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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
1025	20844765	2010	RRWQWR	Lfc5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for E.coli
1026	20844765	2010	RRWQWR	Lfc5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for S. aureus
1027	20844765	2010	RRWQWR	Lfc5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=1.9Î¼M for B. subtilis
1028	20844765	2010	RRWWRF	Com5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=30Î¼M for E.coli
1029	20844765	2010	RRWWRF	Com5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99=7.5Î¼M for S. aureus
1030	20844765	2010	RRWWRF	Com5	6	Free	Free	Cyclic (head-to-tail backbone cyclization)	L	None	Synthetic	Antimicrobial	24 hours	5 µM	~24	Human serum proteases	RP-HPLC	Human serum	in vitro	None	None	LD99.99 ‰¤ 0.45Î¼M for B. subtilis
1088	12578830	2003	LPFFD	iAÎ²5p	5	Free	Free	Linear	L	None	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	100% inhibition of amyloid fibrillogenesis
1089	12578830	2003	LP-(NMe)-FFD	iAÎ²5p-A1	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1090	12578830	2003	LP-(NMe)-FF-(NMe)-D	iAÎ²5p-A4	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1091	12578830	2003	LP-(NMe)-F-(NMe)-FD	iAÎ²5p-A5	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1092	12578830	2003	LP-(NMe)-F-(NMe)-F-(NMe)-D	iAÎ²5p-A7	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1093	12578830	2003	LP-(Î±Me)-F-(Î±Me)-FD	iAÎ²5p-B1	5	Acetylation	Amidation	Linear	L	Î±Me	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Human plasma proteases	RP-HPLC	Human plasma	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1098	12578830	2003	LP-(NMe)-FFD	iAÎ²5p-A1	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1100	12578830	2003	LP-(NMe)-F-(NMe)-FD	iAÎ²5p-A5	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1101	12578830	2003	LP-(NMe)-F-(NMe)-F-(NMe)-D	iAÎ²5p-A7	5	Acetylation	Amidation	Linear	L	NMe	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1102	12578830	2003	LP-(Î±Me)-F-(Î±Me)-FD	iAÎ²5p-B1	5	Acetylation	Amidation	Linear	L	Î±Me	Synthetic	Î²-sheet breaker peptides	Not reported	20 nmol	>24	Proteases in rat brain homogenate	RP-HPLC	Rat brain homogenate	in vitro	None	None	>80% inhibition of amyloid fibrillogenesis
1213	21114599	2010	H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVK-Aib-R	[Aib8,35]hGLP-1(7-36)NH2	30	Free	Amidation	Linear	L	Aib--Aminoisobutyric acid	Analogue of glucagon like peptide1	Regulate blood glucose	Not mentioned	Not mentioned	20.4 ±1.8	Rat plasma proteases	HPLC	Rat plasma	in vitro	14759771	None	EC50=0.06 ±0.04nM for cAMP stimulation
1230	20593470	2010	GVFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS	Peptide 10	41	Free	Amidation	Linear	L	None	Synthetic dipeptide extended GLP-analogs	Regulate blood glucose	168 hours	Not mentioned	20.4	None	HPLC	PBS	in vitro	None	None	Not reported
1242	20560643	2009	YaGF-Nle-PL-Ser(Glc)-W	Peptide 6	9	Free	NH-3,5-Bzl(CF3)2	Linear	Mix	Nle=norleucine, O-Î²-glucosylated serine	Synthetic analogues of TY027	Opioid receptor agonist	24 hours	Not mentioned	>24	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	IC50=17 ±4.3nM for MVD
1771	16892368	2006	WDREINNYTSLIHWDREINNYTSLIH	Dimeric C46	26	Glycosylation	Amidation	Linear	L	None	Derived from T20	HIV-1 fusion inhibitory peptide	Not reported	40 ng peptide/200 mL plasma	1	Rat plasma proteases	ELISA	Rat plasma	in vitro	None	None	Not given
1995	19762245	2009	YaGFMPLW	TY005	8	Free	O-[3 €™,5 €™-(CF3 )2 Bzl]	Linear	Mix	None	Synthetic peptide	Analgesic	Not reported	50 µg/ml	24	Rat plasma proteases	HPLC	Rat plasma	in vitro	None	None	Not available
2086	N.A.	2004	ELAGIGILTV	[NMeEI, Î±MeL8]-Melan-A	10	Free	Free	Linear	L	Methylation of nitrogen of amide bond b/w Glu1 and Leu2 (NMe); Methylation of carboxyl of Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= isomer1(0.5 nM); isomer2(20 nM)
2089	N.A.	2004	PyroGlu-LAGIGILTV	[pEI, Î±MeL8]-Melan-A	10	PyroGlutamic acid at 1st position	Free	Linear	L	Methylation of carboxyl of Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= isomer1(0.02 nM); isomer2(3 nM)
2091	N.A.	2004	ALAGIGILTV	[Î²Al, Î±MeL8]-Melan-A	10	Beta-Alanine1	Free	Linear	L	Methylation of carboxyl of Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= isomer1(0.02 nM); isomer2(0.06 nM)
