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Target
Proteinase-activated receptor 1
Ligand
BDBM50222023
Substrate
n/a
Meas. Tech.
ChEMBL_446321 (CHEMBL895431)
IC50
600±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:
BDBM50222023
Synonyms:
CHEMBL389382 | ethyl (4aS,5S,5aS,6R,8aR,9aS)-5-[(E)-2-[5-(2-methylphenyl)-2-pyridinyl]ethenyl]-decahydro-6-methyl-8-oxofuro[3,4-g]quinoline-1(2H)-carboxylate
Type:
Small organic molecule
Emp. Form.:
C29H34N2O4
Mol. Mass.:
474.5913
SMILES:
CCOC(=O)N1CCC[C@@H]2[C@@H]1C[C@@H]1[C@@H]([C@@H](C)OC1=O)[C@H]2\C=C\c1ccc(cn1)-c1ccccc1C
Structure:
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