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Target
Proteinase-activated receptor 1
Ligand
BDBM50386391
Substrate
n/a
Meas. Tech.
ChEMBL_1849646 (CHEMBL4350187)
IC50
794±n/a nM
Citation
 Gandhi, DM; Rosas, R; Greve, E; Kentala, K; D-R Diby, N; Snyder, VA; Stephans, A; Yeung, THW; Subramaniam, S; DiMilo, E; Kurtenbach, KE; Arnold, LA; Weiler, H; Dockendorff, C The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability. Bioorg Med Chem 27:3788-3796 (2019) [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:
BDBM50386391
Synonyms:
CHEMBL1411333
Type:
Small organic molecule
Emp. Form.:
C17H17BrN2O2
Mol. Mass.:
361.233
SMILES:
CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1
Structure:
Search PDB for entries with ligand similarity: