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Target
Proteinase-activated receptor 1
Ligand
BDBM50222014
Substrate
n/a
Meas. Tech.
ChEMBL_446321 (CHEMBL895431)
IC50
762±n/a nM
Citation
 Chelliah, MV; Chackalamannil, S; Xia, Y; Eagen, K; Clasby, MC; Gao, X; Greenlee, W; Ahn, HS; Agans-Fantuzzi, J; Boykow, G; Hsieh, Y; Bryant, M; Palamanda, J; Chan, TM; Hesk, D; Chintala, M Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists. J Med Chem 50:5147-60 (2007) [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:
BDBM50222014
Synonyms:
(1R,3aR,4aS,8aS,9S,9aS)-decahydro-6-methyl-1-methyl-9-[(e)-2-[5-[3-(trifluoromethyl)phenyl]-2-pyridinyl]ethenyl]furo-[3,4-g]isoquinolin-3(1H)-one | CHEMBL389834
Type:
Small organic molecule
Emp. Form.:
C27H29F3N2O2
Mol. Mass.:
470.5266
SMILES:
C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C)CC[C@H]3[C@H](\C=C\c3ccc(cn3)-c3cccc(c3)C(F)(F)F)[C@H]12
Structure:
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