Target
Platelet-activating factor acetylhydrolase
Ligand
BDBM50117778
Substrate
n/a
Meas. Tech.
ChEBML_156373
IC50
0.170000±n/a nM
Citation
 Blackie, JABloomer, JCBrown, MJCheng, HYElliott, RLHammond, BHickey, DMIfe, RJLeach, CALewis, VAMacphee, CHMilliner, KJMoores, KEPinto, ILSmith, SAStansfield, IGStanway, SJTaylor, MATheobald, CJWhittaker, CM The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man. Bioorg Med Chem Lett 12:2603-6 (2002) [PubMed]  Article 
Target
Name:
Platelet-activating factor acetylhydrolase
Synonyms:
1-alkyl-2-acetylglycerophosphocholine esterase | 2-acetyl-1-alkylglycerophosphocholine esterase | LDL-PLA(2) | LDL-associated phospholipase A2 | PAF 2-acylhydrolase | PAF acetylhydrolase | PAFAH | PAFA_HUMAN | PLA2G7 | Platelet-activating factor acetylhydrolase
Type:
PROTEIN
Mol. Mass.:
50084.41
Organism:
Homo sapiens (Human)
Description:
ChEMBL_156212
Residue:
441
Sequence:
MVPPKLHVLFCLCGCLAVVYPFDWQYINPVAHMKSSAWVNKIQVLMAAASFGQTKIPRGNGPYSVGCTDLMFDHTNKGTFLRLYYPSQDNDRLDTLWIPNKEYFWGLSKFLGTHWLMGNILRLLFGSMTTPANWNSPLRPGEKYPLVVFSHGLGAFRTLYSAIGIDLASHGFIVAAVEHRDRSASATYYFKDQSAAEIGDKSWLYLRTLKQEEETHIRNEQVRQRAKECSQALSLILDIDHGKPVKNALDLKFDMEQLKDSIDREKIAVIGHSFGGATVIQTLSEDQRFRCGIALDAWMFPLGDEVYSRIPQPLFFINSEYFQYPANIIKMKKCYSPDKERKMITIRGSVHQNFADFTFATGKIIGHMLKLKGDIDSNVAIDLSNKASLAFLQKHLGLHKDFDQWDCLIEGDDENLIPGTNINTTNQHIMLQNSSGIEKYN
  
Inhibitor
Name:
BDBM50117778
Synonyms:
2-[2-(4-Fluoro-benzylsulfanyl)-5-(1-methyl-1H-pyrazol-4-ylmethyl)-4-oxo-4H-pyrimidin-1-yl]-N-(2-piperidin-1-yl-ethyl)-N-(4'-trifluoromethyl-biphenyl-4-ylmethyl)-acetamide | CHEMBL314768
Type:
Small organic molecule
Emp. Form.:
C39H40F4N6O2S
Mol. Mass.:
732.833
SMILES:
Cn1cc(Cc2cn(CC(=O)N(CCN3CCCCC3)Cc3ccc(cc3)-c3ccc(cc3)C(F)(F)F)c(SCc3ccc(F)cc3)nc2=O)cn1
Structure:
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