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Target
Proteinase-activated receptor 1
Ligand
BDBM50222015
Substrate
n/a
Meas. Tech.
ChEMBL_446321 (CHEMBL895431)
IC50
10.5±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:
BDBM50222015
Synonyms:
(1R,3aR,4aS,8aS,9S,9aS)-decahydro-1-methyl-3-oxo-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]-furo[3,4-g]isoquinoline-6(3H)-carboxylic acid ethyl ester | CHEMBL390630
Type:
Small organic molecule
Emp. Form.:
C28H31FN2O4
Mol. Mass.:
478.5551
SMILES:
CCOC(=O)N1CC[C@@H]2[C@H](C[C@@H]3[C@@H]([C@@H](C)OC3=O)[C@H]2\C=C\c2ccc(cn2)-c2cccc(F)c2)C1
Structure:
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