2093	N.A.	2004	ELAGIGILTV	[Î²El, Î±MeL8]-Melan-A	10	Beta-Glu1	Free	Linear	L	Methylation of carboxyl of Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= isomer1(0.3 nM); isomer2(0.015 nM)
2095	N.A.	2004	DLAGIGILTV	[Î²Dl, Î±MeL8]-Melan-A	10	Beta-Asp1	Free	Linear	L	Methylation of carboxyl of Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= isomer1(0.2 nM); isomer2(0.02 nM)
2097	N.A.	2004	GLAGIGILTV	[NOHG1, Î±MeL8]-Melan-A	10	Hydroxylation of N-terminal of Glycine	Free	Linear	L	Methylation of carboxyl of Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= isomer1(0.15 nM); isomer2(30 nM)
2098	N.A.	2004	ELAGIGILTV	[Î±MeL2, Î±MeL8]-Melan-A	10	Free	Free	Linear	L	Methylation of carboxyl of Leu2 and Leu8	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= Not mentioned
2100	N.A.	2004	ELAGIGILTV	[Î±MeL2, NMeT9] -Melan-A	10	Free	Free	Linear	L	Methylation of carboxyl of Leu2 and amino-group of Thr9 used in peptide bond	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= 0.5 nM
2101	N.A.	2004	ELAGIGILtV	[Î±MeL2, dT9]-Melan-A	10	Free	Free	Linear	Mix	Methylation of carboxyl of Leu2	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= 10.5 nM
2102	N.A.	2004	Î²ALAGIGILTV	[Î²Al, Ïˆ8-9(CH2-NH)]-Melan-A	10	Beta-Alanine	Free	Linear	L	Reduced bond between Leu8 and Thr9	Melan peptide which binds to HLA	Immunogenic and HLA binding peptides	N.A.	25 nM	24	Human serum proteases	HPLC-ESI-MS	Serum (human)	in vitro	None	EP1395276A1	EC50= 0.35 nM
2177	N.A.	2006	HGDGSFSDEMNTILDNLAARDFINWLIQTLITDK	Derivative of Glucagon Like Peptide-2 (GLP-2)	34	Free	Addition of maleimidopropionic acid (MPA) and amidation	Linear	L	None	GLP-2	Intestine function modulator	N.A.	500 nM/ Kg	23.8	Not mentioned	Radioimmunoassay	Rat plasma (Subcutaneous)	in vivo	None	US7112567B2	Not mentioned
2232	12954066	2003	ELYENKP-N3-Hlys-RPY-tert-Leu-L	KK13	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	>24	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.
2233	12954066	2003	ELYENKP-N3-Hlys-RPY-tert-Leu-L	KK14	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	>24	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.
2242	12220890	2002	lsaydpvdypysnsfakc	Retro-inverso hemagglutinin [(HA) 91 €“108] derivative	18	Acetylation	Amidation	Linear	D	None	Derivative of B-cell epitope hemagglutinin (HA) 91 €“108 from influenza	Modulate immune response	Not mentioned	1 mg/ml	>24	Mice lung homogenate proteases	RP-HPLC	BALB/c mice lung homogenate	in vitro	None	None	IFN-y production in presence of peptide was measured. Splenocyte was collected after 12 days of immunization, cultured in presence / absence of Inactivated virus(500 HAU/well). Level of IFN-y in presence of virus is ~2500 pg/ml as measured by ELISA.
2443	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	>24	SCLC proteases	RP-HPLC and Electrochemical Detection	Small cell lung cancer (SCLC)	in vitro	None	None	Act as growth factors
2444	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	20.9	None	RP-HPLC and Electrochemical Detection	Water	in vitro	None	None	Act as growth factors
2445	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	>24	None	RP-HPLC and Electrochemical Detection	Acetic acid	in vitro	None	None	Act as growth factors
2448	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	22.8	SCLC proteases	RP-HPLC and Electrochemical Detection	Small cell lung cancer (SCLC)	in vitro	None	None	Act as growth factors
2449	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	10 Î¼g/ml	>24	SCLC proteases	RP-HPLC and Electrochemical Detection	Small cell lung cancer (SCLC)	in vitro	None	None	Act as growth factors
2450	7529108	1994	CSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGSPRS	Human big endothelin-1 (Human big-ET-1)	38	Free	Free	Linear	L	None	Human Endothelin-1	Vasoconstricting peptide	180 minute	3 nmol of peptide with 200 ng of enzyme	24 (t1/2 of hydrolysis)	Endopeptidase-24.11(E-24.11)	Radioimmunoassay and RP-HPLC	Purified ET-1 protein sample	in vitro	8269939	None	Not reported
2596	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	0.138 mg/kg	23.1 ±4.3	Rat plasma proteases	Competitive ELISA	Rat plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2597	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	0.69mg/kg	21.5 ±3.6	Rat plasma proteases	Competitive ELISA	Rat plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2598	16982323	2006	(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG	Hematide	42	Acetylation	Beta-alanine-PEG	Linear	L	X1-Napthyl-alanine, X2-Sarcosine	Synthetic dimeric peptide	Erythropoiesis stimulating agent	Not mentioned	1.38 mg/kg	22.2 ±1.7	Rat plasma proteases	Competitive ELISA	Rat plasma (Dose i/v adminstered)	in vivo	None	None	IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2630	17766836	2003	(RRPYIL)-PEG-biotin	NT (Neurotensin) [8-13]	24	Free	Pegylation	Linear (Tetra-branched)	L	4 Hexapeptide bound to PEG-Biotin to form tetra branched	Synthetic	Regulates luteinizing hormone and prolactinrelease	37 °C for 2-24 hours	Not mentioned	>24	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
2631	18249125	2009	HSSKLQ	Prostate Specific Antigen (Prodrug 2)	6	Mu (Morpholino)	Cyclopamine	Linear	L	None	Synthetic	Prostate-specific antigen (PSA)-activated prodrugs against prostate cancer	0.5-18 hours at room temperature	100 µM	22	PSA enzymes	Hydrolysis and RP-HPLC	NA	in vitro	None	None	Not reported
2667	22186872	2011	CYIQNCPLG	Oxytocin	9	Free	Amidation	Cyclic (C1-C6)	L	None	Hypothalamus	Cause contraction of the uterus during labor and intiate milk release from breast	Room Temperature	1mg/mL	1	Hydolytic activity of bacterial strain B-9	HPLC and LC/ITMS	Bacterial strain B-9 cell culture	in vitro	None	None	Not reported
2694	25039358	2014	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Coumarin-modified GLP-1 derivative 9	30	Free	Amidation	Linear	L	X-2 = Lys- conjugated-7-hydroxyCoumarin maleimide	Analog of human GLP-1	Hypoglycaemic	37 °C for 2-72 hours	1000ng/ml	21.6	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vitro	None	None	GLP-1 receptor Activation potency with EC50 = 8.1 ± 0.6 pM in HEK-293 cells
2696	25039358	2014	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	Coumarin-modified GLP-1 derivative 11	30	Free	Amidation	Linear	L	X-2 = Lys- conjugated-7-hydroxyCoumarin maleimide	Analog of human GLP-1	Hypoglycaemic	37 °C for 2-72 hours	1000ng/ml	20.3	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vitro	None	None	GLP-1 receptor Activation potency with EC50 = 19.9 ± 1.4 pM in HEK-293 cells
2701	25039358	2014	HAEGTFTSDVX-2SYLEGQAAKEFIAWLVKGR	Coumarin-modified GLP-1 derivative 7	30	Free	Amidation	Linear	L	X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide	Analog of human GLP-1	Hypoglycaemic	37 °C for 2-72 hours	1000ng/ml	22 .9 ±7.2	Rat plasma proteases	LC-MS/MS	Rat Plasma	in vivo	None	None	GLP-1 receptor Activation potency with EC50 = 18.6 ± 1.3 pM in HEK-293 cells
2713	25594223	2015	CYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF	SL-ENF(Sialic acid Enfuvirtide)	37	Sialic acid	Amidation	Linear	L	None	Synthetic derived from glycosylated ENFs	Anti-viral	0.5-24 hours	1.7Î¼M/Kg	23.1	Rat plasma proteases	HPLC	Sprague-Dawey (SD) rats Plasma	in vivo	None	None	EC50 = 2nM for Anti-viral potency
2758	26222180	2015	HS/QGTFTSDYSKYLDSRRAQDFVQWLMNTKRNRNNIA	OXM(1-37) (Oxyntomodulin)	37	Free	Free	Linear	L	None	Peptide Hormone of colon	Anti-apetizer	Room Temp	0.4 µM	<24	Human plasma proteases + DPP IV	MS	EDTA plasma	in vitro	None	None	Not reported
2825	1329046	1992	fQWAVaHL	[FA]BN(6-13)M [Bombesin antagonist]	8	Fluoryl amide	Methy esterification	Linear	Mix	None	Bombesin analogue	Growth inhibitors	0-1080 minutes	50Î¼M	1388	Degradative enzymes or SCLC cell line proteases	RP-HPLC	SCLC cell line NCI-H345	in vitro	None	None	IC50= 9nM, Peptide were added at a 1 Î¼M dose to inhibit growth of SCLC cell line
3050	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	500Î¼g/kg	21.6	Rats blood proteases	Radioimmunoassay	Intravenous injection of the peptide in Hans Wistar Male rat	in vivo	None	None	Platelet count increased from 1,504Ã—103/mm3 to 2,262Ã—103/mm3,Neutophil count increased from 941/mm3 to 19,802/mm3,Monocyte count increased from 160/mm3 to 7,917/mm3,Eosinophil count increased from 86/mm3 to 1067/mm3,Basophil count increased from 11/mm3 to 653/mm3,Lymphocyte count increased from 4,210/mm3 to 24,759/mm3,RBC count decreased form 7.05Ã—106/mm3 to 5.56Ã—106/mm3,Prothrombin time increased from 13.7 to 16.7 seconds.
3052	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	1000Î¼g/kg	23	Rats blood proteases	Radioimmunoassay	Intravenous injection of the peptide in Hans Wistar Male rat	in vivo	None	None	Platelet count increased from 1,504Ã—103/mm3 to 2,243Ã—103/mm3,Neutophil count increased from 941/mm3 to 18,870/mm3,Monocyte count increased from 160/mm3 to 6,790/mm3,Eosinophil count increased from 86/mm3 to 810/mm3,Basophil count increased from 11/mm3 to 329/mm3,Lymphocyte count increased from 4,210/mm3 to 24,874/mm3,RBC count decreased form 7.05Ã—106/mm3 to 5.53Ã—106/mm3,Prothrombin time increased from 13.7 to 17.2 seconds.
3053	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	1000Î¼g/kg	20.4	Rats blood proteases	Radioimmunoassay	Intravenous injection of the peptide in Hans Wistar Female rat	in vivo	None	None	Platelet count increased from 1,504Ã—103/mm3 to 2,243Ã—103/mm3,Neutophil count increased from 941/mm3 to 18,870/mm3,Monocyte count increased from 160/mm3 to 6,790/mm3,Eosinophil count increased from 86/mm3 to 810/mm3,Basophil count increased from 11/mm3 to 329/mm3,Lymphocyte count increased from 4,210/mm3 to 24,874/mm3,RBC count decreased form 7.05Ã—106/mm3 to 5.53Ã—106/mm3,Prothrombin time increased from 13.7 to 17.2 seconds.
3065	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	1000Î¼g/kg following dose 1	23.4	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus male monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,820Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96Ã—106/mm3 to 6.16Ã—106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3066	10606160	1999	(IEGPTLRQ-Npa-LAAR-Sar)2K	GW395058	29	Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]	Amidation	Linear (branched)	L	Npa-napthylalanine,Sar-sarcosine	AF15705(substituted thrombopoietin mimetic peptide)	Treatment of thrombocytopenia	48 hours	1000Î¼g/kg following dose 1	23.7	Monkey blood proteases	Radioimmunoassay	Intravenous injection in cynomolgus female monkey	in vivo	None	None	Platelet count increased from 381Ã—103/mm3 to 2,820Ã—103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96Ã—106/mm3 to 6.16Ã—106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3107	20687610	2010	HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR	c[E16,K20]-c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2	30	Free	Amidation	Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K34)	L	None	Analog of GLP-1	Diagnosis and treatment of diabetes	24 hours	100Î¼M	>24	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/DB00126	None	EC50=1.8nM,pEC50=8.7 ±0.09
4012	38785334	2024	IsoV-DTHFPCIKFEPRSKGCK	Rusfertide (PTG-300)	18	IsoV = Isovaeryl at position 1	Amidation	Cyclic(C7-C17 Disulfide Linkage)	L	Lys8 conjugation with palmitoyl-Glu(2)-OH	Synthetic	Provides therapy for PV and Hemochromatosis	N.A.	3 mg	21.3 ± 6.2	Human plasma protease	HPLC-MS	Human plasma	In Vivo	None	None	N.A.
4027	38721043	2024	SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFC	EXT607 (R=OH)	35	Free	Cys modified PTH-1 linked with VitD3 through (PEG)36	Linear	L	R= OH for Cys35	PTH-1 derivative	Treatment of Hypoparathyroidism	Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose	0.007 mg/kg	24	Cynomolgus monkeys plasma protease	ELISA	Cynomolgus monkeys plasma	In Vivo	None	None	EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1)
4044	38486997	2024	HsQGTFTSDKSKYLE-Aib-KAAQDFVEWLKAGGPSSGAPPPS	1907-B	40	Free	Replacing the amide bond with a C-terminal acid	Cyclic (Lactam Bridge K17 & D21)	Mix	At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine	GLP-1 analogs	Antidiabetes	Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration	0.05 mg/kg	∼20.5	SD rats plasma protease	LC-MS/MS	SD rats plasma	In Vivo	None	None	GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B)
4241	36902021	2023	RNWELRLK-(PEG)4-RNWELRLK-(PEG)4	PDC	16	Free	PEG4 spacer was designed and subsequently reacted with a cysteine at the carboxyl terminus then, the elongated thiol-modified homodimer peptide was conjugated with DOX	Linear	L	None	HER2-targeting peptide–DOX conjugate	Antitumor	The PDC was incubated with human plasma (final peptide concentration of 50 μM) for 0, 2, 4, 8, 12, 24, and 48 h	50 μM	24	Human plasma protease	HPLC	Human plasma	In Vitro	None	None	The IC50 value for the PDC (Peptide-Drug Conjugate) is 140 nM. This value indicates that the PDC is more potent in killing HER2-positive SKBR-3 cells compared to free DOX, which has an IC50 of 410 nM
4264	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-PEGRh(4.4 ± 1.1nm)	39	Free	PEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCO	Linear	L	Fluorescently labeled	Exendin-4 analogs	Antidiabetes	Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h	1000 nmol kg−1	23.14 ± 3.2(T1/2 Elimination)	Naïve mice plasma protease	Fluorescence assay	Naïve mice plasma	In Vivo	None	None	EC50 = 1.3 ± 0.2 nM
4276	36630826	2023	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS	Ex-PEGRh	39	Fluorescently labelled	Exendin-DBCO was conjugated to azide-functional PEG(27.7KDa)	Linear	L	None	Exendin-4 analogs	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	23.14 ± 3.2 (T1/2 Elimination)	Naïve mice plasma protease	fluorescence assay	Naïve mice plasma	In Vivo	None	None	EC50 (nM) = 1.3 ± 0.2
4295	N.A.	2023	Y-Aib-EGTFISDLSI-Aib-KEEIHQ-Aib-EFIEWLLAQGPSSGAPPPS	SEQ ID NO 19	39	Free	Amidation	Linear	L	Aib = α-aminoisobutyric acid	Exendin-4 analogs	Antidiabetes	Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application	0.5 mg/kg	20.1	Rats plasma protease	LC-MS	Rats plasma	In Vivo	None	EP 2022074607 W	IC50 hGIPR (nM) = 2
4472	36380917	2022	HAEGTFTSDVSSYLEGQAANESIAWLVKGRG	Glycan-GLP-1-3(G2S2)	31	Free	Free	Linear	L	N-glycosylation with sialylated biantennary complex-type N-glycan at Asn26(G2S2 glycoform = sialylated glycan)	GLP-1 analogs	Antidiabetes	37 °C	6 nmol	1393.1 ± 8.9	Mouse serum protease	RP-HPLC	Mouse serum	In Vitro	None	None	BGLmax (mmol L−1) = 25.71 ± 3.19 (In vivo glucose stabilizing capability)
4545	35892256	2022	GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT	RA15127343	51	Free	Free	Linear	L	Albumin binding fatty-acid side chain is coupled to lysine (B29)	Insulin analogue	Antidiabetes	N.A.	200, 400 nmol/kg	21 - 22	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	https://sci-hub.st/10.1016/j.jpba.2018.07.009	None	(Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM
4656	35150805	2022	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSASTKGPS	Exenatide-7aa'-ABNF	46	Free	Albumin binding Nanofitins (ABNF) linked at C terminus by 7 aa	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection	400 nmol/kg	20.8 (Terminal Half Life)	Male CDR1 mice plasma protease	ELISA	Male CDR1 mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.5785 nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4658	35150805	2022	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS(GGGGS)2GG	Exenatide-12aa-ABNF	51	Free	Albumin binding Nanofitins (ABNF) linked at C terminus by 12 aa	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection	400 nmol/kg	21.9 (Terminal Half Life)	Male CDR1 mice plasma protease	ELISA	Male CDR1 mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.8065 nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4660	35150805	2022	HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSHGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSIEGR	Exenatide-Exenatide-4aa-ABNF	82	Free	Albumin binding Nanofitins (ABNF) linked at C terminus by 4 aa	Linear	L	None	GLP-1 analogs	Antidiabetes	Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection	300 nmol/kg	20.5 (Terminal Half Life)	Male CDR1 mice plasma protease	ELISA	Male CDR1 mice plasma	In Vivo	PDB id: 7MLL	None	EC50 = 0.3708 nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4775	35177945	2022	KFRRQRPRLSHKGPMPF	LIT01-196	17	FC [CF3(CF2)7(CH2)2C(O)] conjugation at N terminal	Free	Linear	L	None	Apelin Analog	Diuretic and Cardiovascular effects	Incubated at 37°C for various times, from T0 to T4 h	5 μM	1440	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) = 0.08 ± 0.01
4777	35177945	2022	QRPRLSHKGPMPF	(Lys8GluPAL)apelin-13-amide	13	Free	Amidation	Linear	L	None	Apelin-13 Analogue	Antidiabetes, Anorexic Effects	N.A.	N.A.	>24	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 = 1.2 x 10⁻¹⁰ M
4778	35177945	2022	QRPRLSHKGPMPY	Lys8GluPAL(Tyr13)apelin-13	13	Free	Tyr13 modifcation, carboxylation	Linear	L	None	Apelin-13 Analogue	Antidiabetes, Anorexic Effects	N.A.	N.A.	>24	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 = 1.1 x 10⁻⁹ M
