Target
Proteinase-activated receptor 1
Ligand
BDBM50129483
Substrate
n/a
Meas. Tech.
ChEBML_209261
IC50
2000±n/a nM
Citation
 Zhang, HCWhite, KBMcComsey, DFAddo, MFAndrade-Gordon, PDerian, CKOksenberg, DMaryanoff, BE High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus. Bioorg Med Chem Lett 13:2199-203 (2003) [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:
BDBM50129483
Synonyms:
4-Amino-2-[(S)-2-{3-[1-(2,6-dichloro-benzyl)-3-pyrrolidin-1-ylmethyl-1H-indol-4-yl]-ureido}-3-(3,4-difluoro-phenyl)-propionylamino]-N-(2-pyrrolidin-1-yl-ethyl)-butyramide | CHEMBL70013
Type:
Small organic molecule
Emp. Form.:
C40H48Cl2F2N8O3
Mol. Mass.:
797.764
SMILES:
NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2n(Cc3c(Cl)cccc3Cl)cc(CN3CCCC3)c12)C(=O)NCCN1CCCC1
Structure:
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