Target
Proteinase-activated receptor 1
Ligand
BDBM50077771
Substrate
n/a
Meas. Tech.
ChEMBL_209265 (CHEMBL817562)
IC50
4000±n/a nM
Citation
 McComsey, DFHawkins, MJAndrade-Gordon, PAddo, MFOksenberg, DMaryanoff, BE Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1). Bioorg Med Chem Lett 9:1423-8 (1999) [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:
BDBM50077771
Synonyms:
5-[(E)-3-(4-Methoxy-phenyl)-acryloylamino]-1H-[1,2,4]triazole-3-carboxylic acid {(S)-1-[(S)-1-((S)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-4-guanidino-butylcarbamoyl]-2-cyclohexyl-ethyl}-amide | CHEMBL33033
Type:
Small organic molecule
Emp. Form.:
C37H49N11O6
Mol. Mass.:
743.8551
SMILES:
COc1ccc(C=CC(=O)Nc2nnc([nH]2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 |w:6.5|
Structure:
Search PDB for entries with ligand similarity: