1
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
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
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
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.
4460	36380917	2022	HAEGTFTSNVSSYLEGQAAKEFIAWLVKGRG	Glc-GLP-1-1	31	Free	Free	Linear	L	Glucosylation at Asn15	GLP-1 analogs	Antidiabetes	37 °C	6 nmol	94.1 ± 7.6	Mouse serum protease	RP-HPLC	Mouse serum	In Vitro	None	None	N.A.
4462	36380917	2022	HAEGTFTSDVSSYLEGQAANESIAWLVKGRG	Glc-GLP-1-3	31	Free	Free	Linear	L	Glucosylation at Asn26	GLP-1 analogs	Antidiabetes	37 °C	6 nmol	138.8 ± 14.5	Mouse serum protease	RP-HPLC	Mouse serum	In Vitro	None	None	N.A.
4464	36380917	2022	HAEGTFTSDVSSYLEGQAAKEFIAWLVNGTG	Glc-GLP-1-5	31	Free	Free	Linear	L	Glucosylation at Asn34	GLP-1 analogs	Antidiabetes	37 °C	6 nmol	113.3 ± 11.8	Mouse serum protease	RP-HPLC	Mouse serum	In Vitro	None	None	N.A.
4467	36380917	2022	HAEGTFTSNVSSYLEGQAAKEFIAWLVKGRG	Glycan-GLP-1-1(G2S2)	31	Free	Free	Linear	L	N-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan)	GLP-1 analogs	Antidiabetes	37 °C	0.3 nmol	145.7 ± 4.3	DPP-IV	RP-HPLC	50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV	In Vitro	None	None	BGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability)
4469	36380917	2022	HAEGTFTSDVSSYLEGQAANESIAWLVKGRG	Glycan-GLP-1-3(G2)	31	Free	Free	Linear	L	N-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan)	GLP-1 analogs	Antidiabetes	37 °C	0.3 nmol	185.3 ± 1.1	DPP-IV	RP-HPLC	50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV	In Vitro	None	None	BGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability)
4473	36380917	2022	HAEGTFTSDVSSYLEGQAAKEFIAWLVNGTG	Glycan-GLP-1-5(G2)	31	Free	Free	Linear	L	N-glycosylation with biantennary complex-type N-glycan at Asn34 (G2 glycoform = glycan)	GLP-1 analogs	Antidiabetes	37 °C	0.3 nmol	182.0 ± 0.1	DPP-IV	RP-HPLC	50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV	In Vitro	None	None	BGLmax (mmol L−1) = 14.50 ± 1.62 (In vivo glucose stabilizing capability)
4475	36380917	2022	HAEGTFTSDVSSYLEGQAAKEFIAWLVNGTG	Glycan-GLP-1-5(G2S2)	31	Free	Free	Linear	L	N-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan)	GLP-1 analogs	Antidiabetes	37 °C	0.3 nmol	245.3 ± 1.3	DPP-IV	RP-HPLC	50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV	In Vitro	None	None	BGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability)
4478	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDKKKKKK	Glepaglutide parent	39	Free	Six lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	5 mg	3.8	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.12 nM In vitro potency
4482	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDKKKKKK	Glepaglutide parent	39	Free	Six lysines has been added at C terminal , Amidation	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose)	10 mg	2.8	Human plasma protease	LC-MS	Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses	In Vivo	None	None	EC50 = 0.12 nM In vitro potency
4488	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDKK	Glepaglutide M1	35	Free	Two lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22	1 mg	1.2	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	EC50 = 0.068 nM In vitro potency
4489	36323988	2022	HGEGTFSSELATILDALAARDFIAWLIATKITDK	Glepaglutide M2	34	Free	1 lysines has been added at C terminal	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22	1 mg	2.6	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	EC50 = 0.044 nM In vitro potency
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
4496	36142749	2022	Dmt-kFFKKPFIL	[Ile9]PK20	10	Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1	Free	Linear	Mix	D-amino acid residue (D-Lys) inserted at position 2	PK20 derivative	Analgesic	37°C for 24 h	50 μg/mL	4.69	N.A.	LC-MS	1M NaOH	In Vitro	None	None	EC50 = 1244 nM (potency at mu opioid receptor)
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.
4505	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	N.A.	1.25 mg/kg	1.7	NHP plasma protease	LC-MS/MS	NHP plasma	In Vivo	None	None	KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP)
4509	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	2.3 - 4.4	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vitro	None	None	KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse)
4513	36112771	2022	CP-1Nal-dCM-HArg-DWSTP-HyP-WC	BT8009	16	Acetylation	Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10	Bicyclic	Mix	cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification	BT8009 and MMAE cytotoxin hybrid	Anticancer	24 hours	2 µM	5	Mouse blood protease	LC-MS/MS	Mouse blood sample	In Vitro	None	None	KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse)
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.
4524	36034808	2022	MGHPPLLPLLLLLHTCVPASWGLRCMQCKTNGDCRVEECALGQDLCRTTIVRLWEEGEELELVEKSCTHSEKTNRTLSYRTGLKITSLTEVVCGLDLCNQGNSGRAVTYSRSRYLECISCGSSDMSCERGRHQSLQCRSPEEQCLDVVTHWIQEGEEGRPKDDRHLRGCGYLPGCPGSNGFHNNDTFHFLKCCNTTKCNEGPILELENLPQNGRQCYSCKGNSTHGCSSEETFLIDCRGPMNQCLVATGTHEPKNQSYMVRGCATASMCQHAHLGDAFSMNHIDVSCCTKSGCNHPDLDVQYRSGAAPQPGPAHLSLTITLLMTARLWGGTLLWT	uPAR	335	Free	Free	Linear	L	None	Derived from PLAUR gene	Plays role in thrombosis	N.A.	N.A.	209.6 ± 0.2	BEAS-2B cells lysate protease	Densitometry analysis using NIH Image J	BEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + Cycloheximide	In Vivo	None	None	N.A.
4541	35971165	2022	YLCSSNNNRERDKFRRGGSGGTSFEQFWAWLWP	AR pep‐PROTAC	33	Free	Free	Linear	L	None	Synthetic	Anticancer (Prostate Cancer Therapy)	N.A.	N.A.	1.9	PBS containing 10% serum protease	HPLC	PBS containing 10% serum	In Vitro	None	None	IC50 of Au‐AR pep‐PROTAC on AML 12 cells is 2.41 µM
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.
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.
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
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
4595	35677307	2022	MTPLGPASSLPQSFLLKCLEQVRKIQADGAALLANQVRQVGDGAALQEKLVSELGNALENALPDTLDTLQLDVKDYFSLRAALLAALPTRLRYLQEADAFQRRAGGVLVASHLGTSLQRLALADSGVLRQLLYYIESGPHQAPLGTGGADQGAMNVTCSKELQAYREQILHDCWLPKDLKDLQLLIEMNVTVLVDIDKLVEVLRLRQGVLHGVHVC	rhG-CSF	175	Free	Free	Linear	L	None	Recombinant human methionyl-granulocyte colonystimulating factor	N.A.	Sampling time - 0, 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h	1.0 mg/kg	2.74 ± 0.33	Mice Serum Protease	ELISA	Mice serum	In Vivo	None	None	N.A.
4604	35653695	2022	GCTRQYPCGKG	KLK5 inhibitor	11	Free	A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2	Cyclic (C2-C8 Disulfide Bond)	L	None	Synthetic	Treatment for Netherton syndrome	N.A.	6.2 mg/kg	4.4 ± 0.3 (Terminal Half Life)	Mice plasma protease	HPLC analysis with fluorescence detection	Mice plasma	In Vivo	None	None	Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag)
4609	35646543	2022	HsQGTFTSDYSKYLDKRRAQDFVQWLLNTGGPSSGAPPPS	TB001	40	Free	Amidation, GGPSSGAPPPS introduced in the C-terminal	Cyclic (R17-D21 Lactam Bridge)	Mix	D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3)	GLP-1 and GCG chimera analog	Treatment of Multiple Causes of Hepatic Fibrosis	N.A.	5 μg/kg	3.33 ± 1.57	Rhesus monkeys plasma protease	HPLC–MS/MS	Rhesus monkeys plasma	In Vivo	None	None	GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04
4610	35646543	2022	HsQGTFTSDYSKYLDKRRAQDFVQWLLNTGGPSSGAPPPS	TB001	40	Free	Amidation, GGPSSGAPPPS introduced in the C-terminal	Cyclic (R17-D21 Lactam Bridge)	Mix	D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3)	GLP-1 and GCG chimera analog	Treatment of Multiple Causes of Hepatic Fibrosis	N.A.	20 μg/kg	2.83 ± 1.42	Rhesus monkeys plasma protease	HPLC–MS/MS	Rhesus monkeys plasma	In Vivo	None	None	GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04
4611	35646543	2022	HsQGTFTSDYSKYLDKRRAQDFVQWLLNTGGPSSGAPPPS	TB001	40	Free	Amidation, GGPSSGAPPPS introduced in the C-terminal	Cyclic (R17-D21 Lactam Bridge)	Mix	D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3)	GLP-1 and GCG chimera analog	Treatment of Multiple Causes of Hepatic Fibrosis	N.A.	60 μg/kg	2.47 ± 0.571	Rhesus monkeys plasma protease	HPLC–MS/MS	Rhesus monkeys plasma	In Vivo	None	None	GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04
4612	35646543	2022	HsQGTFTSDYSKYLDKRRAQDFVQWLLNTGGPSSGAPPPS	TB001	40	Free	Amidation, GGPSSGAPPPS introduced in the C-terminal	Cyclic (R17-D21 Lactam Bridge)	Mix	D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3)	GLP-1 and GCG chimera analog	Treatment of Multiple Causes of Hepatic Fibrosis	1 day	20 μg/kg	3.07 ± 1.28	Rhesus monkeys plasma protease	HPLC–MS/MS	Rhesus monkeys plasma	In Vivo	None	None	GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04
4613	35646543	2022	HsQGTFTSDYSKYLDKRRAQDFVQWLLNTGGPSSGAPPPS	TB001	40	Free	Amidation, GGPSSGAPPPS introduced in the C-terminal	Cyclic (R17-D21 Lactam Bridge)	Mix	D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3)	GLP-1 and GCG chimera analog	Treatment of Multiple Causes of Hepatic Fibrosis	7 days	20 μg/kg	1.94 ± 0.305	Rhesus monkeys plasma protease	HPLC–MS/MS	Rhesus monkeys plasma	In Vivo	None	None	GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04
4616	35458385	2022	SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKEL	EK1	36	Free	Free	Linear	L	None	Expression in E. coli	Pan-cov fusion inhibitor	Serum samples were collected before (0 h) and after injection of EK1 (0.5 h, 1 h, 3 h, 7 h, and 12 h) or FL-EK1 (0.5 h, 1 h, 3 h, 7 h, 24 h, 48 h, 72 h, and 96 h)	8.25 mg/kg	1.8 ± 1.0	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	None	None	IC50(nM) = 69.0 ± 20.8 against B.1.1.7 (Alpha), IC50(nM) = 109.9 ± 25.3 against B.1.351 (Beta), IC50(nM) = 191.3 ± 17.0 against P.1 (Gamma), IC50(nM) = 190.6 ± 29.0 against B.1.617.2 (Delta), IC50(nM) = 135.6 ± 11.2 against B.1.525 (Eta), IC50(nM) = 107.1 ± 7.3 against B.1.617.1 (Kappa), IC50(nM) = 68.7 ± 25.4 against C.37 (Lambda), IC50(nM) = 236.8 ± 10.6 against B.1.1.529 (Omicron)
4619	35455421	2022	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	T20 (enfuvirtide)	36	Free	Free	Linear	L	None	Derived from the natural sequence (aa 643–678) of the HIV-1 gp41 C-terminal heptad repeat (CHR) domain	Antiviral (HIV fusion inhibitor)	Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested	1.26 mg/kg	1.22 ± 0.2	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	None	None	IC50(nM)= 55.3 ± 2.4 against HIV-1 96USSN20 (X4/R5, A),IC50(nM) = 49.3 ± 4.9 against HIV-1 96USNG17 (X4, A), IC50(nM) = 50.1 ± 2.0 against HIV-1 90US_873 (R5, B), IC50(nM) =53.9 ± 4.3 against HIV-1 BZ167 (X4, B), IC50(nM) = 45.2 ± 3.2 against HIV-1 SE364 (R5, C), IC50(nM) = 46.9 ± 2.1 against HIV-1 PBL288 (R5, C), IC50(nM) = 77.1 ± 6.8 against HIV-1 92UG001 (X4/R5, D), IC50(nM) = 21.1 ± 1.1 against HIV-1 J32228M4 (R5, D), IC50(nM) = 55.6 ± 1.2 against HIV-1 DJ263 (R5, CRF02_AG), IC50(nM) = 61.2 ± 1.3 against HIV-1 CAM1475MV (R5, CRF02_AG) (infection on MT-4 cell)
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.
4623	35414877	2022	MSFQYFHILWPFSGSGSDYKDDDDK	B_3.2	25	Acetylation	Amidation, FLAG tag	Linear	L	None	Synthetic	Targets GIP receptor	At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins	1 μM	~2	Human plasma protease	LC-MS	80% pooled human Li-heparin plasma	In Vitro	None	None	IC50(nM) = 7890
4624	35414877	2022	MCFTHFHMLWPFCGSGSDYKDDDDK	B_1275	25	Acetylation	Amidation, FLAG tag	Cyclic	L	None	Synthetic	Targets GIP receptor	At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins	1 μM	~3.5	Human plasma protease	LC-MS	80% pooled human Li-heparin plasma	In Vitro	None	None	IC50(nM) = 2076
4626	35414877	2022	MSFTHFHMLWPFSGSGSDYKDDDDK	B_1275.2	25	Acetylation	Amidation, FLAG tag	Linear	L	None	Synthetic	Targets GIP receptor	At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins	1 μM	~2	Human plasma protease	LC-MS	80% pooled human Li-heparin plasma	In Vitro	None	None	IC50(nM) = 8336
4635	35414877	2022	ACFTHFDLLWPFCGSGSDYKDDDDK	B_1275.4	25	Acetylation	Amidation, FLAG tag	Cyclic	L	None	Synthetic	Targets GIP receptor	N.A.	2 μM	3.767 (Elimination half life)	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	None	IC50(nM) = 826
4636	35414877	2022	ACFTHFDLLWPFC	B_1275.5	14	Acetylation	Free	Cyclic	L	None	Synthetic	Targets GIP receptor	N.A.	2 μM	2.367 (Elimination half life)	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	None	IC50(nM) = 2300
4637	35414877	2022	ACFTHFDLLWPFC	B_1275.6	14	C18 diacid-gGlu-2xOEG	Free	Cyclic	L	None	Synthetic	Targets GIP receptor	N.A.	2 μM	250 (Elimination Half Life)	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	None	IC50(nM) = 860
4640	35359494	2022	AMRLSK-Cha-FRDFILQRKK	CSP1-E1A/F7Cha	17	Free	Free	Linear	L	introduction of Cha = cyclohexylalanine residues at position 7,E1A substituitions	CSP1 analog	Modulates Quorum Sensing In Streptococcus Pneumoniae	Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points	1 mM	4	Trypsin	RP-HPLC	PBS solution	In Vitro	None	None	IC50(nM) = 36 for CSP1-E1A/F7Cha against ComD1 receptor
4641	35359494	2022	AMRLSK-Cha-FRDFILQRKK	CSP1-E1A/F7Cha	17	Free	Free	Linear	L	introduction of Cha = cyclohexylalanine residues at position 7	CSP1 analog	Modulates Quorum Sensing In Streptococcus Pneumoniae	Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points	1 mM	4	Chymotrypsin	RP-HPLC	PBS solution	In Vitro	None	None	IC50(nM) = 36 for CSP1-E1A/F7Cha against ComD1 receptor
4642	35359494	2022	EMRLSK-Cha-FRDF-Cha-LQRKK	CSP1-F7Cha/I12Cha	17	Free	Free	Linear	L	introduction of Cha residues at positions 7 and 12	CSP1 analog	Modulates Quorum Sensing In Streptococcus Pneumoniae	Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points	1 mM	3	Trypsin	RP-HPLC	PBS solution	In Vitro	None	None	EC50(nM) = 0.97 for CSP1-F7Cha/I12Cha against ComD1 receptor, EC50(nM) = 70 for CSP1-F7Cha/I12Cha against ComD2 receptor
4664	35046019	2022	MSKGPG-(VPGGGVPGAGVPGYG)10-PGGGG-SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	ELP(0FA)GFP	400	Free	GFP	Linear	L	None	ELP-GFP conjugate	Increases Half Life	1 week	10 μM	1.6	C57Bl/6J mice blood plasma protease	GFP-specific ELISA	C57BL/6J mice blood plasma	In Vivo	None	None	KD MSA - Mouse serum albumin (μM) = n.d. (Binding affinity of ELP-GFP constructs for serum albumin), KD HSA - Human serum albumin (μM) = n.d
4665	35046019	2022	MSKGPG-(VPGGGVPGAGVPG(pAzF-FA)G)1(VPGGGVPGAGVPGYG)9-PGGGG-SKGEELFTGVVPILVELDGDVNGHKFSVRGEGEGDATNGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKRHDFFKSAMPEGYVQERTISFKDDGTYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNFNSHNVYITADKQKNGIKANFKIRHNVEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSVLSKDPNEKRDHMVLLEFVTAAGITHGMDELYKGS	ELP(1FA)GFP	400	Free	GFP	Linear	L	1 Fatty acid conjugation through pAzF (para-azidophenylalanine)	ELP-GFP conjugate	Increases Half Life	1 week	10 μM	1.9	C57Bl/6J mice blood plasma protease	GFP-specific ELISA	C57BL/6J mice blood plasma	In Vivo	None	None	KD MSA (μM) = 126 ± 32.2, KD HSA - Human serum albumin (μM) = n.d
4700	34217775	2022	vFCODVGPFC-3Pal	FE 205030	10	Oxazole-2-carbonyl, D-val at position 1	Amidation	Cyclic (C3-C10 disulfide bond)	Mix	Phe linked with (2-Cbm),3Pal, Orn linked with iPr	Derived from CGRP	Treatment of Acute Episodic Migraine	Blood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min	0.1 mg/kg	82 ± 9	Male göttingen minipigs plasma protease	LC-MS/MS	Male göttingen minipigs plasma	In Vivo	None	None	Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4701	34217775	2022	vFCODVGPFC-3Pal	FE 205030	10	Oxazole-2-carbonyl, D-val at position 1	Amidation, 3-Pal modification at C terminal	Cyclic (C3-C10 disulfide bond)	Mix	Phe linked with (2-Cbm),3Pal, Orn linked with iPr	Derived from CGRP	Treatment of Acute Episodic Migraine	Blood sample was collected at 5, 10, 20, 40, 60, 90, 120, 180, 240, 300 min	0.25 mg/kg	264 ± 80	Male göttingen minipigs plasma protease	LC-MS/MS	Male göttingen minipigs plasma	In Vivo	None	None	Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4702	34217775	2022	vYC-Agp-DVGPFC-3Pal	FE 992325	10	D-val at position 1	Amidation, 3-Pal modification at C terminal	Cyclic (C3-C10 disulfide bond)	Mix	Agp	Derived from CGRP	Treatment of Acute Episodic Migraine	Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min	0.2 mg/kg	69 ± 7	Male cynomolgus monkeys plasma protease	LC-MS/MS	Male cynomolgus monkeys plasma	In Vivo	None	None	Rat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325
4703	34217775	2022	vFCODVGPFC-3Pal	FE 205030	10	Oxazole-2-carbonyl, D-val at position 1	Amidation, 3-Pal modification at C terminal	Cyclic (C3-C10 disulfide bond)	Mix	Phe linked with (2-Cbm),3Pal, Orn linked with iPr	Derived from CGRP	Treatment of Acute Episodic Migraine	Blood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min	0.1 mg/kg	65 ± 5	Male cynomolgus monkeys plasma protease	LC-MS/MS	Male cynomolgus monkeys plasma	In Vivo	None	None	Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4714	N.A.	2022	eeeeeeeeeXPLGLAGrrrrrrrrrk	Alb-e9-XPLGLAG-r9-k(cy5)	25	Alb=albumin	Cy5 linked with Lys side chain at C terminus	Linear	Mix	e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Alb=albumin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker	Synthetic	Transport molecule	Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points	4.8 nmol	3	Mice blood plasma protease	N.A.	Mice blood plasma	In Vivo	None	US 201916457763 A	N.A.
