Target
Proteinase-activated receptor 1
Ligand
BDBM50173444
Substrate
n/a
Meas. Tech.
ChEMBL_321545 (CHEMBL881483)
IC50
900±n/a nM
Citation
 Chackalamannil, SXia, YGreenlee, WJClasby, MDoller, DTsai, HAsberom, TCzarniecki, MAhn, HSBoykow, GFoster, CAgans-Fantuzzi, JBryant, MLau, JChintala, M Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. J Med Chem 48:5884-7 (2005) [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:
BDBM50173444
Synonyms:
(3R,3aS,4S,4aR,8aS,9aR)-4-[(E)-2-(6-Benzyl-pyridin-2-yl)-vinyl]-3-methyl-decahydro-naphtho[2,3-c]furan-1-one | CHEMBL197248
Type:
Small organic molecule
Emp. Form.:
C27H31NO2
Mol. Mass.:
401.5405
SMILES:
C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](\C=C\c3cccc(Cc4ccccc4)n3)[C@H]12
Structure:
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