4779	35177945	2022	QRPRLSHKGPMPV	Lys8GluPAL(Val13)apelin-13	13	Free	Val13 modifcation, carboxylation	Linear	L	None	Apelin-13 Analogue	Antidiabetes, Anorexic Effects	N.A.	N.A.	>24	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 = 2.2 x 10⁻¹⁰M
4780	35177945	2022	pGlu-RPRLSHKGPMPF	pGlu(Lys8GluPAL)apelin-13-amide	13	pGlu = Pyroglutamate	Amidation	Linear	L	None	Apelin-13 Analogue	Antidiabetes, Anorexic Effects	N.A.	N.A.	>24	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 = 3.1 x 10⁻¹⁰M
4991	33607165	2021	KΨ[CH2NH]K-Sip-YIL	JMV5170	6	Free	Free	Linear	L	Pro10 was then substituted by the silylated proline analog silaproline(Sip) , Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	22.1 ± 1.9	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 296 ± 51 for hNTS1
4993	33607165	2021	KΨ[CH2NH]K-Sip-YI-TMSAla	JMV5296	6	Free	Free	Linear	L	Di-substitution with both Sip and TMSAla, Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9	Derived from NT	Analgesic without hypothermia	Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min	0.156 mM	20.6 ± 4.15	Rats plasma protease	UPLC-MS	Rats plasma	In Vivo	None	None	(Binding) Ki (nM) = 610 ± 31 for hNTS1
5099	32858124	2020	(C18-diacid)-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip	Cmpd# 23	16	Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C18-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	> 24	Male SD rats plasma protease	Scintillation proximity assay	Male SD rats plasma	In Vivo	None	None	Rat GTPγS (nM) EC50 ± SE = 117 ± 23.3
5139	32582624	2020	Kψ(CH2NH)K-Sip-YIL	Entry 6	6	Kψ[CH2NH]K substiuition	Free	Linear	L	Sip amino acid substiution	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	22 ± 2	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 300 ± 50 for hNTS1
5149	32582624	2020	Kψ(CH2NH)KP-Dmt-L	Entry 16	5	Kψ[CH2NH]K substiuition	Free	Linear	L	Substiution of Y, I amino acid with Dmt	NT(8-13) analogs	Improve Nts1-Induced Protective Hypothermia	NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C	0.156 mM	>24	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Binding, Ki (nM) = 110 ± 2 for hNTS1
5193	35496622	2020	HGEGTFTSDLSKQMEEEAVRLFIEWLNGGPSSGAPPSKKKKKK	Lixisenatide 1e	44	Free	Amidation	Linear	L	(X2) MPAs modification on Lys12	lixisenatide analogues	Antidiabetes	incubated at 37 °C for 6, 12, 24, and 48 h	1000 ng/mL	21.2	Rats blood plasma protease	LC-MS/MS	Rats blood plasma	In Vitro	None	None	EC50(nM) = 0.13 ± 0.03 for Lixisenatide 1e (in vitro GLP-1 receptor activation potency)
5201	32141733	2020	INPIYRLRY	TB1-RS6	6	Fluorescein	Amidation	Linear	L	Single atom O toS substitution (X=S)	Thioamide-stabilized version	Stabilization of cancer imaging peptides	37 °C	50 μM	>24	Mouse serum protease	HPLC	Mouse serum	In Vitro	https://sci-hub.se/10.1021/acs.molpharmaceut.6b00464	None	KI = 101 ± 24 nM, The IC50 values determined for TB1 and TB1-RS6 (719 ± 143 nM and 1363 ± 323 nM, respectively
5222	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 169 h post injection	5 mg/kg	22.5 ± 1.3 (Terminal Half Life)	Rats plasma protease	LC-MS/MS	Rats plasma	In Vivo	None	None	EC50(nM) = 0.24 for hGLP-2 receptor
5381	31156041	2019	LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK	AD-114-PA600	118	Free	PA-600	Linear	L	None	Fusion protein of AD-114 with PA600	Attenuates Renal fibrosis through blockade Of CXCR	Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h.	0.1 mg/kg	23.53	Cynomolgus monkeys plasma protease	LC–MS/MS	Cynomolgus monkeys plasma dosed at Day 1	In Vivo	PDB id: >5AEA_1	None	Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K
5484	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.	20.5	hplasma protease	LC-MS	hplasma	In Vitro	None	None	EC50(nM) = 11.3 ± 2.1
5650	30226777	2018	WILEYLWKVPFDFWRGVI	E1-NP	18	Free	Free	Linear	L	None	Derived from the E1 envelope protein of GBV-C	HIV-1 fusion inhibitor peptide	At different incubation times (30 min, 1, 2, 4, 8, and 24 h)	1 mg/mL	24	Human serum protease	HPLC	Human serum	In Vitro	None	None	N.A.
5690	30023916	2018	HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRC	(CH30,CH40,CH70)-conjugated peptides	31	CH30/CH40/CH70 linker by linker	Free	Linear	L	Substituition of G for A at position 2	Synthetic	Antidiabetes	37 °C for 2 h	N.A.	22 - 25 (T1/2 Elimination Half life)	0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii	HPLC	N.A.	In Vitro	None	None	N.A.