4716	N.A.	2022	(eeeeeeeeeXPLGLAGrrrrrrrrrk)4	Streptavidin-[e9-XPLGLAG-r9-k(cy5)]4	100	Streptavidin	Cy5 linked with Lys side chain at C terminus	Linear	Mix	e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Strep=Streptavidin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker	Synthetic	Transport molecule	Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points	4 nmol	4	Mice blood plasma protease	N.A.	Mice blood plasma	In Vivo	None	US 201916457763 A	N.A.
4724	N.A.	2022	QTVVTQEPSLTVSPGGTVTLTCRSSTGAVTTSNYANWVQQKPGQAPRGLIGGTNKRAPGTPARFSGSLLGGKAALTLSGVQPEDEAEYYCALWYSNLWVFGGGTKLTVLGGGGSGGGGSGGGGSEVQLVESGGGLVQPGGSLKLSCAASGFTFNTYAMNWVRQAPGKGLEWVARIRSKYNNYATYYADSVKDRFTISRDDSKNTAYLQMNNLKTEDTAVYYCVRHGNFGNSYVSWFAYWGQGTLVTVSSGGGGSQVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTYTDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC-DIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPDRFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC	TROP2 TCE (PC1)	692	Free	Fab heavy chain linked to C terminus of ScFv light chain	Linear	L	None	Synthetic	Mediates tumor cytotoxicity and T cell activation	N.A.	3 ug/kg	1.02	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	US 2021/0062261 W	EC50(nM) = 0.1477 (TROP binding)
4732	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYEER-OH)	Example 1	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)tetradecanedioyl-gGlu-2×OEG), B3E, B27E, B28E modifications, , A and B chain linked with disulfide bond	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1 nmol/kg	103	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	hIGF1R 0.1% HSA (% rel to HI) Ex48 = 66.3
4733	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYTDR-OH)	Example 7	51	Free	B29R, desB30 modificaiton	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)tetradecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bond	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1 nmol/kg	86	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	hIGF1R 0.1% HSA (% rel to HI) Ex48 = 124.4
4734	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYTDR-OH)	Example 10	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modifications, A and B chain linked with disulfide bond	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1 nmol/kg	97	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	hIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3
4736	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGSHLVEALYLVCGERGFFETPR-OH)	Example 45	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	713 pmol/kg	182	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	N.A.
4737	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGSHLVEALYLVCGERGFFETPR-OH)	Example 45	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1714 pmol/kg	148	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	N.A.
4738	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGSHLVEALYLVCGERGFFETPR-OH)	Example 45	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	720 pmol/kg	153	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	N.A.
4739	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGSHLVEALYLVCGERGFFETPR-OH)	Example 45	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	706 pmol/kg	158	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	N.A.
4740	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGSHLVEALYLVCGERGFFETPR-OH)	Example 45	51	Free	B29R, desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications	Insulin Derivative	Antidiabetes	Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1735 pmol/kg	219	Lyd pig plasma protease	ELISA	Lyd pig plasma	In Vivo	None	US 201615754395 A	N.A.
4748	N.A.	2022	(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYEER-OH)	Example 31	51	Free	B29R, desB30 modification	Cyclic (C7-C12 disulfide bond in A chain)	L	A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B27E, B28E modifications, A and B chain linked with disulfide bond	Insulin Derivative	Antidiabetes	Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing	25 nmol/kg	79	SD rats plasma protease	LC-MS	SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative	In Vivo	None	US 201615754395 A	hIGF1R 0.1% HSA (% rel to HI) Ex48 = 55
4772	35177945	2022	QRPRlS-Aib-Ka-P-Nle-P	P26	12	N-Acetylated Arg2	Free	Linear	Mix	D-Leu, D-ala = l and a, Proline side chain linked with (4Br-Phe) at C terminus	Apelin Analog	Diuretic and Cardiovascular effects	Incubated at 37°C for various times, from T0 to T4 h	5 μM	86	Mouse plasma protease	LC-MS	Mouse plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/	None	Ki(nM) = 2.11 ± 0.40
4776	35177945	2022	QRPRLSHKGPMPF	Apelin-13	13	Free	Free	Linear	L	None	Secreted by White Adipose Tissue (Wat) in both humans and animals	Antidiabetes, Anorexic Effects	N.A.	N.A.	2.1	Mouse plasma protease	RP-HPLC	Mouse plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/	None	EC50 = 7.4 x 10⁻⁹ M
4781	35177945	2022	QRPRLSHKGPMPY	Lys8GluPAL(Tyr13)apelin-13	13	Free	Tyr13 modifcation, carboxylation	Linear	L	I125 radioactive labeled	Apelin-13 Analogue	Antidiabetes, Anorexic Effects	Blood (20 microliter) collected at 0, 15, 30, 45, 60, 90, 120, 240, 480, 960 and 1440 min after injection	4.1 nmol/kg	2.5 - 3	NIH swiss mice plasma protease	RP-HPLC	NIH swiss mice plasma	In Vivo	https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/	None	EC50 = 1.1 x 10⁻⁹ M
4783	35177945	2022	pGlu-RPRLSHKGPMPF	(pGlu)apelin-13	13	pGlu = Pyroglutamate	Amidation	Linear	L	None	Apelin-13 Analogue	Insulinotrophic activity	0, 2, 4, 8, 24 h	20 μg	3.8	Mouse plasma protease	RP-HPLC	Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer	In Vitro	https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/	None	EC50(M) = 1.10e-008 (In vitro insulin secretion)
4789	35259149	2022	GIVEQCCTSICSLYQLENYCN-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C3-Mal-CH)	CH-/HPN-Conjugated Insulins (LysB29)	50	Free	K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	3.4	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 2.48
4790	35259149	2022	GIVEQCCTSICSLYQLENYCN-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C3-Mal-CH)	CH-/HPN-Conjugated Insulins (LysB29)	50	Free	K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	4.4	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 2.48
4795	35259149	2022	GIVEQCCTSICSLYQLENYCN-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C6-Mal-CH)	CH-/HPN-Conjugated Insulins (LysB29)	50	Free	K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	2.2	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 1.52
4796	35259149	2022	GIVEQCCTSICSLYQLENYCN-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C6-Mal-CH)	CH-/HPN-Conjugated Insulins (LysB29)	50	Free	K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	2.8	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 1.52
4799	35259149	2022	(CH-Mal-C11-GIVEQCCTSICSLYQLENYCN)-FVNQHLCGSHLVEALYLVCGERGFFYTPK	CH-/HPN-Conjugated Insulins (GlyA1)	50	Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]	Free	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	4.8	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 11.01
4801	35259149	2022	GIVEQCCTSICSLYQLENYCN-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C11-Mal-CH)	CH-/HPN-Conjugated Insulins (LysB29)	50	Free	K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	4.9	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 1.29
4802	35259149	2022	GIVEQCCTSICSLYQLENYCN-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C11-Mal-CH)	CH-/HPN-Conjugated Insulins (LysB29)	50	Free	K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]	Cyclic (C6-C11 disulfide bond in A chain)	L	C7-C7 and C20-C19 disulfide bond between A and B chain	Human insulin analog	Antidiabetes	Blood samples were collected immediately before injection and at various time points up to 48 h after injection	340 nmol/kg	4.4	Mice serum protease	Sandwich ELISA	Mice serum	In Vivo	https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/	None	EC50(nM) = 1.29
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
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
4831	35807558	2022	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36	34	Free	Free	Linear	L	None	Neuropeptide Y	Antidiabetes, Antiobesity	The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)	1 μM	200	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	Ki(nM) = 40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4832	35807558	2022	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3−36 (methylamide)	34	Free	Methyl amide addition at C terminus	Linear	L	None	PYY analogue	Antidiabetes, Antiobesity	The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)	1 μM	200	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	Ki(nM) = >10,000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4836	35807558	2022	IKPEAPGEDASPEELNRYYASLRHYLNLVT-MeArg-QRY	[MeArg33]PYY3−36	34	Free	Methylated Arg33 at C terminus	Linear	L	Methylated Arg33	PYY analogue	Antidiabetes, Antiobesity	The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)	1 μM	200	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	Ki(nM) = 2500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4840	35807558	2022	IKPEAPGEDASPEELNRYYASLRHYLNLVT-βhArg-QRY	[β-homoArg33]PYY3−36	34	Free	β-homoArg33 at C terminus	Linear	L	β-homoArg33 modification	PYY analogue	Antidiabetes, Antiobesity	The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)	1 μM	230	Minipigs plasma protease	LC-MS	Minipigs plasma	In Vitro	https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/	None	Ki(nM) = 200 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
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)
4851	35011324	2021	SAVGRHGRRFGLRKHRKH	AWRK6	18	Free	Free	Linear	L	None	Based on the natural occurring peptide dybowskin-2CDYa	Antimicrobial	Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h	2.35 mg/kg	2.946 ± 2.048	SPF-grade male SD rats plasma protease	LC-MS/MS	SPF-grade male SD rats plasma	In Vivo	None	None	N.A.
4852	35011324	2021	SAVGRHGRRFGLRKHRKH	AWRK6	18	Free	Free	Linear	L	None	Based on the natural occurring peptide dybowskin-2CDYa	Antimicrobial	Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h	4.7 mg/kg	2.941 ± 1.399	SPF-grade male SD rats plasma protease	LC-MS/MS	SPF-grade male SD rats plasma	In Vivo	None	None	N.A.
4853	35011324	2021	SAVGRHGRRFGLRKHRKH	AWRK6	18	Free	Free	Linear	L	None	Based on the natural occurring peptide dybowskin-2CDYa	Antimicrobial	Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h	9.4 mg/kg	2.781 ± 1.021	SPF-grade male SD rats plasma protease	LC-MS/MS	SPF-grade male SD rats plasma	In Vivo	None	None	N.A.
4854	35011324	2021	SAVGRHGRRFGLRKHRKH	AWRK6	18	Free	Free	Linear	L	None	Based on the natural occurring peptide dybowskin-2CDYa	Antimicrobial	Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h	4.7 mg/kg	1.983 ± 0.583	SPF-grade male SD rats plasma protease	LC-MS/MS	SPF-grade male SD rats plasma	In Vivo	None	None	N.A.
4870	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 34	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	4	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4873	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 37	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	2	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4874	34707178	2021	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36 analogues 38	34	Free	Amidation	Linear	L	Fatty acid conjugation at position 30	Derived from PYY	Antiobesity	N.A.	15 nmol/kg	4	Male göttingen minipigs plasma protease	LC-MS	Male göttingen minipigs plasma	In Vivo	None	None	N.A.
4891	34630378	2021	LAEAKVLANRELDKYGVSDYYKNLINNAKTVEGVKALIDEILAALPGPVEDAITAAIGRVADTVGTGPTNSEAIPALTAAETGHTSQVVPGDTMQTRHVKNYHSRSESTIENFLCRSACVYFTEYENSGAKRYAEWVLTPRQAAQLRRKLEFFTYVRFDLELTFVITSTQQPSTTQNQDAQILTHQIMYVPPGGPVPDKVDSYVWQTSTNPSVFWTEGNAPPRMSIPFLSIGNAYSNFYDGWSEFSRNGVYGINTLNNMGTLYARHVNAGSTGPIKSTIRIYFKPKHVKAWIPRPPRLCQYEKAKNVNFQPSGVTTTRQSITTMTNTGAF	ABD-VP1	330	ABD	Free	Linear	L	None	Synthetic	Treatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis	1h at RT	0.25 μg/μL	280	Murine serum protease	ELISA	Murine serum	In Vivo	None	None	ABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73%
4896	34506138	2021	H-Aib-QGTFTSDYSKYLDSRRAQDFVQWL-X1-T	α/sulfono-γ-AApeptide hybrid analogue 15	35	Free	Amidation	Linear	L	Substitution of L-serine at position 2 with α-aminoisobutyric acid (Aib), X1 = Structure given in paper	α/Sulfono-γ-AApeptide Hybrid Analogues of Glucagon	Regulating glucose homeostasis	blood samples were obtained at 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h after injection	5 mg/kg	~4	C57Bl/6J female mice plasma protease	LC-MS/MS	C57BL/6J female mice plasma	In Vivo	None	None	EC50 (nM) = 0.86 (Bioactivity of α/Sulfono-γ-AApeptide Hybrid Analogues in Cre Luc Production Functional Assay)
4903	34402197	2021	HGDGSFSDEMNTILDNLAARDFINWLIQTKITD	Teduglutide	33	Free	Free	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	N.A.	0.05 mg/kg	1.1	Human plasma protease	N.A.	Human adult plasma (in Japanese patients with SBS)	In Vivo	DB id: DB08900	None	N.A.
4904	34402197	2021	HGDGSFSDEMNTILDNLAARDFINWLIQTKITD	Teduglutide	33	Free	Free	Linear	L	None	GLP-2 analogue	Treatment of Short Bowel Syndrome	N.A.	0.05 mg/kg	1.24	Human plasma protease	N.A.	Human adult plasma (in Non-Japanese patients with SBS)	In Vivo	DB id: DB08900	None	N.A.
