Target
Proteinase-activated receptor 1
Ligand
BDBM50257997
Substrate
n/a
Meas. Tech.
ChEMBL_1690092 (CHEMBL4040662)
IC50
>100000±n/a nM
Citation
 Liu, JSun, BZhao, XXing, JGao, YChang, WJi, JZheng, HCui, CJi, ALou, H Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide. J Med Chem 60:7166-7185 (2017) [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:
BDBM50257997
Synonyms:
CHEMBL4096709
Type:
Small organic molecule
Emp. Form.:
C28H31FN2O4
Mol. Mass.:
478.5551
SMILES:
[H][C@@]12COC(=O)[C@@]1([H])[C@]1(C)CC[C@H](OC(N)=O)[C@](C)(\C=C\c3ccc(cn3)-c3cccc(F)c3)[C@@]1([H])CC2 |r|
Structure:
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