Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T01007 | Target Info | |||
Target Name | HUMAN proteinase activated receptor 2 (PAR2) | ||||
Synonyms |
Thrombin receptor-like 1; Proteinase-activated receptor-2; Proteinase-activated receptor 2; Protease activated receptor 2; PAR-2; GPR11; G-protein coupled receptor 11; Coagulation factor II receptor-like 1
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Gene Name | F2RL1 | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
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Compound Name |
5-Isoxazoyl-Cha-Ile-(4-aminophenyl)-(4-[aminomethyl]piperidin-1-yl)methanone
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1269135; BDBM50329490
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Activity |
EC50 ~ 50000 nM
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[1] | |||
Compound Name |
2-Furoyl-Cha-Ile-NH2
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1271235; BDBM50329483
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Activity |
EC50 ~ 50000 nM
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[1] | |||
Compound Name |
CC(C)(C)OC(=O)N1CCN(C(=O)c2cn3nc(cc(c3n2)C(C)(C)C)-c2ccc(F)cc2)C(C)(C)C1
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3582251; SCHEMBL16598394; BDBM50091327
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Activity |
IC50 ~ 50000 nM
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[2] | |||
Compound Name |
CC(C)c1cc(nn2cc(nc12)C(=O)N1CCN(CC1(C)C)C(=O)OC(C)(C)C)-c1ccc(F)cc1
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3582248; SCHEMBL16598565; BDBM50091326
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Activity |
IC50 = 51000 nM
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[2] | |||
Compound Name |
5-Isoxazoyl-Cha-Ile-4-aminophenyl-(4morpholin-1-yl)ethan-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1269143; BDBM50329487
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Activity |
IC50 = 57000 nM
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[3] | |||
Compound Name |
1,7-Bis(4-methoxyphenyl)heptane-3,5-dione
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Investigative | Compound Info | ||
Synonyms |
CHEMBL4126288; SCHEMBL9404116; BDBM50274116; 1,7-bis(4-methoxyphenyl)-3,5-heptanedione
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Activity |
IC50 = 67800 nM
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[4] | |||
Compound Name |
2-Pyrazoyl-Cha-Ile-NH2
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1270927; BDBM50329484
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Activity |
EC50 ~ 100000 nM
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[1] | |||
Compound Name |
4-(2-Methyloxazoyl)-Cha-Ile-NH2
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Investigative | Compound Info | ||
Synonyms |
CHEMBL1271236; BDBM50329486
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Activity |
EC50 ~ 100000 nM
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[1] | |||
Compound Name |
(2S)-2-[[2-[(2-Amino-2-cyclohexylacetyl)amino]acetyl]amino]-5-(diaminomethylideneamino)pentanamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL4086537; BDBM50233750
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Activity |
EC50 ~ 100000 nM
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[5] | |||
Compound Name |
(2S)-2-[[2-[[2-[(2-Amino-3-cyclohexylpropanoyl)amino]-2-cyclohexylacetyl]amino]acetyl]amino]-5-(diaminomethylideneamino)pentanamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL4075046; BDBM50233746
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Activity |
EC50 ~ 100000 nM
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[5] | |||
Click to Show/Hide the Information of All Poor Binders |
Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
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Compound Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2431618; BDBM50440867
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Activity |
IC50 = 700000 nM
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[3] | |||
Compound Name |
6-Amino-1-[4-(3-methylbutanoyl)piperazin-1-yl]hexan-1-one
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Investigative | Compound Info | ||
Synonyms |
ENMD-1068; UNII-STV44CBK1W; STV44CBK1W; CHEMBL3734977; SCHEMBL31551; Piperazine, 1-(6-amino-1-oxohexyl)-4-(3-methyl-1-oxobutyl)-; 1-Hexanone, 6-amino-1-(4-(3-methyl-1-oxobutyl)-1-piperazinyl)-; BDBM50134201; ZINC37815137; AKOS008143439; MCULE-9859952650; NE16107; EN300-66569; n1-3-methylbutyryl-n4-6-aminohexanoyl-piperazine; Q27289393; Z1263529589
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Activity |
IC50 = 5000000 nM
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[6] |
References | Top | ||||
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REF 1 | Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40. | ||||
REF 2 | Inhibitors of the PAR-2 Signaling Pathway May Treat Pain and Inflammation. ACS Med Chem Lett. 2015 Apr 15;6(5):487-8. | ||||
REF 3 | Toward drugs for protease-activated receptor 2 (PAR2). J Med Chem. 2013 Oct 10;56(19):7477-97. | ||||
REF 4 | Isoxazole-tethered diarylheptanoid analogs: Discovery of a new drug-like PAR2 antagonist. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2285-2288. | ||||
REF 5 | Potent Small Agonists of Protease Activated Receptor 2. ACS Med Chem Lett. 2015 Nov 30;7(1):105-10. | ||||
REF 6 | Discovery of 2-aryloxy-4-amino-quinazoline derivatives as novel protease-activated receptor 2 (PAR2) antagonists. Bioorg Med Chem. 2015 Dec 15;23(24):7717-27. |
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