Target
Proteinase-activated receptor 1
Ligand
BDBM230679
Substrate
n/a
Meas. Tech.
FLIPR Assay
IC50
38.6±n/a nM
Citation
 Mandal, MBlizzard, TAChen, HChobanian, HGuo, YPio, BWu, ZBiftu, TGreenlee, WJZhu, JZ Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists US Patent  US9340530 Publication Date 5/17/2016 
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:
BDBM230679
Synonyms:
US9340530, 17
Type:
Small organic molecule
Emp. Form.:
C32H35F2N3O5
Mol. Mass.:
579.6342
SMILES:
C[C@H]1OC(=O)[C@@]2(CC(F)(F)C(C)[C@H](\C=C\c3ccc(cn3)-c3ccccc3C#N)C12)C1(O)CN(C1)C(=O)OC(C)(C)C |r|
Structure:
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