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Target
Proteinase-activated receptor 1
Ligand
BDBM50202073
Substrate
n/a
Meas. Tech.
ChEMBL_423382 (CHEMBL909901)
Ki
11±n/a nM
Citation
Clasby, MC; Chackalamannil, S; Czarniecki, M; Doller, D; Eagen, K; Greenlee, W; Kao, G; Lin, Y; Tsai, H; Xia, Y; Ahn, HS; Agans-Fantuzzi, J; Boykow, G; Chintala, M; Foster, C; Smith-Torhan, A; Alton, K; Bryant, M; Hsieh, Y; Lau, J; Palamanda, J Metabolism-based identification of a potent thrombin receptor antagonist. J Med Chem 50:129-38 (2007) [PubMed] Article
More Info.:
Target
Name:
Proteinase-activated receptor 1
Synonyms:
CF2R | Coagulation factor II receptor | F2R | PAR-1 | PAR1 | PAR1_HUMAN | Proteinase activated receptor 1 | Proteinase-activated receptor 1 (PAR-1) | TR | Thrombin receptor | Thrombin receptor/ Proteinase-activated receptor 1(Par-1)
Type:
Protein
Mol. Mass.:
47450.07
Organism:
Homo sapiens (Human)
Description:
P25116
Residue:
425
Sequence:
MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEEKNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLNIMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTAAFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLKEQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSSAVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVSSISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIYKKLLT
Inhibitor
Name:
BDBM50202073
Synonyms:
(3R,3aS,4S,4aR,7R,8aR,9aR)-decahydro-7-hydroxy-3-methyl-4-[(E)-2-[5-[3-(trifluoromethyl)phenyl]-2-pyridinyl]ethenyl]naphtho[2,3-c]furan-1(3H)-one | CHEMBL218933
Type:
Small organic molecule
Emp. Form.:
C27H28F3NO3
Mol. Mass.:
471.5113
SMILES:
C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](\C=C\c3ccc(cn3)-c3cccc(c3)C(F)(F)F)[C@H]12 |r|