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Target
Platelet-activating factor acetylhydrolase
Ligand
BDBM50197654
Substrate
n/a
Meas. Tech.
ChEMBL_1619621 (CHEMBL3861790)
IC50
3900±n/a nM
Citation
 Woolford, AJ; Day, PJ; Bénéton, V; Berdini, V; Coyle, JE; Dudit, Y; Grondin, P; Huet, P; Lee, LY; Manas, ES; McMenamin, RL; Murray, CW; Page, LW; Patel, VK; Potvain, F; Rich, SJ; Sang, Y; Somers, DO; Trottet, L; Wan, Z; Zhang, X Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA J Med Chem 59:10738-10749 (2016) [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:
BDBM50197654
Synonyms:
CHEMBL3930398
Type:
Small organic molecule
Emp. Form.:
C18H21FN2O4S
Mol. Mass.:
380.434
SMILES:
Fc1ccc(OCCN2CC(CC2=O)C2CCS(=O)(=O)CC2)cc1C#N
Structure:
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