5710	29799205	2018	HGEGTYTNDVTEYLEEEAAKEFIEWLI-X1-GK	4d	29	Free	Free	Linear	L	X1 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	20.2	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) = 0.49 ± 0.07
5713	29799205	2018	HGEGTYTNDVTEYLEEEAA-X1-EFIEWLIKGKPSSGAPPPS	4g	38	Free	Free	Linear	L	X1 = structure given in paper	Xenopus GLP-1 analogs	Antidiabetes	37°C over 72 h	1000 ng/mL	21.5	Rats plasma protease	LC-MS/MS.	Rats plasma	In Vitro	None	None	EC50(nM) =0.18 ± 0.02
5779	29602308	2018	HSTPSSP	P4-Chlorambucil-PEG-AuNP	7	Free	Chlorambucil	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	21	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5781	29602308	2018	HSTPSSP	P4-Melphalan-PEG-AuNP	7	Free	Melphalan	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	22	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5783	29602308	2018	HSTPSSP	P4-Bendamustine-PEG-AuNP	7	Free	Bendamustine	Linear	L	None	Protein drug conjugate	Anticancer	37 °C	100 μl/ ml	22.3	N.A.	LC–MS/MS	Buffer pH 7.4	In Vitro	None	None	The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5806	29517911	2018	CSF-Aze-Y-hArg-CVYYPDICA-(Sar)3-rr	4b	17	Acetylation	Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues	Bicyclic (Cyclized On C1, C7, C14 By 1,3,5 Trismethylbenzene)	L	HArg, Aze substituitions	synthetic	Antidiabetes (Treatment of Diabetic Macular Edema)	The animals were sacrificed 15 min, 1 h, 4 h, 8 h, 24 h, 48, and 96 h after injection	2 mg/mL	~22	Rabbit eye plasma protease	HPLC	Rabbit eye plasma	In Vivo	None	None	Ki Values (nM) = ∼2,650 against PKal from Rabbit
5807	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)	24 h at 37 °C	0.16 mM	>24	Human vitreous protease	LC-MS/MS	Human vitreous	In Vitro	None	None	Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats
5808	29517911	2018	CSFPY-hArg-CAHQDLC	2d	13	Acetylation	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions	2a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	24 h at 37 °C	0.16 mM	>24	Human vitreous protease	LC-MS/MS	Human vitreous	In Vitro	None	None	Ki Values (nM) = 30 ± 9 against PKal from Rats
5809	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	>24	Human vitreous protease	LC-MS/MS	Human vitreous	In Vitro	None	None	Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats
5810	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)	24 h at 37 °C	0.16 mM	>24	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vitro	None	None	Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats
5811	29517911	2018	CSFPY-hArg-CAHQDLC	2d	13	Acetylation	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions	2a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	24 h at 37 °C	0.16 mM	>24	Mouse plasma protease	LC-MS/MS	Mouse plasma	In Vitro	None	None	Ki Values (nM) = 30 ± 9 against PKal from Rats
5813	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)	24 h at 37 °C	0.16 mM	>24	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	None	None	Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats
5814	29517911	2018	CSFPY-hArg-CAHQDLC	2d	13	Acetylation	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions	2a analogue	Antidiabetes (Treatment of Diabetic Macular Edema)	24 h at 37 °C	0.16 mM	>24	Rats plasma protease	LC-MS/MS	Rats plasma	In Vitro	None	None	Ki Values (nM) = 30 ± 9 against PKal from Rats
5816	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	24 h at 37 °C	0.16 mM	>24	Human plasma protease	LC-MS/MS	Human plasma	In Vitro	None	None	Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats
5817	29517911	2018	CSFPY-hArg-CAHQDLC	2d	13	Acetylation	Free	Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)	L	Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions	2a analogue	Antidiabetes	24 h at 37 °C	0.16 mM	>24	Human plasma protease	LC-MS/MS	Human plasma	In Vitro	None	None	Ki Values (nM) = 30 ± 9 against PKal from Rats
5829	29461833	2018	RPRL-Sx-HKG-X-Nle-PF	Pyr analogue 9	13	pGlu = Pyroglutamate	Free	Cyclic (Sx6-X10 Bond)	L	X= allylglycine, Sx=Na-allyl-serine, 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	>24	Rats plasma protease	UPLC-MS	Rats plasma	In Vitro	None	None	Ki binding (nM) = 41 ±4 for 9L
5876	29335522	2018	N.A.	PAK2	N.A.	N.A.	N.A.	N.A.	N.A.	N.A.	Synthetic	Role in PDAC cancer invasion and metastasis	N.A.	N.A.	>24	Miapaca-2 cell lysate protease	Western blotting	Miapaca-2 cells lysate with PKM2 expression (treated with 20 μg/ml cycloheximide (CHX))	In Vitro	None	None	N.A.
5884	29329072	2018	YFLFRRN	Compound 42	7	Acetylation	Amidation	Linear	L	Oic = octahydroindole carboxylic acid modification between R5 and R6	NMU-analogs	Regulation Of Feeding Behavior, The Stress Response And Nociception	37 °C	112 µM	1426.1 ± 67.4	Human plasma protease	RP-HPLC	Human plasma	In Vitro	None	None	EC50(nM) = 28.8, IC50(nM) = 11.2 for hNMUR1 and EC50(nM) = 1.8, IC50(nM) = 13.9 for hNMUR2
5958	28799326	2017	DAHKSEVAHRFKDLGEENFKALVLIAFAQYLQQCPFEDHVKLVNEVTEFAKTCVADESAENCDKSLHTLFGDKLCTVATLRETYGEMADCCAKQEPERNECFLQHKDDNPNLPRLVRPEVDVMCTAFHDNEETFLKKYLYEIARRHPYFYAPELLFFAKRYKAAFTECCQAADKAACLLPKLDELRDEGKASSAKQRLKCASLQKFGERAFKAWAVARLSQRFPKAEFAEVSKLVTDLTKVHTECCHGDLLECADDRADLAKYICENQDSISSKLKECCEKPLLEKSHCIAEVENDEMPADLPSLAADFVESKDVCKNYAEAKDVFLGMFLYEYARRHPDYSVVLLLRLAKTYETTLEKCCAAADPHECYAKVFDEFKPLVEEPQNLIKQNCELFEQLGEYKFQNALLVRYTKKVPQVSTPTLVEVSRNLGKVGSKCCKHPEAKRMPCAEDYLSVVLNQLCVLHEKTPVSDRVTKCCTESLVNRRPCFSALEVDETYVPKEFNAETFTFHADICTLSEKERQIKKQTALVELVKHKPKATKEQLKAVMDDFAAFVEKCCKADDKETCFAEEGKKLVAASQAALGL	WT-albumin	585	Free	Free	Linear	L	None	Produced by secretion from yeast	Carrier protein	Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours	5 mg/kg	21.5	NMR1 mice serum protease	AlphaLISA	NMR1 mice serum	In Vivo	None	None	KD±SD (nM) = 548.7 ±90.2 against human FcRn receptor
5966	28741871	2017	Y-Aib-EGTFTSDYSIYLDKQAA-Aib-EFVNWLLAGGPSSGAPPPSK	RG7697	40	Free	Acylated at a C-terminal lysine with a saturated C16 lipid	Cyclic (L14-E21, Q17-N24 Lactam Bridge)	L	Aib modification at position 2, 20	chimera of GLP-1 and GIP peptides	Antidiabetes	RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted	0.6 mg	23.2 (T1/2b- Appearant Terminal Half Life)	Human plasma protease	LC-MS	Human plasma	In Vivo	None	None	for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors
5990	28623878	2017	FEFKFEFKK	FITC-F9 hydrogel	9	Fluoresceinisothiocyanate labelled	Free	Linear	L	None	F9 analogue	Therapeutic drug delivery	5 days	0.01 M	1 to 4	Mice plasma protease	fluorescence assay	Mice plasma	In Vivo	None	None	N.A.
