Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T62841 | Target Info | |||
| Target Name | 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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| Target Type | Clinical trial Target | ||||
| Gene Name | F2RL1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
|---|---|---|---|---|---|
| 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
|
[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
|
[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
|
[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
|
[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
|
[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
|
[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
|
[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
|
[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
|
[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
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| 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
|
[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
|
[6] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| 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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