4907	34393794	2021	KFRRQRPRLSHLGPMPF	LIT01-196	17	Fluorocarbon chain (CF3(CF2)7(CH2)2C(O)) attached to the N-terminal part of K17F	Free	Linear	L	None	Apelin-17 Analog	Treatment of Hypertension	N.A.	15 nmol/kg	156	Rats plasma protease	RIA	Rats plasma	In Vivo	Pubchem CID Apelin: 56841713	None	IC50 = 0.56 ± 0.04 nmol/l for LIT01-196
4910	34358122	2021	GGGGDRVYIHPF	AT1-HSA-MRN-NPs	12	Free	HSA linked through PEG4	Linear	L	None	Synthetic	Treatment of Cardiovascular Disease	Blood was collected from the jugular vein at the following timepoints: 0, 5, 15, 30, 45, 60, 120, and 360 min	50 μg/kg	101.3	Rats plasma protease	HPLC	Rats plasma	In Vivo	None	None	N.A.
4929	34048741	2021	HGEGTFTSDLSMQMEEEAVLLFIEWLMNGGPSSGAPPPSC	M4	40	Free	Cys addition at C terminal	Linear	L	M, R amino acid substitutions	Synthetic	Antidiabetes	Blood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h	0.07 mg/kg	1.80 ± 0.23	Male SD rats plasma protease	ELISA	Male SD rats plasma	In Vivo	None	None	EC50(nM) = 38.49 ± 4.58 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation)
4935	33918853	2021	TSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIKKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLG	HFn/DOX	172	Free	Free	Linear	L	None	Synthetic	Antitumor	Blood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C	3.0 mg/kg	3.07 ± 0.06	SD rats serum protease	Fluorescence spectrometry	SD rats serum	In Vivo	PDB id: 3AJO	None	IC50 (μg mL−1) = 0.49 ± 0.11
4942	33825469	2021	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLPETGGG	FITC-labeled Ex4−DNP 9	44	FITC-Ahx	Ex4 linked to DNP9 = Dinitro phenol by (PEG)n spacer	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection.	75 nmol/kg	2.07 ± 0.05	C57Bl/6 mice plasma protease	Fluorescence assay	C57BL/6 mice plasma	In Vivo	None	None	EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency)
4943	33825469	2021	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLPETGGG	FITC-labeled Ex4−DNP 10	44	FITC-Ahx	Ex4 linked to DNP10 = Dinitro phenol by (PEG)n spacer	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection.	75 nmol/kg	3.55 ± 0.33	C57Bl/6 mice plasma protease	Fluorescence assay	C57BL/6 mice plasma	In Vivo	None	None	EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency)
4944	33825469	2021	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLPETGGG	FITC-labeled Ex4−DNP 11	44	FITC-Ahx	Ex4 linked to DNP11 = Dinitro phenol by (PEG)n spacer	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection.	75 nmol/kg	2.62 ± 0.17	C57Bl/6 mice plasma protease	Fluorescence assay	C57BL/6 mice plasma	In Vivo	None	None	EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency)
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%
4964	33672039	2021	HGEGTFTSDVSSYLEGQAAKEFIAWLVRGRC	GLP1_8G37C-HSA	31	Free	HSA	Linear	L	Substituition of amino acid G at position 2	GLP-1 analogs	Antidiabetes	Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration	10 nmol/kg	3.2 (T1/2a)	BALB/c mice plasma protease	Sandwich ELISA	BALB/c mice plasma	In Vivo	None	None	EC50= 1340 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells)
4965	33672039	2021	HAGTFTSDVSSYLEGQAAKEFIAWLVRGRC	GLP1_8A37C-HSA	30	Free	HSA	Linear	L	Substituition of amino acid A at position 2	GLP-1 analogs	Antidiabetes	Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration	10 nmol/kg	3.3 (T1/2a)	BALB/c mice plasma protease	Sandwich ELISA	BALB/c mice plasma	In Vivo	None	None	EC50=185 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells)
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
4977	33656323	2021	PTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKKATELKHLQCLEEELKPLEEVLNLAQSKNFHLRPRDLISNINVIVLELKGSETTFMCEYADETATIVEFLNRWITFCQSIISTLT-(ED)6-LPETGGGK	B6	146	Free	Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid	Cyclic (C57-C104 Disulfide Bond) In IL-2	L	None	Synthetic	Anticancer, Autoimmune diseases treatment	Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding	0.6 mg/kg	3.595 ± 0.518(T1/2b)	Mouse plasma protease	Sandwich ELISA	Mouse plasma	In Vivo	pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf	None	KD (M) = (1.952 ± 0.130) × 10−8 for IL-2
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
4994	33555858	2021	LEGREKVRAQI-Aib-Aib-EGMSTWS-Aib-RKK	B10-33 (Cpd 58)	24	Acetylation	Amidation	Linear	L	Lys24 conjugated with(-(γE)3-C16), Aib	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h	1 mg/kg	4.3	Rats plasma protease	LCHRMS	Rats plasma	In Vivo	None	None	EC50 nM = 17.6 ± 8.1(97%) in OVCAR5 cells
4997	33555858	2021	LEGREKVRAQI-Aib-Aib-EG-Nle-STWS-Aib-RK-PEG12-K	Cpd 61(B10-33 )	24	Acetylation	Amidation	Linear	L	Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle	Synthetic	Treatment of Cardiovascular Diseases	N.A.	1 mg/kg	4.8	Rats plasma protease	LCHRMS	Rats plasma	In Vivo	None	None	EC50 nM = 1.0 ± 0.9 (79%) in OVCAR5 cells
4998	33555858	2021	LEGREKVRAKI-Aib-Aib-EG-Nle-STWS-Aib-RKK-PEG12-K	Cpd 62(B10-33 )	24	Acetylation	Amidation	Linear	L	Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23	Synthetic	Treatment of Cardiovascular Diseases	N.A.	1 mg/kg	4.3	Rats plasma protease	LCHRMS	Rats plasma	In Vivo	None	None	EC50 nM = 0.6 ± 0.4 (95%) in OVCAR5 cells
5000	33555858	2021	LEGREKVRAKI-Aib-Aib-EG-Nle-STWS-Aib-RKKK	Cpd 64(B10-33 )	24	Acetylation	Amidation	Linear	L	Lys24 conjugated with (-(PEG2)3-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23	Synthetic	Treatment of Cardiovascular Diseases	N.A.	1 mg/kg	3.9	Rats plasma protease	LCHRMS	Rats plasma	In Vivo	None	None	EC50 nM = 0.2 ± 0.1 (89%) in OVCAR5 cells
5001	33555858	2021	LEGREKVRAKI-Aib-Aib-EG-Nle-STWS-Aib-RKK-(PEG2)3-K	Cpd 65(B10-33 )	24	Acetylation	Amidation	Linear	L	Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23	Synthetic	Treatment of Cardiovascular Diseases	N.A.	1 mg/kg	3.4	Rats plasma protease	LCHRMS	Rats plasma	In Vivo	None	None	EC50 nM = 0.1 ± 0.1 (88%) in OVCAR5 cells
5002	33555858	2021	LEGREKVRAKI-Aib-Aib-EG-Nle-STWS-Aib-RKK-(PDGA)3-K	Cpd 66(B10-33 )	24	Acetylation	Amidation	Linear	L	Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23	Synthetic	Treatment of Cardiovascular Diseases	N.A.	1 mg/kg	3.96	Rats plasma protease	LCHRMS	Rats plasma	In Vivo	None	None	EC50 nM = 0.4 ± 0.2 (88%) in OVCAR5 cells
5007	33387593	2021	APARSPSPSTQPWECDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE	GMOP-IFN	179	GM-CSF O-glycosylated Peptide	Free	Linear	L	None	Synthetic	Antiviral, Antiproliferative	Blood samples were taken at different times post-injection	100000 U	3.0 ± 0.4(T1/2 Elimination)	Rats plasma protease	Sandwich ELISA	Rats plasma	In Vivo	PDB id: 1ITF	None	Antiviral SBA (IU/ng) = 190 ± 30 in GMOP-IFN, Antiproliferative SBA (IU/ng) = 280 ± 40
5008	33387593	2021	APARSPSPTPTPTPT-CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE	mGMOP-IFN	180	Modified GOMP	Free	Linear	L	None	Synthetic	Antiviral, Antiproliferative	Blood samples were taken at different times post-injection	100000 U	2.5 ± 0.2 (T1/2 Elimination)	Rats plasma protease	Sandwich ELISA	Rats plasma	In Vivo	PDB id: 1ITF	None	Antiviral SBA (IU/ng) = 280 ± 50 in mGMOP-IFN, Antiproliferative SBA (IU/ng = 95 ± 5
5009	33245951	2021	YAEGTFISDYSIAMDKIRQQNFVNWLLAQKGKKSDWKHNITQ	GIP(1–42)	42	Free	Free	Linear	L	None	Secreted by entero-endocrine K cells located in the proximal intestine	Insulinotrophic Effect	Blood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min	25 nmol/kg	93 ± 2	Mouse plasma protease	RIA	Mouse plasma	In Vivo	https://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type=	None	N.A.
5016	33129837	2021	VDKPPYLPRPRPIRrPGGr	OM19r-8	19	Free	Amidation	Linear	Mix	replacing L-Arg15,19 with D-Arg15,19	Derived from the antibacterial peptide OM19R	Antibacterial	Aliquots were analyzed after 0, 20, 30, 40, 60, 80, 90, 100, 120, 150, 180, 210, 240, 175 and 270min	31.5 μmol/L	71.10 ± 3.43	Wistar rats blood plasma protease	HPLC	Wistar rats blood plasma	In Vitro	None	None	MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin
5017	33129837	2021	VDKPPYLPRPRPIRrPGGr	mPEG5- OM19r-8	19	mPEG5	Amidation	Linear	Mix	replacing L-Arg15,19 with D-Arg15,19	Derived from the antibacterial peptide OM19R	Antibacterial	Aliquots were analyzed after 0, 20, 30, 40, 60, 80, 90, 100, 120, 150, 180, 210, 240, 270, 300, 400, 600 and 1000min	31.5 μmol/L	242.44 ± 39.21	Wistar rats blood plasma protease	HPLC	Wistar rats blood plasma	In Vitro	None	None	MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin
5039	32078672	2020	KTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG	rFVIIIFc	865	Free	IgG1 Fc	Linear	L	None	Synthetic	Role In Clotting	N.A.	200 IU/kg	1.85	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
5051	33310780	2020	TIEEQR-2-(7-octenyl)alanine-KTFLDK-S-2-(4-pentenyl)alanine-NHEAEDLFYQ-S-2-(4-pentenyl)alanine-SLA-S-2-(4-pentenyl)alanine-WN	NYBSP-4	34	Acetylation	Amidation	Linear	L	2-(7-octenyl)alanine-2-(4-pentenyl)alanine modifications	Derived from ACE2	Antiviral	0, 10, 30, 60, and 120 min	1mM	>289	Human plasma protease	LC-MS/MS	Human plasma	In Vitro	None	None	IC50 = 1.97 ± 0.14 μM in HT1080/ACE2 cells
5052	33310780	2020	TIEEQAKTFLDKFNHEAEDLFYQSSLASWN	NYBSP-C	30	Acetylation	Amidation	Linear	L	None	Derived from ACE2	Antiviral	0, 10, 30, 60, and 120 min	1 mM	>289	Human plasma protease	LC-MS/MS	Human plasma	In Vitro	None	None	IC50 >27.7 μM in HT1080/ACE2 cells
5053	33284103	2020	YLGASVPSPDPLEPTREQCELNPACDELSDQYGLKTAYKRIYGITI	Mouse ucOCN	46	Free	Free	Cyclic (C19-C25 Disulfide bond)	L	Uncarboxylation at all glutamic acid	Osteoblast Derived hormone	Antidiabetes	0 to 5 hr at 37°C	100 ng/mL	~120	Mouse plasma protease	ELISA	Mouse plasma	In Vitro	None	None	N.A.
5054	33284103	2020	YLGASVPSPDPLEPTREQCELNPACDELSDQYGLKTAYKRIYGITI	Mouse O-glycosylated ucOCN	46	Free	Free	Cyclic (C19-C25 Disulfide bond)	L	O-glycosylation likely at Ser8 in SVPSPDP, Uncarboxylation at all glutamic acid	Osteoblast Derived hormone	Antidiabetes	0 to 5 hr at 37°C	100 ng/mL	>5	Mouse plasma protease	ELISA	Mouse plasma	In Vitro	None	None	N.A.
5055	33284103	2020	YLGASVPSPDPLEPTREQCELNPACDELSDQYGLKTAYKRIYGITI	Mouse O-glycosylated ucOCN	46	Free	Free	Cyclic (C19-C25 Disulfide bond)	L	O-glycosylation likely at Ser8 in SVPSPDP, Uncarboxylation at all glutamic acid	Osteoblast Derived hormone	Antidiabetes	2 hours at 37°C	40 ng/g	~182	Mice serum protease	OCN ELISA	Mice serum	In Vivo	None	None	N.A.
5056	33284103	2020	YLGASVPSPDPLEPTREQCELNPACDELSDQYGLKTAYKRIYGITI	Mouse ucOCN	46	Free	Free	Cyclic (C19-C25 Disulfide bond)	L	Uncarboxylation at all glutamic acid	Osteoblast Derived hormone	Antidiabetes	2 hours at 37°C	40 ng/g	~108	Mice serum protease	OCN ELISA	Mice serum	In Vivo	None	None	N.A.
5060	33125843	2020	H-Aib-EGTYTNDVTEYCEEEAAKCFIEWLIKGKPSSGAPPPSYGWLDF	5a	45	Free	Either or nonsulfated gastrin-6 were coupled to the C-terminus of 2d and 2k through two OEG spacers, affording 5a−5d	Linear	L	Aib substiuition at position 2, Ser39 linked with fatty acid	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus	50 nmol/kg	1.7	SD rats plasma protease	LC−MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 0.040 ± 0.011 (Effects of 5a on GLP-1R)
5061	33125843	2020	H-Aib-EGTYTNDVTEYLEEEAAKCFIEWLICGKPSSGAPPPSYGWLDF	5b	45	Free	Either or nonsulfated gastrin-6 were coupled to the C-terminus of 2d and 2k through two OEG spacers, affording 5a−5d	Linear	L	Aib substiuition at position 2,Ser39 linked with fatty acid	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus	50 nmol/kg	1.9	SD rats plasma protease	LC−MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 0.048 ± 0.018 (Effects of 5b on GLP-1R)
5062	33125843	2020	H-Aib-EGTYTNDVTEY-C1-EEEAAK-C1-FIEWLIKGKPSSGAPPPSYGWLDF	6a	45	Free	4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d	Linear	L	C1 = structure given in paper, Aib substiuition at position 2,Ser39 linked with fatty acid	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus	50 nmol/kg	4.6	SD rats plasma protease	LC−MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 0.022 ± 0.008 (Effects of 6a on GLP-1R)
5063	33125843	2020	H-Aib-EGTYTNDVTEYLEEEAAK-C1-FIEWLI-C1-GKPSSGAPPPSYGWLDF	6b	45	Free	4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d	Linear	L	C1 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus	50 nmol/kg	5	SD rats plasma protease	LC−MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R)
5064	33125843	2020	H-Aib-EGTYTNDVTEY-C2-EEEAAK-C2-FIEWLIKGKPSSGAPPPSYGWLDF	7a	45	Free	4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d	Linear	L	Modification of 6a and 6b with the introduction of C2 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus	50 nmol/kg	2.9	SD rats plasma protease	LC−MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R)
5065	33125843	2020	H-Aib-EGTYTNDVTEYLEEEAAK-C2-FIEWLI-C2-GKPSSGAPPPSYGWLDF	7b	45	Free	4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d	Linear	L	Modification of 6a and 6b with the introduction of C2 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus	50 nmol/kg	3.1	SD rats plasma protease	LC−MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R)
5066	33057063	2020	GTSHLVKCAEKEKTFCVNGGECFMVKDLSNPSRYLCKCPNEFTGDRCQNYVMASFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTFPPSQEEMTKNQVSLRCLVKGFYPSDIAVEWESNGQPENNYKTTKPVLDSDGSFRLESRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLS	NRG1-MFc	268	Free	fusion of the C-terminus of NRG1 to the N-terminus of the Fc fragment	Linear	L	None	Synthetic	Her4-Selective Agonism	Overnight at 4 °C	10 μg/mL	1.4	Mouse serum protease	ELISA	Mouse serum	In Vitro	PDB ID: 3U7U	None	HER4 binding KD = 640 nM
5068	33057063	2020	GGGGSGGGGSGTSHLVKCAEKEKTFCVNGGECFMVKDLSNPSRYLCKCPNEFTGDRCQNYVMASFGGGGSGGGGS	ALM6	75	Free	Free	Linear	L	None	Synthetic	Her4-Selective Agonism	Overnight at 4 °C	10 μg/mL	1.4	Mouse serum protease	ELISA	Mouse serum	In Vitro	None	None	HER4 binding KD = 440 nM
5070	33008433	2020	HSQFIGYPITLFVEKER	Hypoxic-Ischemic Brain Damage Associated Peptide (HIBDAP)	17	Free	Free	Linear	L	None	derives from the 210st to 226st amino acids of HSP90AA1	Involved In The Nod-Like Receptor (Nlr) Signaling Pathway	N.A.	N.A.	3.5	Mammalian reticulocytes protease	N.A.	Mammalian reticulocytes with OGD ( oxygen and glucose deprivation (OGD))	In Vitro	None	None	N.A.
