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BioAssay: AID 643990

Inhibition of recombinant N-terminus hexahistidine-tagged human lipoprotein-associated phospholipase A2 expressed in Escherichia coli using 2-thio-PAF as substrate preincubated for 20 mins measured 1 hr post substrate addition by spectrophotometric analysis in presence of 20 uM ZnCl2

AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA(2) did not change. Subsequent metal screening experiments determined the inhibition to be Zn(2+) dependent. Structure-activity relationship studies indicated the presence of the 4-hydroxy group to be critical and selected substituted phenyl, polycyclic, and cycloaliphatic amides of xanthurenic acid to be well tolerated. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 643990
Data Source: ChEMBL (801438)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Platelet-activating factor acetylhydrolase; Short=PAF acetylhydrolase; AltName: Full=1-alkyl-2-acetylglycerophosphocholine esterase; AltName: Full=2-acetyl-1-alkylglycerophosphocholine esterase; AltName: Full=Group-VIIA phospholipase A2; Short=gVIIA-PLA2; AltName: Full=LDL-associated phospholipase A2; Short=LDL-PLA(2); AltName: Full=PAF 2-acylhydrolase; Flags: Precursor
Description ..   
Protein Family: Platelet-activating factor acetylhydrolase, isoform II
Comment ..   

Gene:PLA2G7     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).

Abstract: AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA(2) did not change. Subsequent metal screening experiments determined the inhibition to be Zn(2+) dependent. Structure-activity relationship studies indicated the presence of the 4-hydroxy group to be critical and selected substituted phenyl, polycyclic, and cycloaliphatic amides of xanthurenic acid to be well tolerated.
(PMID: 22217870)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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