Target
Proteinase-activated receptor 1
Ligand
BDBM50181509
Substrate
n/a
Meas. Tech.
ChEMBL_1585283 (CHEMBL3821546)
IC50
60±n/a nM
Citation
 Eggert, EHillig, RCKoehr, SStöckigt, DWeiske, JBarak, NMowat, JBrumby, TChrist, CDTer Laak, ALang, TFernandez-Montalvan, AEBadock, VWeinmann, HHartung, IVBarsyte-Lovejoy, DSzewczyk, MKennedy, SLi, FVedadi, MBrown, PJSanthakumar, VArrowsmith, CHStellfeld, TStresemann, C Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2. J Med Chem 59:4578-600 (2016) [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:
BDBM50181509
Synonyms:
CHEMBL3817930
Type:
Small organic molecule
Emp. Form.:
C21H19Cl2FN6O2
Mol. Mass.:
477.319
SMILES:
CCN(C1CN(N=C1c1ccc(Cl)cc1)C(\Nc1ccc(F)c(Cl)c1)=N/C#N)C(=O)CO |c:6|
Structure:
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