6033	28323965	2017	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGFSSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Measured at the final randomized dose (following the second dose)	0.66 mg/kg	22.4	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 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6070	27815337	2017	KFRRQRPRLSHKGPMPF	LIT01-196	18	CF3(CF2)7(CH2)2C(O)	Free	Linear	L	None	Apelin analogs	Diuretic and Cardiovascular Effects	37°C	5 μM	1440	Mouse plasma protease	LC-MS	Mouse plasma	In Vitro	None	None	Recruitment of b-arrestin2 by BRET, EC50 (nM) = 16 ± 5.6
6085	N.A.	2017	ASDEEIQDVSGTWYLKAMTVDRFKIASWPRSVTPMTLTTLEGGNLEAKVTMNWWGRSQEVKAVLERTDEPGKYTAQGDRHVAYIIRSPVKDHYIFYSEGNLQGETVPGVWLVGRDPKNNLEALEDFEKAAGARGLSTESILIPRQSETSSPGGGGSLAEAKEAANAELDSYGVSDFYKRLIDKAKTVEGVEALKDAILAALPG	SEQ ID NO 83	203	Free	ABP-G148 (Albumin binding protein) conjugation	Linear	L	None	Lipocalin muteins	Pcsk9-Specific Lipocalin Muteins	N.A.	N.A.	24	Rats plasma protease	Sandwich ELISA	Rats plasma	In Vivo	None	US 201715445066 A	IC50(nM) = 1.93 without HSA for LDLR binding
6121	27337048	2016	CKASAPPSCYDGDD	SFTI-a	14	Free	Free	Cyclic (C1-C9 Disulfide Bond)	L	None	Sunflower trypsin inhibitor derivative	Immunomodulatory inhibitors of the CD2:CD58 protein–protein interaction	37 °C at various time points from 0 min to 24 h	2 mg/ml	<=24	Human serum protease	HPLC, MS	Human serum	In Vitro	None	None	Cell adhesion inhibition IC50 (µM) = 0.043 ± 0.025 in T cell OVCAR-3
6163	26818056	2016	YPAKPEAPGEDASPEELSRYYASLRHYLNLVTRQRY	PYY1–36	36	Free	Amidation	Linear	L	None	Released from enteroendocrine cells	Anorexic effects	Samples were taken regularly (t = 0, 0.5, 1, 2, 3, 4, 6, 8, 21, and 24 h)	0.6 pmol/mL	22.8 ± 8.0 − 3.6 ± 0.6	Human blood plasma protease	RIA (when correcting for NH2-terminal degradation)	Human blood with EDTA, aprotinin (500 KIE/ml), and the DPP-4 inhibitor valine pyrrolidide (0.01 mmol/l, final concentration (when correcting for NH2-terminal degradation)	In Vitro	https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x	None	The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l
6167	26808199	2016	LRHYLNLLTRQRY	PYY24–36-Leu31 conjugates 8	13	R8( structure given in paper) at NH terminal	Amidation	Linear	L	Leu31 substituitions	PYY analog	Antiobesity	An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point	1000 ng/mL	24	SD rats plasma protease	LC–MS/MS	SD rats plasma	In Vitro	None	None	HSA binding correlated well with plasma stability
6221	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 181	30 mg/kg	22.44 ± 12.53	Monkeys serum protease	Sandwich ELISA	Monkeys 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)
6222	26713839	2016	SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ	MOD-4023	275	CTP fused to hGH	2 CTP fused	Linear	L	None	Synthetic	Treatment of GHD	Day 181	30 mg/kg	22.54 ± 19.55	Monkeys serum protease	Sandwich ELISA	Monkeys 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)