Target
Proteinase-activated receptor 1
Ligand
BDBM50179575
Substrate
n/a
Meas. Tech.
ChEMBL_340412 (CHEMBL863749)
IC50
275±n/a nM
Citation
 Clasby, MCChackalamannil, SCzarniecki, MDoller, DEagen, KGreenlee, WJLin, YTsai, HXia, YAhn, HSAgans-Fantuzzi, JBoykow, GChintala, MFoster, CBryant, MLau, J Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists. Bioorg Med Chem Lett 16:1544-8 (2006) [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:
BDBM50179575
Synonyms:
(+/-)-tert-butyl 2-(2-(2-((3R,3aS,4S,4aR,8aS,9aR)-3-methyl-1-oxo-dodecahydronaphtho[2,3-c]furan-4-yl)vinyl)quinolin-6-yloxy)ethylcarbamate | CHEMBL381506
Type:
Small organic molecule
Emp. Form.:
C31H40N2O5
Mol. Mass.:
520.6597
SMILES:
C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](C=Cc3ccc4cc(OCCNC(=O)OC(C)(C)C)ccc4n3)[C@H]12 |w:15.16|
Structure:
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