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Target
Proteinase-activated receptor 1
Ligand
BDBM230729
Substrate
n/a
Meas. Tech.
FLIPR Assay
IC50
2.9±n/a nM
Citation
 Mandal, M; Blizzard, TA; Chen, H; Chobanian, H; Guo, Y; Pio, B; Wu, Z; Biftu, T; Greenlee, WJ; Zhu, 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:
BDBM230729
Synonyms:
US9340530, 64
Type:
Small organic molecule
Emp. Form.:
C32H26F2N4O3
Mol. Mass.:
552.5706
SMILES:
[H][C@@]12[C@@H](C)OC(=O)[C@@]1(CC(F)(F)[C@@]([H])(C)[C@@H]2\C=C\c1ccc(cn1)-c1ccccc1C#N)NC(=O)c1ccc(cc1)C#N |r|
Structure:
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