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Target
Proteinase-activated receptor 1
Ligand
BDBM398063
Substrate
n/a
Meas. Tech.
PAR-1 FLIPR Assay
IC50
25.3±n/a nM
Citation
 Yang, Z; Dong, G; Maletic, M Preparation and use of 7a-heterocycle substituted-6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists US Patent  US10322140 Publication Date 6/18/2019 
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:
BDBM398063
Synonyms:
2-(6-((E)-2- ((3R,3aS,4R,5S,7aR)- 7a-(5-(tert-butyl)-1- methyl-1H-pyrazol-3- yl)-6,6-difluoro-3,5- dimethyl-1- oxooctahydroisobenzo furan-4-yl)vinyl) pyridin-3- yl)benzonitrile | US10322140, Example 10
Type:
Small organic molecule
Emp. Form.:
C33H36F2N4O2
Mol. Mass.:
558.6613
SMILES:
C[C@H]1OC(=O)[C@@]2(CC(F)(F)[C@@H](C)[C@H](\C=C\c3ccc(cn3)-c3cccc(C)c3C#N)[C@H]12)c1cc(n(C)n1)C(C)(C)C |r|
Structure:
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