Target
Proteinase-activated receptor 1
Ligand
BDBM50202070
Substrate
n/a
Meas. Tech.
ChEMBL_423382 (CHEMBL909901)
IC50
28±n/a nM
Citation
 Clasby, MCChackalamannil, SCzarniecki, MDoller, DEagen, KGreenlee, WKao, GLin, YTsai, HXia, YAhn, HSAgans-Fantuzzi, JBoykow, GChintala, MFoster, CSmith-Torhan, AAlton, KBryant, MHsieh, YLau, JPalamanda, J Metabolism-based identification of a potent thrombin receptor antagonist. J Med Chem 50:129-38 (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:
BDBM50202070
Synonyms:
(3R,3aS,4S,4aS,8R,8aS,9aR)-decahydro-8-hydroxy-3-methyl-4-[(E)-2-[5-[3-(trifluoromethyl)phenyl]-2-pyridinyl]ethenyl]naphtho[2,3-c]furan-1(3H)-one | CHEMBL374265
Type:
Small organic molecule
Emp. Form.:
C27H28F3NO3
Mol. Mass.:
471.5113
SMILES:
C[C@H]1OC(=O)[C@@H]2C[C@@H]3[C@H](O)CCC[C@H]3[C@H](\C=C\c3ccc(cn3)-c3cccc(c3)C(F)(F)F)[C@H]12 |r|
Structure:
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