Target
Proteinase-activated receptor 1
Ligand
BDBM135850
Substrate
n/a
Meas. Tech.
Binding Assay
pH
7.5±n/a
IC50
1700±n/a nM
Comments
extracted
Citation
 Heinelt, UWehner, VHerrmann, MSchoenafinger, KSteinhagen, H Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments US Patent  US8853206 Publication Date 10/7/2014 
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:
BDBM135850
Synonyms:
US8853206, 72
Type:
Small organic molecule
Emp. Form.:
C27H39N6O4
Mol. Mass.:
511.6358
SMILES:
CCOc1nn2c(NC)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(c3)C(C)(C)C)c2c(C)c1C
Structure:
Search PDB for entries with ligand similarity: