Target
Proteinase-activated receptor 1
Ligand
BDBM50261116
Substrate
n/a
Meas. Tech.
ChEMBL_556010 (CHEMBL964660)
Ki
3.7±n/a nM
Citation
 Chackalamannil, SWang, YGreenlee, WJHu, ZXia, YAhn, HSBoykow, GHsieh, YPalamanda, JAgans-Fantuzzi, JKurowski, SGraziano, MChintala, M Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem 51:3061-4 (2008) [PubMed]  Article 
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:
BDBM50261116
Synonyms:
CHEMBL453277 | ethyl methyl((1R,3aR,4aR,6R,8aR,9S,9aS)-1-methyl-3-oxo-9-((E)-2-(5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)vinyl)-dodecahydronaphtho[2,3-c]furan-6-yl)carbamate
Type:
Small organic molecule
Emp. Form.:
C31H35F3N2O4
Mol. Mass.:
556.6158
SMILES:
CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@@H]3[C@@H]([C@@H](C)OC3=O)[C@H]2\C=C\c2ccc(cn2)-c2cccc(c2)C(F)(F)F)C1 |r|
Structure:
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