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.
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.
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.
5088	32858124	2020	hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip{nt:C6-γGlu-OEG-OEG}	Cmpd# 6	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.1 mg/kg	2.31	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 2.31 ± 0.57
5089	32858124	2020	C13-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 10	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.1 mg/kg	3.4	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6
5090	32858124	2020	C15-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 12	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C15	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.1 mg/kg	1.84	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 4.39 ± 0.73
5091	32858124	2020	C17-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 14	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.1 mg/kg	2.18	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE =7.42 ± 0.9
5092	32858124	2020	(C6-diacid)-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 17	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 diacid	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.1 mg/kg	2.32	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 4.10 ± 0.62
5094	32858124	2020	C6-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 6	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.5 mg/kg	2.6	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 2.31 ± 0.57
5098	32858124	2020	(C6-diacid)-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 17	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 diacid	Free	Linear	Mix	hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid	Derived from pyr-apelin-13	Treatment of Chronic Hepatic Failure	N.A.	0.5 mg/kg	4.1	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 4.10 ± 0.62
5100	32847850	2020	IRDVPPADQEKLFIQKLRQCCVLFDFVSDPLSDLKWKEVKRAALSEMVEYITHNRNVITEPIYPEVVHMFAVNMFRTLPPSSNPTGAEFDPEEDEPTLEAAWPHLQLVYEFFLRFLESPDFQPNIAKKYIDQKFVLQLLELFDSEDPRERDFLKTTLHRIYGKFLGLRAYIRKQINNIFYRFIYETEHHNGIAELLEILGSIINGFALPLKEEHKIFLLKVLLPLHKVKSLSVYHPQLAYCVVQFLEKDSTLTEPVVMALLKYWPKTHSPKEVMFLNELEEILDVIEPSEFVKIMEPLFRQLAKCVSSPHFQVAERALYYWNNEYIMSLISDNAAKILPIMFPSLYRNSKTHWNKTIHGLIYNALKLFMEMNQKLFDDCTQQFKAEKLKEKLKMKEREEAWVKIENL	PPP2R5A	407	Free	Free	Linear	L	Blue fluorescent protein (BFP) labeling	encoded by the PPP2R5A gene in humans	Antiviral	48 hours	250 ng	~2	293T Cell Line Lysate Protease	flow cytometry	293T cell line lysate with Vif	In Vivo	PDB id = 2IAE	None	N.A.
5103	32844654	2020	PKPEAPGKDASPEEWNRYYADLRHYLNWLTRQRY	Peptide 11	34	Free	Amidation	Linear	L	None	PYY analog	Antiobesity	Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion	0.033 mg/kg	1.2	Mouse plasma protease	UPLC-MS/MS	Mouse plasma	In Vivo	None	None	EC50 (nM) = 0.29 ± 0.03 for hNPY2R (cAMP)
5105	32844654	2020	PKPEAPGKDASPEEWNRYYACLRHYLNCLTRQRY	Peptide 18	34	Free	Amidation	Cyclic (Cys-Cys Disulfide Bond)	L	Cysteine substiution at 23, 30	PYY analog	Antiobesity	Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion	0.033 mg/kg	4.5	Mouse plasma protease	UPLC-MS/MS	Mouse plasma	In Vivo	None	None	EC50 (nM) = 0.91 ± 0.08 for hNPY2R (cAMP)
5106	32844654	2020	PKPEAPGKDASPEEWNRYYADLRHYLNWLTRQRY	Peptide 11	34	Free	Amidation	Linear	L	None	PYY analog	Antiobesity	Blood samples were collected between 0.25 and 48 h	0.1 mg/kg	1.21	Rats plasma protease	UPLC-MS/MS	Rats plasma	In Vivo	None	None	EC50 (nM) = 0.29 ± 0.03 for hNPY2R (cAMP)
5112	32812282	2020	SYSMEHFRWGKPVGKKRRPVKVYPNGAEDESAEAFPLEF	ACTH	39	Free	Free	Linear	L	None	Deriving from the pro-opimelanocortin (POMC)	Stimulates The Adrenal Cortex To Produce And Secrete Cortisol	4 ◦C for 15 min	40 μM	250	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	N.A.
5120	32759365	2020	MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGR	hAβ40	40	Free	Free	Linear	L	None	Synthesized in neurons and degraded in the brain and liver	Treatment of Alzheimer's diseases	Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose	64.5 ± 13.2 µg/kg	75.5 ± 17.9 (Terminal Half Life)	Untreated rats CSF protease	ELISA	untreated rats CSF	In Vivo	pdb id: 8KEW	None	N.A.
5123	32736262	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLKEAKEKAIEELKKAGITSDYYFDLINKAKTVEGVNALKDEILKA	EX-AFF	84	Free	AFF	Linear	L	None	Synthetic	Antiobesity	Blood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio	50 nmol/kg	1.5	ICR mice plasma protease	ELISA	ICR mice plasma	In Vivo	None	None	Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1))
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.
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.
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
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
5154	32506501	2020	SYSMEHFRWGKPVGKKRRPVKVYPNGAEDESAEAFPLEF	ACTH	39	Free	Free	Linear	L	None	Derived from POMC	Stimulates the adrenal glands to release cortisol	37 °C	2 µM	3.79	Human plasma protease	Glo-sensor transfected cell-based luminescence assay	Human plasma	In Vitro	None	None	EC50 (M) = 1.54E-09 for MC1R-ACTH
5156	32506501	2020	YVMGHFRWDRFGRRNSSSSGSSGAGQ	gamma3-MSH	26	Free	Free	Linear	L	None	Derived from POMC	Antiinflammatory and Cardiovascular function	37 °C	2 µM	2.62	Human plasma protease	Glo-sensor transfected cell-based luminescence assay	Human plasma	In Vitro	None	None	EC50 (M) = 9.37E-10 for MC1R-g3-MSH
5159	32506501	2020	YVMGHFRWDRFG	gamma2-MSH	12	Free	Amidation	Linear	L	None	Derived from POMC	Antiobesity	37 °C	2 µM	1.44	Human CSF protease	Glo-sensor transfected cell-based luminescence assay	Human CSF	In Vitro	None	None	EC50 (M) = 7.749E-10 for MC1R-g2-MSH
5166	32380198	2020	RPRLSHKGPMPF	Apelin-12	12	Free	Free	Linear	L	None	Smallest fragment of a 77 amino acid prepropeptide	Cardioprotective Properties	N.A.	2-3 mg/ml	165 (Terminus Half Life)	Human blood plasma protease	1H-NMR	Human blood plasma	In Vitro	None	None	peptide M showed a significantly more pronounced effect in improving LV systolic function in Dox-induced cardiomyopathy compared to apelin-12 at a dose of 50 μg/kg
5167	32348108	2020	Aib-EGTFTSD-(R-octenyl alanine)-SSYLEG-(Bis-pentenyl glycine)-AAKEFIAWLVKGR	SAH-GLP-1-A8J(16,23)	28	Aminoisobutyric acid	Free	Linear	L	Modifications include (R-octenyl alanine) and (Bis-pentenyl glycine)	Single-stapled analogs of GLP-1	Antidiabetes	20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min	1 mM	120	Proteinase K	LC-MS/MS	DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4	In Vitro	PDB:3IOL	None	EC50 = 160 pM for SAH-GLP-1(16, 23, 30)
5169	32348108	2020	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	stitched GLP-1	30	Free	Free	Cyclic (I, I+7 Stitched GLP)	L	None	Stitched GLP-1	Antidiabetes	20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min	1 mM	220	Proteinase K	LC-MS/MS	DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4	In Vitro	None	None	EC50 = 160 pM for SAH-GLP-1(16, 23, 30)
5173	32348108	2020	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min	10 μM	170	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vitro	None	None	EC50 = 160 pM for SAH-GLP-1(16, 23, 30)
5198	32169063	2020	MALTFALLVALLVLSCKSSCSVGCDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKESSSSKAPPPSLPSPSRLPGPSDTPILPQ	IFN-1CTPON	216	Free	Carboxyl-terminal peptide (CTP) of the human chorionic gonadotropin β subunit and N-linked glycosylation sequences were linked to rhIFN-α2b at C terminus	Linear	L	None	Derived from rhIFN-α2b	Antiviral, Antitumor	Intraocular venous blood was collected at 0.5, 1, 2, 4, 8, and 24 h postinjection	50 μg/kg	2.62 ± 0.34	Mice blood protease	ELISA	Mice blood sample	In Vivo	PDB id: 1ITF	None	Antiviral activities of IFN-1CTPON = 8.22 × 106 IU/mg
5199	32169063	2020	SSSSKAPPPSLPSPSRLPGPSDTPILPQMALTFALLVALLVLSCKSSCSVGCDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKESSSSKAPPPSLPSPSRLPGPSDTPILPQ	IFN-2CTPON	244	Carboxyl-terminal peptide (CTP) of the human chorionic gonadotropin β su bunit and N-linked glycosylation sequences were linked to rhIFN-α2b at N terminus	Carboxyl-terminal peptide (CTP) of the human chorionic gonadotropin β su bunit and N-linked glycosylation sequences were linked to rhIFN-α2b at C terminus	Linear	L	None	Synthetic	Antiviral, Antitumor	Intraocular venous blood was collected at 0.5, 1, 2, 4, 8, and 24 h postinjection	50 μg/kg	3.45 ± 0.87	Mice blood protease	ELISA	Mice blood sample	In Vivo	PDB id: 1ITF	None	Antiviral activities of IFN-2CTPON = 3.12 × 106 IU/mg
5200	32169063	2020	CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMNEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE	rhIFN-α2b	165	Free	Free	Linear	L	None	Synthetic	Antiviral, Antitumor	Intraocular venous blood was collected at 0.5, 1, 2, 4, 8, and 24 h postinjection	50 μg/kg	1.34 ± 0.48	Mice blood protease	ELISA	Mice blood sample	In Vivo	PDB id: 1RH2	None	Antiviral activities of rhIFN-α2b = 5.29 × 107 IU/mg
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
5216	32075870	2020	HGDGSFSDE-Nle-fTILDLLAARDFINWLIQTKITD	Apraglutide	33	Free	Amidation	Linear	L	Gly2, Nle10, D-Phe11, Leu16 modification	Derived from hGLP-2	Treatment of Short Bowel Syndrome	Blood samples were collected at multiple time points up to 6 h post injection	0.2 mg/kg	159 ± 27(Elimination Half Life)	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	EC50(nM) = 0.24 for hGLP-2 receptor
5220	32075870	2020	HGDGSFSDEMNTILDNLAARDFINWLIQTKITD	Teduglutide	33	Free	Free	Linear	L	G amino acid substituition at position 2	Derived from hGLP-2	Treatment of Short Bowel Syndrome	Blood samples were collected at multiple time points up to 6 h post injection	0.100 mg/kg	88 ± 11 (Elimination Half Life)	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 0.09 for hGLP-2 receptor
5228	32075870	2020	HGDGSFSDEMNTILDNLAARDFINWLIQTKITD	Teduglutide	33	Free	Free	Linear	L	G amino acid substituition at position 2	Derived from hGLP-2	Treatment of Short Bowel Syndrome	Blood samples were collected at multiple time points up to 169 h post injection	0.15 mg/kg	2.7 ± 0.8 (Terminal Half Life)	Göttingen minipigs plasma protease	LC-MS/MS	Göttingen minipigs plasma	In Vivo	None	None	EC50(nM) = 0.09 for hGLP-2 receptor
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
5232	31996466	2020	DYLKEVFEKLRDLYEKFTPAVSTYTGIFTDQVLSVLKGEE	D6PV	40	Free	Free	Linear	L	Replaces 18A with a modified central region of apoC-II	Derived from apoC-II	TG-Lowering Effects	N.A.	46.7 mg/kg	3 (Initial Elimination Half Life)	Mice plasma protease	LC-MS/MS	Mice plasma	In Vivo	None	None	Equilibrium dissociation constant (Kd) of D6PV binding to HDL was determined to be 18.5 μM
5238	31926774	2020	QHWSYLLRPX	PEG5K-LEU	10	Free	Free	Linear	L	PEGylation at His2	Derived from leuprolide	Anticancer (Treatment of Advanced Prostate Cancer)	Blood samples were collected from rats orbit at predetermined time interval	1.0 mg/kg	1.28 ± 0.64	SD rats serum protease	UPLC–MS/MS	SD rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/	None	The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group
5239	31926774	2020	QHWSYLLRPX	PEG5K-LEU	10	Free	Free	Linear	L	PEGylation at His2	Derived from leuprolide	Anticancer (Treatment of Advanced Prostate Cancer)	Blood samples were collected from rats orbit at predetermined time interval	1.0 mg/kg	1.51 ± 0.127	SD rats serum protease	UPLC–MS/MS	SD rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/	None	The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group
5242	31841696	2020	LSPPRYPGGGS	P9	11	Free	Amidation	Linear	L	None	Synthetic	Anticancer	37 °C for 5, 10, 20, 25, 30, 45 min	N.A.	19	Human plasma protease	HPLC	Human plasma	In Vitro	https://sci-hub.se/10.1007/s13277-015-3435-x	None	IC50 of P48 for Hela229 = 0.6 nM
5243	31841696	2020	SPPRYPGGGS	P48	10	Leucine reduction	Amidation	Linear	L	None	Generated with P9 degradation	Anticancer	1, 2, 3, 4, 5, 10, 12 h.	N.A.	4	Human plasma protease	HPLC	Human plasma	In Vitro	https://sci-hub.se/10.1007/s13277-015-3435-x	None	IC50 of P48 for Hela229 = 0.6 nM
5246	31776208	2020	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hour after sHDL administration	50 mg/kg	2.1	Rats serum protease	LC-MS	SD rats serum	In Vivo	None	None	The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD
5247	31776208	2020	PVLDLFRELLNELLEALKQKLKP	22A-P	23	Free	Proline addition at C terminal	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hour after sHDL administration	50 mg/kg	4.2	Rats serum protease	LC-MS	SD rats serum	In Vivo	None	None	The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD
5248	31776208	2020	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration	50 mg/kg	3.3	Rats serum protease	LC-MS	SD rats serum	In Vivo	None	None	The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD
5249	31776208	2020	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration	50 mg/kg	3	Rats serum protease	LC-MS	SD rats serum	In Vivo	None	None	The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD
5250	31776208	2020	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration	50 mg/kg	3.3	Rats serum protease	LC-MS	SD rats serum	In Vivo	None	None	The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD
5251	31776208	2020	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration	50 mg/kg	3.3	Rats serum protease	LC-MS	SD rats serum	In Vivo	None	None	The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD
5267	N.A.	2020	CSWPARCLHQDLC	Ac-(06-34-18) (wildtype)	12	Acetylation	Free	Linear	L	None	Synthetic	Targets plasma kallikrein	N.A.	5 uM	2.3	Rats plasma protease	Waters Xevo TQ-MS	Rats plasma	In Vitro	None	US 201214350192 A	IC50(nM)(rat kallikrein) = 1.7
5269	N.A.	2020	CSWPA-4GuanPhe-CLHQDLC	Ac-(06-34-18) ( 4GuanPhe5)	12	Acetylation	Free	Linear	L	4GuanPhe6 replaces Arg (R)	Synthetic	Targets plasma kallikrein	N.A.	5 uM	2.8	Rats plasma protease	Waters Xevo TQ-MS	Rats plasma	In Vitro	None	US 201214350192 A	IC50(nM)(rat kallikrein) = 21
5276	N.A.	2020	CSFPY-4GuanPhe-CLHQDLC	Ac-(06-34-18) Phe2 Tyr4 4GuanPhe5	12	Acetylation	Free	Linear	L	4GuanPhe replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr	Synthetic	Targets plasma kallikrein	N.A.	5 uM	5	Rats plasma protease	Waters Xevo TQ-MS	Rats plasma	In Vitro	None	US 201214350192 A	IC50(nM)(rat kallikrein) = 2.5
5298	31843919	2019	VCKRWKKWKRKWKKWCV	ZY4	17	Free	Amidation	Cyclic (C2-C16 Disulfide Bond)	L	None	Cathelicidin-BF15 analogs	Antimicrobial	Blood samples were drawn retroorbitally under short-term anesthesia at different time points (1, 5, 10, 30, 60 min, and 2, 5, 10, 18, 24 h)	8 mg/kg	1.859	Mice plasma protease	LC-MS/MS	Mice plasma	In Vivo	None	None	MIC (µM) = 1.9 for ZY4 in P. aeruginosa CICC21625 , MIC (µM) = 2 for ZY4 in B. subtilis , MIC (µM) = 2 for ZY4 in S. aureus , MIC (µM) = 2 for ZY4 in C. albicans
5304	31805154	2019	MTWEEWDKKIEEYTKKIEELIKKS	CP24	24	Free	Free	Linear	L	None	Synthetic	Antiviral (HIV-1 Fusion Inhibitory Peptide)	Serial blood samples were collected from monkeys that received CP24 or IBP-CP24 before injection and at 2, 4, 6, 24, 72 and 144 h post-injection	10 mg/kg	1.69	Rhesus monkeys plasma protease	Sandwich ELISA	Rhesus monkeys plasma	In Vivo	None	None	IC50(nM) = 0.8±0.2 for CP24 in virus subtype A (92UG029)
5309	31654685	2019	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRAEAAAAKEAAAAKEAAAAKA	Off-target repebody-fused GLP-1	50	Repebody	GLP-1(7-36) (A8G) fused to the off-target repebody through linker (A(EAAAAK)3A) at C terminus	Linear	L	None	Synthetic	Antidiabetes	Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis	25 nmol/kg	1.3 (Initial Half Life)	Mice plasma protease	Sandwich ELISA	Mice plasma	In Vivo	PDB id: 5VAI	None	C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases
5310	31654685	2019	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRAEAAAAKEAAAAKEAAAAKA	Repebody-fused GLP-1 in complex with HSA	50	Repebody	GLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminus	Linear	L	None	Synthetic	Antidiabetes	Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis	25 nmol/kg	4.2 (Initial Half Life)	Mice plasma protease	Sandwich ELISA	Mice plasma	In Vivo	PDB id: 5VAI	None	C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases
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)
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)
5320	31580912	2019	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	Fluorescence dye	Synthetic	Hypoglycemic Activity	Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h	1 mg/ml	1.6	Nude mice serum protease	Fluorescence assay	Nude mice serum	In Vivo	PDB id: 7MLL	None	EC50(M) = 6.1 × 10−10 ± 9.3 × 10−11
5321	31580912	2019	HGEGTFTSDLSCQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide K12C	39	Free	Amidation	Linear	L	K12C modification, fluorescence dye	Synthetic	Hypoglycemic Activity	Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h	1 mg/ml	2.5	Nude mice serum protease	Fluorescence assay	Nude mice serum	In Vivo	None	None	EC50(M) = 4.0 × 10−11 ± 1.4 × 10−12 for K12C-PEG 5KDa
5322	31580912	2019	HGEGTFTSDLSCQMEEEAVRLFIEWLKNGGPSSGAPPPS	K12C-PEG 5kD	39	Free	Amidation	Linear	L	K12C modification, fluorescence dye, PEG(5KDa) conjugation at Lys27	Synthetic	Hypoglycemic Activity	Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h	1 mg/ml	1.7	Nude mice serum protease	Fluorescence assay	Nude mice serum	In Vivo	None	None	EC50(M) = 4.0 × 10−11 ± 1.4 × 10−12
5325	31580912	2019	HGEGTFTSDLSCQMEEEAVRLFIEWLKNGGPSSGAPPPS	K12C-PEG 10 kD-K12C	39	Free	Free	Linear	L	Lys27 conjugaged with (PEG(10KDa)-HGEGTFTSDLSCQMEEEAVRLFIEWLKNGGPSSGAPPPS)	Synthetic	Hypoglycemic Activity	Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h	1 mg/ml	2.1	Nude mice serum protease	Fluorescence assay	Nude mice serum	In Vivo	None	None	EC50(M) = 4.4 × 10−11 ± 4.9 × 10−12
5329	31389463	2019	HSQGTFTSDYSKYLDSRRAQDFVQWLMNTKRNKNNIA	OXM	37	Free	Free	Linear	L	None	Secreted postprandially by intestine L-cells	Antidiabetes, Antiobesity	blood was sampled pre-dose and at 0.5, 1, 2, 4, 8, 24, 48, 72, and 96 h post-dose	30 nmoL/kg	2.1 ± 0.6	SD rats plasma protease	LC-MS, ELISA	SD rats plasma	In Vivo	pdb id: 7LLY_5	None	EC50(nM) = 0.691 for Human GLP-1R
5331	31368418	2019	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGOPSSGAPPPS	EX	39	Free	Free	Linear	L	O=Ornithine	GLP-1 analogs	Antidiabetes	Blood samples were collected before and after administration at 1, 3, and 6 h and 1–35 d	2 mg/kg	2.59 ± 0.05	SD rats plasma protease	ELISA	SD rats plasma	In Vivo	None	None	The blood glucose levels of saline-treated controls remained at 20 mM, while EX or LA-EX rapidly decreased the levels of blood glucose to approximately 10 mM after administration, which were maintained for approximately 6 h
5335	31480738	2019	CWMEWDREINNYTSLIHSLIEESQNQQEKNEQELL	PEG2kC34	35	2 kDa PEG conjugated to the N-terminus of cC34 through Mal linker	Free	Linear	L	None	Synthetic	Antiviral (HIV-1 fusion inhibitory peptides)	Blood samples (300 μL) were harvested from the tail vein before injection and at different time intervals after injection (0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10.0 and 24.0 h	1.7 μmol/kg	2.57 ± 0.71	Rats plasma protease	N.A.	Rats plasma	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC7343207/	None	EC50 =4.14 ± 1.89 for NL4-3 strain
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.
5339	31443263	2019	LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES	LL-37	37	Free	Free	Linear	L	None	Synthetic	Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions)	37 °C	N.A.	242.47 ± 45.09	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
5341	31443263	2019	IGKEFKRIVQRIKDFLRNLVPRTERKDVY	LTP	29	Free	TP5 conjugated with LTP(13-36) at C terminus	Linear	L	None	Synthetic	Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions)	37 °C	N.A.	240.03 ± 55.14	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
5349	31278957	2019	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	Labeled with Flamma® 675 vinylsulfone	Exendin-4 analogs	Antidiabetes	The fluorescence images of the mice were measured at 0, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 147 h after injection	20 μg	2.2	Mouse body protease	In vivo imaging system	Mouse body	In Vivo	PDB id: 7MLL	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.
5384	31100806	2019	MAATHEHSAQWLNNYKKGYGYGPYPLGINGGMHYGVDFFMNIGTPVKAISSGKIVEAGWSNYGGGNQIGLIENDGVHRQWYMHLSKYNVKVGDYVKAGQIIGWSGSTGYSTAPHLHFQRMVNSFSNSTAQDPMPFLKSAGYGKAGGTVTPTPNTGWKTNKYGTLYKSESASFTPNTDIITRTTGPFRSMPQSGVLKAGQTIHYDEVMKQDGHVWVGYTGNSGQRIYLPVRTWNKSTNTLGVLWGTIKLEHHHHHH	Lysostaphin	255	Free	Free	Linear	L	None	Produced by Staphylococcus simulans	Antibacterial	The blood was sampled from the tail vein at 25 min, 40 min, 1 h, 2 h, and 4 h time points in the group that received lysostaphin	1 mg/ml	1.5 ± 0.7	Rats plasma protease	Sandwich ELISA	Rats plasma	In Vivo	PDB id: 4LXC	None	Minimum inhibitory concentration (MIC) of Lst-HDD towards S. aureus ATCC 29,213 was 3.2 µg/mL and concentration is 0.1 µg/mL
5385	31100806	2019	MGSAATHEHSAQWLNNYKKGYGYGPYPLGINGGMHYGVDFFMNIGTPVKAISSGKIVEAGWSNYGGGNQIGLIENDGVHRQWYMHLSKYNVKVGDYVKAGQIIGWSGSTGYSTAPHLHFQRMVNSFSNSTAQDPMPFLKSAGYGKAGGTVTPTPNTGWKTNKYGTLYKSESASFTPNTDIITRTTGPFRSMPQSGVLKAGQTIHYDEVMKQDGHVWVGYTGNSGQRIYLPVRTWNKSTNTLGVLWGTIKGRSPGSGSGSGSGSGARSGSKQLEKELKQLEKELQAIEKQLAQLQWKAQARKKKLAQLKKKLQAPGSGSRS	Lst-HDD	320	Free	Free	Linear	L	None	Derived from Lysostaphin	Antibacterial	25 min, 40 min, 1 h, 2 h, 4 h, and 6 h time points in the group that received Lst-HDD	1 mg/ml	3.1 ± 0.6	Rats plasma protease	Sandwich ELISA	Rats plasma	In Vivo	None	None	MIC of Lst-HDD is 32 times higher than the MIC of lysostaphin in S. aureus ATCC 29,213 in —0.1 µg/mL
5412	31040673	2019	IVRRADRAAVPGGGGGNQWFI	ES2-AF	21	Free	VEGFR1-selective hexapeptide (GNQWFI, AF) ,amidation	Linear	L	FITC labeled	Synthetic	Antiangiogenic	Blood samples were collected through the fundus venous plexus, 0.5–24 hours after administration	20 mg/kg	2.34 ± 0.43	Mice plasma protease	Fluorescence spectrometry	Mice plasma	In Vivo	None	None	The inhibitory rates of ES2-AF and CS-ES2-AF were similar (5 μg/mL–100 μg/mL), which indicated that the activity of ES2-AF was similar to CS-ES2-AF at relatively low concentrations
5419	30986342	2019	KAANNLLMAAS	P-T4-Cy5.5	11	PEGylation	Conjugated with Cy5.5	Linear	L	Diethylaminopropyl isothiocyanate (DEAP) conjugation at Lys1 side chain	Synthetic	Antitumor	N.A.	N.A.	2	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
5420	30973007	2019	QNSPNIFGQWM	GBAP	11	Free	Free	Cyclic (Ser3-Met11 bond)	L	None	Produced by Enterococcus faecalis	Antibacterial	Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, and 24 hr	0.28 mM	4	N.A.	HPLC	pH 7.2 buffer	In Vitro	None	None	EC50 (nM) = 1.15 for GBAP
5426	35520704	2019	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	32	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected	50 nmol/kg	3.9 ± 0.3	Kunming mice plasma protease	LC-MS/MS	Kunming mice plasma	In Vivo	None	None	EC50 = 0.72 ± 0.27 nM
5427	35520704	2019	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRCHGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	Di-GLP-1	62	Free	Bis-maleimide-NH2	Linear	L	None	GLP-1 analogs	Antidiabetes	At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected	50 nmol/kg	1.8 ± 0.2	Kunming mice plasma protease	LC-MS/MS	Kunming mice plasma	In Vivo	PDB id: 5VAI	None	EC50 = 0.039 ± 0.007 nM
5431	30901967	2019	EMTWEEKWEKKIEEYIKKIEEILKKSQNQQIDL	YIK	34	Free	Free	Linear	L	T639I mutation	HP23-E6-IDL analogue	Antiviral (Anti-Hiv Activity)	Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides YIK	5 mg/kg	1.3	Mice serum protease	N.A.	Mice serum	In Vivo	None	None	IC50(pM) = 784 ± 32 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of YIK against infection by HIV-1 mutants resistant to T20)
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
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
5439	30817059	2019	EAENPQAGAVELGGGLGGLQALALEGPPQ	Porcine C‐Peptide	29	Free	Free	Linear	L	None	Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide	Used as marker of insulin production	Blood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection	200 pmol/kg	92 ± 21 (Terminal Elimination Half Life)	Rats plasma protease	ELISA	Rats plasma	In Vivo	https://www.jbc.org/article/S0021-9258(19)41064-8/pdf	None	N.A.
5443	30814652	2019	ASPAAPAPASPAAPAPSAPA	Adnectin C-PAS#1(200)	20	Free	PAS#1(200)	Linear	L	None	Adnectin C analogs	Anticancer	Blood samples were taken after 5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, and 96 h	5 mg/kg	226.2	Mice plasma protease	ELISA	Mice plasma	In Vivo	None	None	Kd(1/s) =2.476E − 5
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
5464	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin6	20	R1 = PALM-Lys-Phe-Arg	Free	Linear	L	None	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	1.5	RHNEP	LC-MS	Apelin6	In Vitro	None	None	EC50(nM) = 2.6 ± 0.8
5474	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin7	20	R1 = PEG-Lys-Phe-Arg	Free	Linear	L	None	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	1.4	RhKLKB1	LC-MS	Apelin7	In Vitro	None	None	EC50(nM) = 6.3 ± 1.0
5475	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin8	20	R1 = PALM-Lys-Phe-Arg	Free	Linear	L	R2= Me, Methylation at Gln8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	2.1	RhKLKB1	LC-MS	Apelin8	In Vitro	None	None	EC50(nM) = 11.3 ± 2.1
5476	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin9	20	R1 = PEG-Lys-Phe-Arg	Free	Linear	L	R2= Me, Methylation at Gln8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	2.9	RhKLKB1	LC-MS	Apelin9	In Vitro	None	None	EC50(nM) = 2.5 ± 1.5
5479	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin3	20	R1 = NH2-Lys-Phe-Arg	Free	Linear	L	R2=Me, Methylation at Glu8	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	1.2	hplasma protease	LC-MS	hplasma	In Vitro	None	None	EC50(nM) = 4.9 ± 1.0
5482	30690406	2019	KFRKFRRQRPRLSHKGPMPF	Apelin6	20	R1 = PALM-Lys-Phe-Arg	Free	Linear	L	None	Apelin analogs	Blood Pressure lowering agents	37 C for up to 72 h	N.A.	4.5	hplasma protease	LC-MS	hplasma	In Vitro	None	None	EC50(nM) = 2.6 ± 0.8
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)
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)
5516	30605634	2019	pGlu-RPRLSHKGPMPF	(Pyr)1-apelin-13	13	pGlu = Pyroglutamate	Free	Linear	L	None	Apelin analogs	Hemodynamic Effects In Humans	N.A.	10 mg/kg	3.6	Dogs plasma protease	LC-MS/MS	Dogs plasma	In Vivo	None	None	N.A.
5518	30600870	2019	VEPNCDIHVKWECFERLYal	cot-biPEPEDB-VEGF	20	Acetylation	Amidation	Cyclic (C5-C13 Disulfide Bond In pepVEGF)	Mix	Lys10 linked with (OEG-Cotinine-OEG-SSSPIQGSWTWENGKWTWKGIIRLEQ-NH2), D-alanine	Synthetic	Antitumor	N.A.	200nM	1.18 (Clearance Half Life)	Mice serum protease	ELISA	Mice serum	In Vivo	None	None	tumor growth inhibition was not significantly different between cot-biPEPEDB-VEGF and PBS control groups, despite a trend toward greater inhibition in the cot-biPEPEDB-VEGF group
5527	30521347	2019	SSSPIQGSWTWENGKWTWKGIIRLEQ	cot-APTEDB-SN38	26	Free	Free	Cyclic (2 Trp-Trp Bond)	L	Lys15 linked with (Cot-Mal-PEG4-Ala-SN38)	Linker is Mal-PEG4	Anticancer	Those mice were sacrificed at 0.08, 0.5, 1, 3, 6, 12, 24, and 48 h post injection	1 mg/kg	1.36	ICR mice plasma protease	HPLC	ICR mice plasma	In Vivo	https://sci-hub.st/10.1016/j.jconrel.2012.08.029	None	HC[cot-APTEDB−SN38/Abcot] at an SN38/kg dose-equivalent of 2 mg effectively suppressed tumor growth and showed much greater antitumor activity (49.8% inhibition) than both cotAPTEDB-SN38 alone (23.9% inhibition) and CPT-11 (10.6% inhibition)
5528	30517073	2019	QDSTSDLIPAPPLSKVPLQQNFQDNQFHGKWYVVGVAGNGFLREDKDPIKMAATIYELKEDKSYNVTFNKFPMKKCQYNTDTLVPGSQPGEFTLGNIKSEPGYTSWLVRVVSTNYNQHAMVFFKAVQQNREDFFITLYGRTKELTSELKENFIRFSKSLGLPENHIVFPVPIDQCIDG	D6.2	178	Free	Free	Linear	L	V69M/I80T/F83L mutation in D6.1	LCN-2 derivative	Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications	25°C	256 nM	1.5	N.A.	Surface Plasmon Resonance (SPR)	PBS	In Vitro	Uniprot id: P80188	None	KD(pM) = 790
5529	30517073	2019	QDSTSDLIPAPPLSKVPLQQNFQDNQFHGKWYVVGVAGNGFLREDMDPIKMAATIYELKEDKSYNVTFMKFPMKXCQYNTDTLVPGSQPGEFTLGNIKSEPGYTSWLVRVVSTNYNQHAMVFFIAVQQNREDFFITLYGRTIELTSELKENFIRFSKSLGLPENHIVFPVPIDQCIDG	EI.1	178	Free	Free	Linear	L	K46M/K75X/N79M/ K142I mutations on D6.2	LCN-2 derivative	Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications	25°C	256 nM	3.1	N.A.	Surface Plasmon Resonance (SPR)	PBS	In Vitro	Uniprot id: P80188	None	KD(pM) = 829
5530	30517073	2019	QDSTSDLIPAPPLSKVPLQQNFQDNQFHGEWYVVGVAGNGFLREDKDPIKMAATIYELKEDKSYNVTFMKFPMKKCQYNTDTLVPGSQPGEFILGNIKSEPGYTSWLVRVVSTNYNQHAMVFFKAVQQNREDFFITLYGRTKELTSELKENFIRFSKSLGLPENHIVFPVPIDQCIDG	EI.3	178	Free	Free	Linear	L	K30E/I41F/X75K/T135I/I142K mutation on El.1	LCN-2 derivative	Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications	25°C	256 nM	3.4	N.A.	Surface Plasmon Resonance (SPR)	PBS	In Vitro	Uniprot id: P80188	None	KD(pM) = 548
5535	30504081	2019	(VPGAG)80	VPGAG80	400	A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488	Free	Linear	L	X1 =G , X2= A	Zwitterionic polypeptide derivative	Intrinsically disordered zwitterionic polypeptides for drug delivery	10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein	300 μM	5.0 ± 0.1	N.A.	N.A.	N.A.	In Vitro	None	None	EC50 = 10 nM for GLP1-VPGAG160
5540	30504081	2019	(VPGAG)120	VPGAG120	600	A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488	Free	Linear	L	X1 =G , X2= A	Zwitterionic polypeptide derivative	Intrinsically disordered zwitterionic polypeptides for drug delivery	10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein	300 μM	4.5 ± 0.2	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	EC50 = 10 nM for GLP1-VPGAG160
5552	30165247	2019	MAPTSAFLTALVLLSCNAICSLGCDLPQTHSLAHTRALRLLAQMRRISPFSCLDHRRDFGSPHEAFGGNQVQKAQAMALVHEMLQQTFQLFSTEGSAAAWNESLLHQFCTGLDQQLRDLEACVMQEAGLEGTPLLEEDSILAVRKYFHRLTLYLQEKSYSPCAWEIVRAEVMRSFSSSRNLQDRLRKKE	PoIFN-α	189	Free	Free	Linear	L	None	Porcine IFN-α	Antiviral And Immune Regulatory Effects	Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection	2.5 mg/kg	4.02 ± 0.06	Rats serum protease	ELISA	Rats serum	In Vivo	None	None	On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard
5636	30496575	2018	GPVPTSKPTTTKGGCHIGRFKSLSPQELASFKKARDALEESLKLKNWSCSSPVFPGNWDLRLLQVRERPVALEAELALTLKVLEAAAGPALEDVLDQPLHTLHHILSQLQACIQPQPTAGPRPRGRLHHWLHRLQEAPKKESAGCLEASVTFNLFRLLTRDLKYVADGNLCLRTSTHPEST	rhIFN-λ1	181	Free	Human chorionic gonadotropin β subunit carboxyl-terminal peptide (CTP) and an N-glycosylation sequence linked to its C-terminus	Linear	L	None	Recombinant human interferon-λ1	Antiviral, Antiproliferation, And Nk Cell Cytotoxicity-Promoting Activities	Venous blood was collected at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h post-injection	40 μg/kg	3.37 ± 0.70	Mice blood protease	ELISA	Mice blood sample	In Vivo	None	None	Antiviral activity of the purified rhIFN-λ1 expressed by CHO cells was 2.5 × 105 IU/mg
5639	30411073	2018	MVRIKPGSANKPSDD	sPIF	15	Free	Free	Linear	L	None	Human embryo‐derived peptide analogs	Treatment Of Autoimmune Hepatitis	Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8	0.5 mg/kg	63	Human serum protease	LC-MS	Human serum	In Vivo	None	None	N.A.
5640	30411073	2018	MVRIKPGSANKPSDD	sPIF	15	Free	Free	Linear	L	None	Human embryo‐derived peptide analogs	Treatment Of Autoimmune Hepatitis	Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8	1 mg/kg	109	Human serum protease	LC-MS	Human serum	In Vivo	None	None	N.A.
5641	30407790	2018	EEGYHWYGYTPQNVI	GENP-Gem-Ola	12	C18-EEG	Amidation	Linear	L	None	Synthetic	Treat Pancreatic Cancer With Breast Cancer 2 (Brca2) Mutation	Blood samples were collected at 0.5, 1, 2, 3, 5, 8, 12, and 24 h postinjection	equivalent concentrations of Gem (5 mg/kg) and Ola (50 mg/kg)	4	Mice plasma protease	HPLC	Mice plasma	In Vivo	None	None	Tumors from the GENP-Gem-Ola group showed extensive apoptosis (51% c-caspase-3 positive)
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
5647	30309736	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	Exendin-4	Antidiabetes	Blood samples were collected at 0, 0.25, 0.5, 0.75, 1, 2, 4, 6,8, and 12 h after injection	100 nmoL/kg	1.7 ± 0.3	SD rats serum protease	ELISA	SD rats serum	In Vivo	PDB id: 7MLL	None	EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold
5655	30170067	2018	IVRRADRAAVPIVRRADRAAVPGGGGGGNQWFI	ES2-AF	33	ES2	Free	Linear	L	None	Synthetic	Treatment of diseases caused by Diabetic Eye Disease, Rheumatoid Arthritis And Other Neo-Vascularization, Anti-Angiogenesis Activity	Blood samples were collected through the jugular vein at 5 min, 15 min, 30 min, 1 h, 2 h, 6 h, 12 h, 24 h, and 48 h after administration	25 mg/kg	2.785	Wistar rats plasma protease	Fluorescence spectrometry	Wistar rats plasma	In Vivo	None	None	KD (mol· L−1) = 3.011 × 10−4
5660	30096651	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	31	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	At 1, 2, 3, 4, 6, 12, 24 and 48 h after injection, three Kunming mice were sacrificed at each time point and blood samples (~200 mL) were collected through extracting eyeball	50 nmol/kg	3.6 ± 0.2	Kunming mice plasma protease	LC-MS/MS	Kunming mice plasma	In Vivo	None	None	the potency of 6 was 5.2 times higher than liraglutide
5661	30096651	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	31	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	Blood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin	50 nmol/kg	4.2 ± 0.3	SD rats plasma protease	LC-MS/MS	SD rats plasma	In Vivo	None	None	the potency of 6 was 5.2 times higher than liraglutide
5667	30041153	2018	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	HI	51	Free	Free	Cyclic (3 S-S Bond)	L	None	Synthetic	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	> 4	Rats SCT protease	LC-HRMS	1 mg/ml rats SCT protein	In Vitro	https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1	None	N.A.
5668	30041153	2018	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	HI	51	Free	Free	Cyclic (3 S-S Bond)	L	None	Synthetic	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	3.43	Rats SCT protease	LC-HRMS	2 mg/ml rats SCT protein	In Vitro	https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1	None	N.A.
5670	30041153	2018	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	HI	51	Free	Free	Cyclic (3 S-S Bond)	L	None	Synthetic	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	50 µM	> 4	Rats SCT protease	LC-HRMS	1 mg/ml rats SCT protein	In Vitro	https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1	None	N.A.
5671	30041153	2018	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	HI	51	Free	Free	Cyclic (3 S-S Bond)	L	None	Synthetic	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	50 µM	> 4	Rats SCT protease	LC-HRMS	2 mg/ml rats SCT protein	In Vitro	https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1	None	N.A.
5672	30041153	2018	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	HI	51	Free	Free	Cyclic (3 S-S Bond)	L	None	Synthetic	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	50 µM	> 4	Rats SCT protease	LC-HRMS	4 mg/ml rats SCT protein	In Vitro	https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1	None	N.A.
5673	30041153	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	Human SCT protease	LC-HRMS	1 mg/ml human SCT protein	In Vitro	PDB id: 7MLL	None	N.A.
5675	30041153	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	31	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	Human SCT protease	LC-HRMS	1 mg/ml human SCT protein	In Vitro	None	None	N.A.
5676	30041153	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	3	Human SCT protease	LC-HRMS	1 mg/ml human SCT protein	In Vitro	None	None	N.A.
5677	30041153	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	SD rats SCT protease	LC-HRMS	1 mg/ml SD rats SCT protein	In Vitro	PDB id: 7MLL	None	N.A.
5679	30041153	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	31	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	SD rats SCT protease	LC-HRMS	1 mg/ml SD rats SCT protein	In Vitro	None	None	N.A.
5681	30041153	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	Göttingen minipigs SCT protease	LC-HRMS	1 mg/ml göttingen minipigs SCT protein	In Vitro	PDB id: 7MLL	None	N.A.
5683	30041153	2018	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG	Liraglutide	31	Free	Free	Linear	L	Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu	GLP-1 analogs	Antidiabetes	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	Göttingen minipigs SCT protease	LC-HRMS	1 mg/ml göttingen minipigs SCT protein	In Vitro	None	None	N.A.
5684	30041153	2018	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG	Semaglutide	31	Free	Free	Linear	L	Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)	GLP-1 analogs	Attenuates Renal Fibrosis	At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture	10 µM	>4	Göttingen minipigs SCT protease	LC-HRMS	1 mg/ml göttingen minipigs SCT protein	In Vitro	None	None	N.A.
5699	29958697	2018	TLQPPASSRRRHFHHALPPAR	125I-TLQP-21	21	125I labelled	Free	Linear	L	None	Derived from the proteolytic cleavage of the 617-aa VGF	Isoproterenol stimulated lipolysis	At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL)	1 mM	110 (T1/2 Terminal Phase)	Rats plasma protease	LC-MS	Rats plasma	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.
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.
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.
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.
5738	29738954	2018	FGRKKRRQRRR	CtrlTat	11	Acetylation	Amidation	Linear	L	None	Derived from the human immunodeficiency virus 1 (HIV-1) tat protein	Antibacterial and Anti-Tb	N.A.	10 mM	4	Trypsin	RP-HPLC	Tris-EDTA buffer	In Vitro	None	None	MIC (micromolar) = 6.27 ± 0.05 for E.coli
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
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
5754	29673717	2018	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points	1000 ng/mL	3.6	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	PDB id: 7MLL	None	EC50 (pM) = 1.8 ± 0.8
5763	29669811	2018	MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK-GGGGS-125I-MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK	125I-3E8.G4S dimer	561	125I labelled	Free	Linear	L	125I-labeled, 2 ScFv joined by G4S linker	Derived from the 3E8 antibody	Optimizes biophysical properties, serum half-life and high-specificity tumor imaging	Blood samples (5 μl) were drawn from the saphenous vein by puncture, using a 30-gauge syringe needle, at 0.5, 1, 5, 24, 48, and 72 h postinjection for 3E8.G4S	5 μCi	2	Mice blood protease	Radioiodination assay	Mice blood sample	In Vivo	None	None	KD of 3.6 nM for 3E8.G4S
5764	29669811	2018	MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK-GGGGS-125I-MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK-GGGGS-125I-MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK	125I-3E8.G4S oligomer (Trimeric)	844	125I labelled	Free	Linear	L	125I-labeled, 3 ScFv joined by G4S linker	Derived from the 3E8 antibody	Optimizes biophysical properties, serum half-life and high-specificity tumor imaging	0.5, 1.5, 3, 6, 24, 48, and 72 h	5 μCi	3.3	Mice blood protease	Radioiodination assay	Mice blood sample	In Vivo	None	None	KD of 3.6 nM for 3E8.G4S
5765	29669811	2018	MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK-GGGGS-125I-MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK-GGGGS-125I-MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK-GGGGS-125I-MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK	125I-3E8.G4S oligomer (Tetrameric)	1127	125I labelled	Free	Linear	L	125I-labeled, 4 ScFv joined by G4S linker	Derived from the 3E8 antibody	Optimizes biophysical properties, serum half-life and high-specificity tumor imaging	0.5, 1.5, 3, 6, 24, 48, and 72 h	5 μCi	3.3	Mice blood protease	Radioiodination assay	Mice blood sample	In Vivo	None	None	KD of 3.6 nM for 3E8.G4S
5789	29540315	2018	HGDGSFTSELSTYKDALAARDFIAWLIQTKITD	GUB09-145	34	Free	Amidation	Linear	L	Lipidation at Lys14 (C16-yE-)	GUB09-123 analogue	GLP-1/GLP-2 co-agonist	Blood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point)	800nmol/kg	2.7	Mice plasma protease	LC-MS/MS	Mice plasma	In Vivo	None	None	GLP-1R, EC50 (nM) = 0.17
5799	29528634	2018	HGDGSFSDEMNTILDNCAARDFICWLIQTKITDPSSGAPPPS	GLP-2 analog 8	42	Free	Amidation	Cyclic (C17-C24 Stapled Using Linker L3)	L	None	GLP-2 analogues	Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models	Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h)	10 nmol/kg	2.7	Mice plasma protease	In vitro cell based activity assay	Mice plasma	In Vivo	None	None	EC50(nM) = 0.068 ± 0.003
5800	29528634	2018	HGDGSFSDCMNTILDCLAARDFINWLIQTKITDPSSGAPPPS	GLP-2 analog 9	42	Free	Amidation	Cyclic (C9-C16 Stapled Using Linker L3)	L	None	GLP-2 analogues	Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models	Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h)	10 nmol/kg	3.1	Mice plasma protease	In vitro cell based activity assay	Mice plasma	In Vivo	None	None	EC50(nM) = 0.041 ± 0.005
5801	29528634	2018	HGDGSFSDEMCTILDNLCARDFINWLIQTKITDPSSGAPPPS	GLP-2 analog 10	42	Free	Amidation	Cyclic (C11-C18 Stapled Using Linker L3)	L	None	GLP-2 analogues	Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models	Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h)	10 nmol/kg	4.7	Mice plasma protease	In vitro cell based activity assay	Mice plasma	In Vivo	None	None	EC50(nM) = 0.028 ± 0.002
5802	29517911	2018	CNTWNPWCPWDAPLCA-(Sar)3-rr	1b	18	Replaced the Nterminal Ala with an acetyl group	Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues	Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene)	Mix	None	1a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	Serial blood samples were taken from each animal via temporary indwelling tail vein cannulae at 5, 10, 20, 30, 60, 120, 180, and 240 min postdose,	5 mg/kg	78	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats
5812	29517911	2018	CSWPARCLHQDLC	2b	13	Free	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	None	2a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	24 h at 37 °C	0.16 mM	1.5	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vitro	None	None	Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats
5815	29517911	2018	CSWPARCLHQDLC	2b	13	Free	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	None	2a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	24 h at 37 °C	0.16 mM	2.8	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	None	None	Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats
5820	29464007	2018	QWECPYGLCWIQ	99mTc-F1A	18	99mTc-HHEDEG	Free	Cyclic (C-C Disulfide Bond In C Terminal)	L	Interconnected through a diethylene glycol (DEG) spacer	Fibrin-specific natural peptide analogue	99MTC-F4A is a high-avidity prototype probe for characterizing thrombus in Lvads	Serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter	N.A.	124.7 ± 41.3 (T1/2b Elimination Half Life)	Mice plasma protease	Radioactivity assay	Mice plasma	In Vivo	None	None	99mTc-F4A probe was not displaced by F1A
5821	29464007	2018	QWECPYGLCWIQ	99mTc-F1A	18	99mTc-HHEDEG	Free	Cyclic (C-C Disulfide Bond In C Terminal)	L	Interconnected through a diethylene glycol (DEG) spacer	Fibrin-specific natural peptide analogue	99MTC-F4A is a high-avidity prototype probe for characterizing thrombus in Lvads	Serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter	N.A.	174.2 ± 26.2 (T1/2b Elimination Half Life)	Mice plasma protease	Radioactivity assay	Mice plasma	In Vivo	None	None	Kd ~10.2 µM for 99mTc-F1A (bound to uniform fibrin clots in PBS)
5823	29461833	2018	Rx-PRL-X-HKGP-Nle-PF	Pyr analogue 3	13	pGlu = Pyroglutamate	Free	Cyclic (Rx2-X6 Bond)	L	X= allylglycine, Rx=Na-ally-arginine, Nle = Nor-leucine	Pyr-13 analogue	Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock	At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).	1 mM	2.2 ± 0.3	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Ki binding (nM) = 4.5 ±1.4 for 3
5825	29461833	2018	R-X-RLS-X-KGP-Nle-PF	Pyr analogue 5	13	pGlu = Pyroglutamate	Free	Cyclic (X3-X7 Bond)	L	X= allylglycine, Nle = Nor-leucine	Pyr-13 analogue	Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock	At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).	1 mM	3.9 ± 0.6	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Ki binding (nM) = 3 ±0.1 for 5
5828	29461833	2018	RPR-X-SHK-X-P-Nle-PF	Pyr analogue 8	13	pGlu = Pyroglutamate	Free	Cyclic (X5-X9 Bond)	L	X= allylglycine, Nle = Nor-leucine	Pyr-13 analogue	Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock	At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).	1 mM	3.5 ± 0.8	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Ki binding (nM) = 3.9 ±1.4 for 8L
5830	29461833	2018	RPRL-X-HKG-X-Nle-PF	Pyr analogue 10	13	pGlu = Pyroglutamate	Free	Cyclic (X6-X10 Bond)	L	X= allylglycine, Nle = Nor-leucine	Pyr-13 analogue	Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock	At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).	1 mM	4.1 ±0.8	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Ki binding (nM) = 194 ±70 for 10L
5832	29461833	2018	RPRLSH-X-GP-Nle-X-F	Pyr analogue 12	13	pGlu = Pyroglutamate	Free	Cyclic (X8-X12 Bond)	L	X= allylglycine, Nle = Nor-leucine	Pyr-13 analogue	Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock	At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).	1 mM	4.6 ±0.7	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Ki binding (nM) = 14 ±7 for 12
5838	29436835	2018	(hpcdypewqwlcelGk)3	Palm-PIE12-trimer	48	Palm-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	5 min to 24 h	1.2 mg/kg	1.8	Rats plasma protease	LC-MS/MS using an Agilent HPLC	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.54 ± 0.029 (antiviral potency)
5839	29436835	2018	(hpcdypewqwlcelGk)3	Palm-PIE12-trimer	48	Palm-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	15 min to 48 h	1.2 mg/kg	2.2	Rats plasma protease	LC-MS/MS using an Agilent HPLC	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.54 ± 0.029 (antiviral potency)
5841	29436835	2018	(hpcdypewqwlcelGk)3	C16-PIE12-trimer	48	C16-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	15 min to 48 h	1 mg/kg	1.2	Rats plasma protease	LC-MS/MS using an Agilent HPLC	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.11 ± 0.012 (antiviral potency)
5842	29436835	2018	(hpcdypewqwlcelGk)3	C18-PIE12-trimer	48	C18-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	5 min to 24 h	1 mg/kg	1.1	Rats plasma protease	LC-MS/MS using an Agilent HPLC	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.087 ± 0.012(antiviral potency)
5843	29436835	2018	(hpcdypewqwlcelGk)3	C18-PIE12-trimer	48	C18-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	15 min to 48 h	1 mg/kg	1.4	Rats plasma protease	LC-MS/MS using an Agilent HPLC	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.087 ± 0.012(antiviral potency)
5844	29436835	2018	(hpcdypewqwlcelGk)3	Chol-PIE12-trimer	48	Chol-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	5 min to 24 h	1 mg/kg	1.8	Rats plasma protease	UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.022 ± 0.0018 (antiviral potency)
5845	29436835	2018	(hpcdypewqwlcelGk)3	Chol-PIE12-trimer	48	Chol-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	15 min to 48 h	1 mg/kg	2.7	Rats plasma protease	UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.022 ± 0.0018 (antiviral potency)
5846	29436835	2018	(hpcdypewqwlcelGk)3	Chol-PIE12-trimer	48	Chol-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	5 min to 24 h	1 mg/kg	1.6	Rats plasma protease	UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.022 ± 0.0018 (antiviral potency)
5847	29436835	2018	(hpcdypewqwlcelGk)3	Chol-PIE12-trimer	48	Chol-Maleimide joined by linker PEG24	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	15 min to 48 h	1 mg/kg	3.9	Rats plasma protease	UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.022 ± 0.0018 (antiviral potency)
5850	29436835	2018	(hpcdypewqwlcelGk)3	CPT31	48	Chol-Maleimide joined by linker PEG31	Free	Linear	Mix	All D-amino acids except Gly	Synthetic	Antiviral (HIV Entry Inhibitor)	5 min to 24 h	1 mg/kg	3.3	Rats plasma protease	Ultra-High Performance Liquid Chromatography (UHPLC)	Rats plasma	In Vivo	None	None	JRFL(nM) = 0.015 ± 0.0062 (antiviral potency)
5854	29433929	2018	LEKLAAENKEQWEQAARILEEIKKTYREIEDRWDCWTM	CT105	38	Amidation	Acetylation	Linear	L	None	Synthetic	Antiviral (against HIV Virus)	Serial blood samples were collected from each animal before injection and at 0.08, 0.25, 0.5, 1, 2, 4 and 8 h after injection	6 mg/kg	2.7	Rats plasma protease	IC-ELISA	Rats plasma	In Vivo	None	None	IC50(nM) =0.26 against HIV variant R3A
5855	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	Day 1 (cycle 1 - 28days)	6 mg/m2	2.3	Human plasma protease	ELISA	Human plasma	In Vivo	https://www.lens.org/lens/patent/124-764-042-412-641/fulltext?l=en	None	N.A.
5856	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 1 (cycle 1 - 28days)	12 mg/m2	2.1	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5857	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 1 (cycle 1 - 28days)	24 mg/m2	3.2	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5858	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 1 (cycle 1 - 28days)	48 mg/m2	4.9	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5860	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 29 (Cycle 2 day1)	6 mg/m2	2.8	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5861	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 29 (Cycle 2 day1)	12 mg/m2	2	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5862	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 29 (Cycle 2 day1)	24 mg/m2	3.7	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5863	29423221	2018	wwtfflpstlwerk	dTCApFs	14	Free	Free	Linear	D	None	Synthetic	Anticancer	day 29 (Cycle 2 day1)	48 mg/m2	4.6	Human plasma protease	N.A.	Human plasma	In Vivo	None	None	N.A.
5871	29421564	2018	RPKPQQFFGLM	SP	11	Free	Free	Linear	L	None	Synthetic	Therapeutic Regeneration By Facilitating Mobilization Of Endogenous Stem Cells From Bone Marrow To The Injured Sites	0 to 72 h at 37°C	5 nmol	5	Diabetic rats serum protease	ELISA	Diabetic rats serum	In Vitro	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.
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
5886	29141139	2018	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	ApoA-I mimetic peptide	Treatment of Cardiovascular Diseases	At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing	20 mg/mL	4.588	Rats serum protease	LC-MS	Rats serum after 50 mg/kg sHDL	In Vivo	None	None	N.A.
5887	29141139	2018	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	ApoA-I mimetic peptide	Treatment of Cardiovascular Diseases	At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing	20 mg/mL	4.25	Rats serum protease	LC-MS	Rats serum after 2.5 mg/kg sHDL-PEG2k	In Vivo	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
5904	N.A.	2018	(GIVEQCCTSICSLYQLENYCN-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTDK-OH)	Prior Art analogue 2	50	Free	B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A and B chain linked with disulfide bond,B28D,modifications	Insulin Derivative	Treatment of Hypoglycaemia	Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1 nmol/kg	121	Pig plasma protease	ELISA	Pig plasma	In Vivo	None	US 201615754342 A	N.A.
5905	N.A.	2018	(GIVEQCCTSICSLYQLENYCN-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTDK)	Prior Art analogue 2	50	Free	B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications	Cyclic (C7-C12 disulfide bond in A chain)	L	A and B chain linked with disulfide bond,B28D, modifcations	Insulin Derivative	Treatment of Hypoglycaemia	Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes	1 nmol/kg	159	Pig plasma protease	ELISA	Pig plasma	In Vivo	None	US 201615754342 A	N.A.
5913	N.A.	2018	(GIVEQCCTSICSLYQLENYCA-OH)-(FVEQHLCGSHLVEALYLVCGERGFFYPK)	Example 15	49	Free	B29K(N(Eps)Hexadecanedioyl-gGlu-2×OEG), desB30 modifications	cyclic (C7-C12 disulfide bond in A chain)	L	A and B chain linked with disulfide bond,A21A, B3E, desB27, modificaitons	Insulin Derivative	Treatment Of Hypoglycaemia	Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing	25 nmol/kg	67	SD rats plasma protease	ELISA	SD rats plasma with Zinc Ion	In Vivo	None	US 201615754342 A	Lipogenesis 1% HSA (%rel to HI) = 1.8
5915	N.A.	2018	(GIVEQCCTSICSLYQLENYCN-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK)	Prior Art analogue 7	50	Free	B29K(N(Eps)Hexadecanedioyl-gGlu), desB30 modifications	cyclic (C7-C12 disulfide bond in A chain)	L	A and B chain linked with disulfide bond,modifications	Insulin Derivative	Treatment Of Hypoglycaemia	Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing	25 nmol/kg	200	SD rats plasma protease	ELISA	SD rats plasma with 3 Zinc Ion Per Hexamer	In Vivo	None	US 201615754342 A	N.A.
5930	29029327	2017	TGFHHVAQAALKLLSSSNPPTKASQSARITD	Alu-HCG	31	Free	HCG	Linear	L	None	Derived from the exonization of an Alu-J element in the glycoprotein hormone alpha (GPHA) gene	Role in Placental development	N.A.	2 mg/ml	82.3	Rats serum protease	ELISA	Rats serum	In Vivo	None	None	N.A.
5931	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	rE-4	39	Free	Deamidation at C terminal	Linear	L	None	Exendin-4 analogs	GLP-1R agonist	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1	5 µg	1.8	Human plasma protease	ELISA	Human plasma	In Vivo	None	None	N.A.
5932	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	Synthetic	Antidiabetes	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1	5 µg	1.6	Human plasma protease	ELISA	Human plasma	In Vivo	PDB id: 7MLL	None	N.A.
5933	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	rE-4	39	Free	Deamidation at C terminal	Linear	L	None	Exendin-4 analogs	GLP-1R agonist	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1	5 µg	1.8	Human plasma protease	ELISA	Human plasma with Metformin	In Vivo	None	None	N.A.
5934	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	rE-4	39	Free	Deamidation at C terminal	Linear	L	None	Exendin-4 analogs	GLP-1R agonist	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8	5 µg	1.9	Human plasma protease	ELISA	Human plasma	In Vivo	None	None	N.A.
5935	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	Synthetic	Antidiabetes	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8	5 µg	1.3	Human plasma protease	ELISA	Human plasma	In Vivo	PDB id: 7MLL	None	N.A.
5936	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	rE-4	39	Free	Deamidation at C terminal	Linear	L	None	Exendin-4 analogs	GLP-1R agonist	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8	5 µg	1.9	Human plasma protease	ELISA	Human plasma with Metformin	In Vivo	None	None	N.A.
5937	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	rE-4	39	Free	Deamidation at C terminal	Linear	L	None	Exendin-4 analogs	GLP-1R agonist	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84	10 µg	1.6	Human plasma protease	ELISA	Human plasma	In Vivo	None	None	N.A.
5938	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	Synthetic	Antidiabetes	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84	10 µg	1.8	Human plasma protease	ELISA	Human plasma	In Vivo	PDB id: 7MLL	None	N.A.
5939	28932995	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	rE-4	39	Free	Deamidation at C terminal	Linear	L	None	Exendin-4 analogs	GLP-1R agonist	Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84	10 µg	1.3	Human plasma protease	ELISA	Human plasma	In Vivo	None	None	N.A.
5951	28821462	2017	MTTASTSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIQKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLGDSDNES	wtFN	183	Free	Free	Linear	L	Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages	Synthetic	Antitumor	N.A.	50 mg/kg	1.1 ± 0.1	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	PDB id: 1FHA	None	N.A.
5952	28821462	2017	MTTASTSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIQKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLGDSDNESGSSGGSGSSGGSGGGDEADGSRGSQKAGVDE	LCFN36	183	Free	Fusing the XTEN peptide of 36 amino acids through a linker	Linear	L	Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages	wtFN derivative	Antitumor	N.A.	50 mg/kg	3.5 ± 0.3	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	None	None	N.A.
5962	28771355	2017	HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG	GLP-1 analogue 6	31	Free	Diflunisal is linked to the GLP-1 peptide through its hydroxyl group	Linear	L	K34R substituition at GLP-1, at Lys20 indomethacin is linked through a γGlu residue-Lys, DIF=diflunisal, Dehydroxylation of DIF	GLP-1 analogs	Antidiabetes	Blood sampled at eight time-points within 24 h	5 mL/kg	299	Lean mice plasma protease	Luminescent Oxygen Channeling Immunoassay	Lean mice plasma	In Vivo	None	None	GLP-1R EC50 ± SEM (nM) = 0.547 ± 0.211
5970	28721592	2017	MAGPATQSPMKLMALQLLLWHSALWTVQEATPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWAPLSSCPSQALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQQMEELGMAPALQPTQGAMPAFASAFQRRAGGVLVASHLQSFLEVSYRVLRHLAQP	G-CSF	204	Met addition at N terminal of G-CSF	Free	Linear	L	None	Human derived	Selectively stimulate proliferation	Blood samples were drawn from the rats at selected time points (0, 3, 6, 12, 18, and 24 h after injection)	150 μg/kg	1.2	Rats serum protease	ELISA	Rats serum	In Vivo	Genbank accession no. NM_172219	None	in vitro activity of GCSF-La reached 48% of that of the G-CSF monomer
5973	28714475	2017	EYEKEYEACRWPARCVHQDLCG	tagPK128	22	tag	Free	Bicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128)	L	Lys4 linked with Palm fatty acid	Synthetic	Inhibit plasma kallikrein	N.A.	0.5 mg/kg	2.9 ± 0.7 (T1/2b)	Rats plasma protease	RP-HPLC using a fluorescence detector	Rats plasma	In Vivo	None	None	Albumin binding (Kd) (nM) = 720±90 for rat albumin
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
5987	28668697	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin-4	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h	50 nmol	2.35 ± 0.23 (Elimination Half Life)	SD rats plasma protease	LC-MS/MS	SD rats plasma	In Vivo	None	None	EC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation)
5988	28668697	2017	HGEGTYTNDVTEYLEE-X2-AAKEFIEWLIKGK	7b	29	Free	Free	Linear	L	X2 = Structure given in paper, n= 40	Derived from Xenopus GLP-1	Antidiabetes	Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h	50 nmol	2.78 ± 0.14 (Elimination Half Life)	SD rats plasma protease	LC-MS/MS	SD rats plasma	In Vivo	None	None	EC50 (nM) = 1.4 ± 0.2 for peptide 7 (potency on the cloned human GLP-1 receptor)
6009	28522195	2017	HGDGSFSDEMNTILDNLAARDFINWLIQTKITD	[Gly2]GLP-2	33	Free	Free	Linear	L	Ala2 to Gly2	GLP-2 analogue	Treatment of Short Bowel Syndrome	Blood samples were collected from the tail vein at 0, 1, 2, 3, 4, 5,6, 9 and 12 h after administration	2 mg/mL	1.62 (Terminal Half Life)	Rats plasma protease	N.A.	Rats plasma	In Vivo	None	None	EC50 values of [Gly2]GLP-2 = 8.40 nM
6010	28522195	2017	HADGSFSDEMNTILDNLAARDFINWLIQTKITD	native GLP-2	33	Free	Free	Linear	L	None	Glucagon	Treatment of Short Bowel Syndrome	Blood samples were collected from the tail vein at 0, 1, 2, 3, 4, 5,6, 9 and 12 h after administration	2 mg/mL	4.59 (Terminal Half Life)	Rats plasma protease	N.A.	Rats plasma	In Vivo	None	None	EC50 values of GLP-2 = 2.58 nM
6019	28457895	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPSGSEGSEGEGGSEGSEGEGHAHFNFGSWTWENGKWTWKGIWLPAR	Exenatide-APTHSA	83	Free	C-terminal part of exenatide was connected to the N-terminal part of APTHSA using a long (18-mer) linker	Linear	L	None	Exendin-4 analogs	Antihyperglycemic	1 hour	25 nmol/kg	~1.3	ICR mice retro-orbital sinus protease	Exenatide ELISA	ICR mice retro-orbital sinus	In Vivo	PDB id: 7MLL	None	both exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity
6021	28437610	2017	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Native Ex4	39	Free	Amidation	Linear	L	None	GLP-1 analogs	Antidiabetes	N.A.	25 nmol/kg	1.9	Murine plasma protease	ELISA	Murine plasma	In Vivo	PDB id: 7MLL	None	N.A.
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
6030	28356733	2017	MHSDAVFTDQYTRLRKQLAAKKYLQSLKQKRY	DBAYL	32	Free	Free	Linear	L	None	PACAP-derived peptide	Antidiabetes	Orbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing	1 mg/kg	1.98	DB/DB mice orbital blood protease	LC-MS/MS	DB/DB mice orbital blood sample	In Vivo	None	None	EC50 of DBAYL at VPAC1 was 804 nM
6034	28323965	2017	FPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF	r-HGH	191	Free	Free	Linear	L	None	Synthetic	Treatment of GHD	Measured following 2 weeks of daily administration	0.24 mg/kg	3.5	Human serum protease	IDS-iSys chemiluminescence assay	Human serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU, https://sci-hub.se/10.1021/acs.molpharmaceut.5b00868	None	EC50 = 0.36 ± 0.06 ng/ml (Proliferation of BAFB2B2 cells)
6037	28209419	2017	HADGSFSDEMNTILDNLAARDFINWLIQTKITD	Native GLP-2	33	Free	Free	Linear	L	None	Glucagon	Treatment of Short Bowel Syndrome	N.A.	8 μg/kg	~120	Human plasma protease	GLP-2 (1–33) specific radioimmunoassay	Adult human plasma	In Vivo	PDB id: 2L63	None	N.A.
6041	28138743	2017	ILPWKWPWWPWRR	Indolicidin	13	Free	Amidation	Linear	L	None	Synthetic	Antimicrobial	A plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h)	10 μM	1.53	Mouse plasma protease	LC-HRMS.	Mouse plasma	In Vitro	None	None	N.A.
6044	28097629	2017	AGYKPDEGKRGDACEGSDGGPFV	PEG20k-Cys14-TP508	23	Free	Amidation	Linear	L	PEGylation at Cys14 through Mal-modified PEG20K, TAMRA-labeled	Synthetic	Treatment of Diabetic Foot Ulcers	N.A.	Molar equivalent of 5 mg/mL TP508	70	Male CD1 mice plasma protease	Fluorescence assay	Male CD1 mice plasma	In Vivo	None	None	N.A.
6045	28097629	2017	AGYKPDEGKRGDACEGSDGGPFV	PEG20k-TP508	23	PEG20K	Amidation	Linear	L	TAMRA-labeled	Synthetic	Treatment of Diabetic Foot Ulcers	N.A.	2.16 mM	93	Male CD1 mice plasma protease	Fluorescence assay	Male CD1 mice plasma	In Vivo	None	None	N.A.
6046	28097629	2017	AGYKPDEGKRGDACEGSDGGPFV	PEG30k-TP508	23	PEG30K	Amidation	Linear	L	TAMRA-labeled	Synthetic	Treatment of Diabetic Foot Ulcers	N.A.	Molar equivalent of 1 mg/mL TP508	258	Male CD1 mice plasma protease	Fluorescence assay	Male CD1 mice plasma	In Vivo	None	None	N.A.
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.
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.
6060	27881716	2017	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing	75 mg/kg	3.81	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	EC50 (mg /dL) = 142.81
6061	27881716	2017	PVLDLFRELLNELLEALKQKLK	22A	22	Free	Free	Linear	L	None	Synthetic	Treatment of Cardiovascular Diseases	Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing	75 mg/kg	4.43	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	EC50 (mg /dL) = 142.81
6063	27881716	2017	PVLDLFRELLNELLEALKQKLK	22A-sHDL	22	Free	sHDL	Linear	L	None	22A and sHDL fusion protein	Antiatherosclerotic	Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing	75 mg/kg	4.14	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	EC50 (mg /dL)= 47.63
6064	27881716	2017	PVLDLFRELLNELLEALKQKLK	22A-sHDL	22	Free	sHDL	Linear	L	None	22A and sHDL fusion protein	Antiatherosclerotic	Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing	150 mg/kg	2.57	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	EC50 (mg /dL) = 53.77
6065	27881716	2017	PVLDLFRELLNELLEALKQKLK	22A-sHDL	22	Free	sHDL	Linear	L	None	22A and sHDL fusion protein	Antiatherosclerotic	Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing	150 mg/kg	2.74	Rats serum protease	LC-MS	Rats serum	In Vivo	None	None	EC50 (mg /dL)= 47.63
6067	27815337	2017	RPRlS-Aib-Ka-ProNle-PF	P26	12	Acetylation	Pro(4-Br)Phe substituition	Linear	Mix	Aib, DLeu,ProNle, D-Ala	Apelin analogs	Diuretic and Cardiovascular Effects	37°C	5 μM	86	Mouse plasma protease	LC-MS	Mouse plasma	In Vitro	None	None	Recruitment of b-arrestin2 by BRET, EC50 (nM) = 138 ± 30
6072	27784692	2017	MCLPVASCGGPGVG-(VPGxG)160-VPGWPGSGGC	KTP-ELP	822	Conjugation of KTP cyclic peptide at N terminal	Free	Linear	L	x = Val,Gly or Ala	Fusion protein of KTP and ELP	Carrier protein	Whole-animal fluorescence images were collected at regular intervals for 24 hours	100 mg/kg	234.83 (T1/2,Terminal)	Rats plasma protease	whole-body fluorescence imaging	Rats plasma	In Vivo	None	None	KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours
6073	27784692	2017	MCGPGVG-(VPGxG)160-VPGWPGSG	ELP	815	Free	Free	Linear	L	x = Val,Gly or Ala	Synthetic	Carrier protein	Whole-animal fluorescence images were collected at regular intervals for 24 hours	5 mg/kg	90.3 (T1/2,Terminal)	Swine plasma protease	whole-body fluorescence imaging	Swine plasma	In Vivo	None	None	KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours
6074	27784692	2017	MCLPVASCGGPGVG-(VPGxG)160-VPGWPGSGGC	KTP-ELP	822	Conjugation of KTP cyclic peptide at N terminal	Free	Linear	L	x = Val,Gly or Ala	Fusion protein of KTP and ELP	Carrier protein	Whole-animal fluorescence images were collected at regular intervals for 24 hours	5 mg/kg	118.6 (T1/2,Terminal)	Swine plasma protease	whole-body fluorescence imaging	Swine plasma	In Vivo	None	None	KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours
6103	27804918	2016	SSSPIQGSWTWENGKWTWKGIIRLEQ	APTEDB–SN38	26	Free	Free	Cyclic (2 Trp-Trp Bond)	L	Ala-modified SN38 (Cys-Mal-PEG4-Ala-SN38) linked with Cys-modified APT EDB through Lys15	Linker is Mal-PEG4	Anticancer	At different times (0.08, 0.5, 1, 3, 6, 12 h) after injection	1 mg/kg	1.77	Mice plasma protease	HPLC	Mice plasma	In Vivo	https://sci-hub.st/10.1016/j.jconrel.2012.08.029	None	IC50 = 472.6 nM
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
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
6116	27558296	2016	QRPRLSHKKP-Nle-Aib-F	Compound 31	13	Palmitic acid conjugation	Free	Linear	L	Gly9 was exchanged with Lys, TAMRA = 5,6-carboxytetramethylrhodamine at Lys9 modification at Lysine , Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12	compound 31 analogues	Inotropic Agent	37 C	0.00001 M	~4	Porcine liver homogenate protease	HPLC using a fluorescence detector	Porcine liver homogenate	In Vitro	None	None	EC50(nM) = 21.6 ± 4.5 for compound 31
6118	27393654	2016	CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE	IFN-α	165	Free	Free	Linear	L	None	Human derived	Antiproliferative, Immunoregulatory and Antiviral	At desired time points (1, 5, 15, 30 min, 1, 3, 6, 24,48, 72 and 96 h)	1 mg IFN-α equivalent/kg	1.49 (T1/2b-Terminal Half Life)	Mice plasma protease	ELISA	Mice plasma	In Vivo	PDB id: 1ITF	None	IC50 = 10.77 pg/mL
6122	27243004	2016	OWOWORPVYOPRPRPPHPRL	Api793	20	Gu: N,N,N',N' tetramethylguanidino	Free	Linear	L	O = L-ornithine, (WO)2 repititive motifs substituited	Analogs of Api137	Antimicrobial	After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v)	70 mg/L	246	Mouse serum protease	N.A.	Mouse serum	In Vitro	None	None	IC50(g/L) = 0.64 ± 0.05 in HEK293
6125	27243004	2016	OIOIOIORPVYOPRPRPPHPRL	Api796	22	Gu: N,N,N',N' tetramethylguanidino	Free	Linear	L	O = L-ornithine, (IO)3 repititive motifs substituited	Analogs of Api137	Antimicrobial	After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v)	70 mg/L	249	Mouse serum protease	N.A.	Mouse serum	In Vitro	None	None	IC50(g/l) > 0.6 in HEK293
6126	27240277	2016	YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	ENF	36	Free	Free	Linear	L	None	Synthetic	Antiviral (against HIV infection)	N.A.	1.7 μmol/kg	1.5 ± 0.1 (Elimination Half Life)	SD rats plasma protease	HPLC	SD rats plasma	In Vivo	None	None	EC50(nM) = 3 ± 0
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)
6140	27157666	2016	KSLSRHDHIHHH	cMBP2-PEG-Stp/NIS Polyplex	12	Free	PEG-Stp = succinoyl-tetraethylene pentamine/NIS gene	Linear	L	123I labeling	Synthetic	Antitumor	48 hours after polyplex administration, mice received an intraperitoneal injection of 18.5 MBq 123I	18.5 MBq 123I	3	Huh7 subcutaneous mice xenografts protease	Gamma counter	Huh7 subcutaneous mice xenografts	In Vivo	https://sci-hub.st/10.1016/j.nucmedbio.2009.01.005	None	N.A.
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
6158	26869426	2016	ASCRTPKDCADPCAKETGCPYGKCMNRKCKCNRC	HsTX1[R14A]	34	Free	Amidation	Cyclic (C3-C24, C9-C29, C13-C31 Disulfide Linkage)	L	R14A substituitions	Isolated from the scorpion Heterometrus spinnifer	Treatment of Autoimmune Diseases	Blood samples (500 mL) were collected at 5, 15,30, 60, 120, 180, 240, and 300 min	2 mg/kg	79.6 ± 6.5 (Terminal elimination half life)	Rats plasma protease	LC-MS	Rats plasma	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/instance/2144240/pdf/10631983.pdf	None	IC50 value of 45 pM (affinity for Kv1.3 channels)
6159	26835125	2016	MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR	IONP-HA-GEM-CTX-Cy5.5	36	Conjugation of HA into CTX at N terminal in IONP-HA-GEM	Cy5.5 labeled	Linear	L	None	Synthetic	Glioblastoma therapy	At 1.5, 3, 6, 16, 24 and 48 h after injection, blood (20-50 L) was collected from tail veins	2 mg/ml	~2.8	BALB/c mice blood plasma protease	Fluorescence spectrometry	BALB/c mice blood plasma	In Vivo	PDB id: 1CHL	None	N.A.
6172	26806490	2016	CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMNEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE	Wild-type IFN	165	Free	Free	Linear	L	None	Recombinant human IFN-α2b	Antiviral, Anticancer	N.A.	1*106 U / 200 g	1.4 ± 0.3 (Elimination Half Life)	Wistar rats plasma protease	N.A.	Female Wistar rats plasma	In Vivo	PDB id: 1RH2	None	Specific antiviral bioactivity (U ng−1) = 185 ± 30, Specific antiproliferative bioactivity (U ng−1) = 309 ± 65
6176	26774588	2016	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36	34	Free	Amidation	Linear	L	None	Isolated and purified from porcine small intestine	Decrease appetite and food-intake	Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min	1 µM	175	Minipigs heparin-plasma protease	LC-MS	Minipigs heparin-plasma	In Vitro	None	None	N.A.
6177	26774588	2016	IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY	PYY3-36	34	Free	Amidation	Linear	L	None	Isolated and purified from porcine small intestine	Decrease appetite and food-intake	Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min	1 µM	220	Minipigs heparin-plasma protease	LC-MS	minipigs heparin-plasma with 10 mM EDTA	In Vitro	None	None	N.A.
6180	26754785	2016	MDTQTQTKLTVGCKCNPCKCQPLCKCGTTSSCNCQPCENCDPCSCNPCKCGATESCQCNPCKCAECKCCTHAVKTSACKCDPCSCNPCKCGVTQSCQCNPCTCAECKC	TfCuMT	108	Free	Free	Cyclic (4 Disulfide Bond Cys-Cys)	L	None	Copper metallothionein derived from ciliate Tetrahymena farahensis	Involved in metal homeostasis and metal detoxification by forming metal-thiolate complex	37°C	N.A.	103	N.A.	SDS PAGE	Sonicated sample (20ml) +5 ml SDS loading buffer (50% glycerol, 10% SDS,0.5 M dithiothreitol, 0.25% bromophenol blue, 0.25 M Tris-Cl pH6.8)	In Vitro	None	None	N.A.
6181	26752086	2016	WQRPSSWGGLRSLGRKILRAWKKYGQRLGNQWAVGHLM	ABB28	38	7 mer ABD domain conjugated at N terminus	Amidation	Linear	L	Biotinylation	Synthetic	Antitumor	N.A.	30 nmol	2	BALB/c mice plasma protease	ELISA	BALB/c mice plasma	In Vivo	None	None	IC50 ranges from 2.1–2.5 mM (In the absence of FBS) for ABB28
6188	26725426	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Exendin-4 analogs	Antihyperglycemic	N.A.	23.88 nmol/mL	3.53	Aminopeptidase N	Mass spectrometry	Intestinal fluid buffer (pH 6.8) with APN (0.2 U/mL)	In Vitro	PDB id: 7MLL	None	N.A.
6192	26725426	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Exendin-4 analogs	Antihyperglycemic	37°C	100 µg/mL	1.718	Intestinal duodenum homogenate protease	Ultraviolet spectroscopy	Intestinal duodenum homogenate	In Vitro	PDB id: 7MLL	None	N.A.
6193	26725426	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Exendin-4 analogs	Antihyperglycemic	37°C	100 µg/mL	1.462	Intestinal jejunum homogenate protease	Ultraviolet spectroscopy	Intestinal jejunum homogenate	In Vitro	PDB id: 7MLL	None	N.A.
6194	26725426	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exenatide	39	Free	Amidation	Linear	L	None	Exendin-4 analogs	Antihyperglycemic	37°C	100 µg/mL	1.229	Intestinal ileum homogenate protease	Ultraviolet spectroscopy	Intestinal ileum homogenate	In Vitro	PDB id: 7MLL	None	N.A.
6195	28989813	2016	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Exendin	39	Free	Amidation	Linear	L	Fluorescently labeled with Alexa Fluor	Derived from Heloderma suspectum	Antidiabetes	10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection	75 nmol/kg	1.7 ± 0.2 (T1/2 Elimination Half Life)	Mice plasma protease	Fluorescence assay	Mice plasma	In Vivo	PDB id: 7MLL	None	EC50(nM) = 0.08 ± 0.01
6199	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 1	3.6 mg/kg	3.12	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU	None	EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6200	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 1	3.6 mg/kg	4.33	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU	None	EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6201	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 1	36 mg/kg	3.69	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU	None	EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6203	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 1	180 mg/kg	4.79	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU	None	EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6207	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 26	36 mg/kg	3.71	Rats serum protease	Sandwich ELISA	Rats serum	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU	None	EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6225	26574515	2016	DWLKAFYDKVAEKLKEAFPAMSTYTGIFTDQVLSVLKGEE	CII-a	40	Free	Free	Linear	L	Two amphipathic helices linked by proline19	Synthetic	Treatment of Hypertriglyceridemia	0, 0.5, 1, 4, 7, 24, and 48 hours	1.0μmol/kg of body weight	1.33 ± 0.72	Apoc2 Mutant Mice Plasma Protease	MALDI-TOF MS	Apoc2 mutant mice plasma	In Vivo	https://pmc.ncbi.nlm.nih.gov/articles/PMC4293430/	None	peptide C-II-a dose of 5 μmol/kg achieved a maximum decrease of approximately 90% after 30 minutes, with plasma TG remaining below baseline levels for up to 48 hours
6226	26574515	2016	DWLKAFYDKVAEKLKEAFPAMSTYTGIFTDQVLSVLKGEE	CII-a	40	Free	Free	Linear	L	Two amphipathic helices linked by proline19	Synthetic	Treatment of Hypertriglyceridemia	0, 0.5, 1, 4, 7, 24, and 48 hours	1.0 μmol/kg of body weight	1.33 ± 0.72	Apoc2 mutant mice plasma protease	MALDI-TOF MS	Apoc2 mutant mice plasma	In Vivo	None	None	peptide C-II-a dose of 5 μmol/kg achieved a maximum decrease of approximately 90% after 30 minutes, with plasma TG remaining below baseline levels for up to 48 hours
6227	26565554	2016	SarLys-RPPGFSPf	NG29-TFacetate	10	SarLys = N-methyl glycine and Lysine	TFacetate = Trifluoroacetate addition at C terminal	Linear	Mix	D-Phenyalanine substituitions for L-Phenylanine and Arg9 removal from C terminal	BK analogue	Role in Neurological and Ischemic Cardiovascular diseases and brain cancer	N.A.	75 mg/kg	2.28 (Elimination Half Life)	Wistar Han rats plasma protease	LC-MS/MS	Wistar Han rats plasma	In Vivo	https://sci-hub.st/10.1139/y02-053	None	IC50(nM) = 0.3 for SarLys[dPhe8]desArg9BK ( for hB1R )
6228	26565554	2016	SarLys-RPPGFSPf	NG29-acetate	10	SarLys = N-methyl glycine and Lysine	Acetate addition at C terminal	Linear	Mix	(f) D-Phenyalanine substituitions for L-Phenylanine (F) and Arg9 removal from C terminal	BK analogue	Role in Neurological and Ischemic Cardiovascular diseases and brain cancer	N.A.	75 mg/kg	2.38 (Elimination Half Life)	Wistar Han rats plasma protease	LC-MS/MS	Wistar Han rats plasma	In Vivo	None	None	IC50(nM) = 0.3 for SarLys[dPhe8]desArg9BK ( for hB1R )