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Target
Proteinase-activated receptor 1
Ligand
BDBM50380012
Substrate
n/a
Meas. Tech.
ChEMBL_810573
IC50
13±n/a nM
Citation
 Chelliah, MV; Chackalamannil, S; Xia, Y; Eagen, K; Greenlee, WJ; Ahn, HS; Agans-Fantuzzi, J; Boykow, G; Hsieh, Y; Bryant, M; Chan, TM; Chintala, M Discovery of nor-seco himbacine analogs as thrombin receptor antagonists. Bioorg Med Chem Lett 22:2544-9 (2012) [PubMed]  Article  BDB Entry
Target
Name:
Proteinase-activated receptor 1
Synonyms:
Coagulation factor II receptor | PAR-1 | Proteinase activated receptor 1 | Proteinase-activated receptor 1 (PAR-1) | 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:
BDBM50380012
Synonyms:
CHEMBL2012497
Type:
Small organic molecule
Emp. Form.:
C25H27Cl2NO2
Mol. Mass.:
444.393
SMILES:
CC[C@@H]1[C@@H](C)C[C@@H]2[C@@H]([C@@H](C)OC2=O)[C@H]1\C=C\c1ccc(cn1)-c1cccc(Cl)c1Cl |r|
Structure:
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