Reaction Details
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Proteinase-activated receptor 1
Ligand
BDBM50173419
Substrate
n/a
Meas. Tech.
ChEMBL_320796 (CHEMBL884751)
Ki
2.7±n/a nM
Citation
Chackalamannil, S; Xia, Y; Greenlee, WJ; Clasby, M; Doller, D; Tsai, H; Asberom, T; Czarniecki, M; Ahn, HS; Boykow, G; Foster, C; Agans-Fantuzzi, J; Bryant, M; Lau, J; Chintala, M Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. J Med Chem 48:5884-7 (2005) [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:
BDBM50173419
Synonyms:
(3R,3aS,4S,4aR,8aS,9aR)-3-Methyl-4-{(E)-2-[5-(3-trifluoromethyl-phenyl)-pyridin-2-yl]-vinyl}-decahydro-naphtho[2,3-c]furan-1-one | (3R,3aS,4S,4aR,8aS,9aR)-3-methyl-4-(2-(5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)vinyl)-decahydronaphtho[2,3-c]furan-1(3H)-one | (3R,3aS,4S,4aR,8aS,9aR,E)-3-methyl-4-(2-(5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)vinyl)-decahydronaphtho[2,3-c]furan-1(3H)-one | CHEMBL371069 | SCH-205831
Type:
Small organic molecule
Emp. Form.:
C27H28F3NO2
Mol. Mass.:
455.5119
SMILES:
C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](\C=C\c3ccc(cn3)-c3cccc(c3)C(F)(F)F)[C@H]12
Structure:
