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BioAssay: AID 739337

Inhibition of recombinant human sEH expressed in Escherichia coli assessed as inhibition of substrate PHOME hydrolysis to 6-methoxy-2-naphthaldehyde at 10 ug/ml after 5 mins by fluorescence assay

A series of novel 4-substituted benzoxazolone derivatives was synthesized, characterized and evaluated as human soluble epoxide hydrolase (sEH) inhibitors and anti-inflammatory agents. Some compounds showed moderate sEH inhibitory activities in vitro, and two novel compounds, 3g and 4j, exhibited the highest activities with IC50 values of 1.72 and 1.07 muM, respectively. Structure-activity more ..
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 Tested Compounds
 Tested Compounds
All(29)
 
 
Unspecified(29)
 
 
 Tested Substances
 Tested Substances
All(29)
 
 
Unspecified(29)
 
 
 Related BioAssays
 Related BioAssays
AID: 739337
Data Source: ChEMBL (951905)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-09-05

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Bifunctional epoxide hydrolase 2; Includes: RecName: Full=Cytosolic epoxide hydrolase 2; Short=CEH; AltName: Full=Epoxide hydratase; AltName: Full=Soluble epoxide hydrolase; Short=SEH; Includes: RecName: Full=Lipid-phosphate phosphatase
Description ..   
Protein Family: HAD_like
Comment ..   

Gene:EPHX2     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Synthesis and biological activity of 4-substituted benzoxazolone derivatives as a new class of sEH inhibitors with high anti-inflammatory activity in vivo.

Abstract: A series of novel 4-substituted benzoxazolone derivatives was synthesized, characterized and evaluated as human soluble epoxide hydrolase (sEH) inhibitors and anti-inflammatory agents. Some compounds showed moderate sEH inhibitory activities in vitro, and two novel compounds, 3g and 4j, exhibited the highest activities with IC50 values of 1.72 and 1.07 muM, respectively. Structure-activity relationships (SARs) revealed that introduction of a lipophilic amino acid resulted in an obvious increase in the sEH inhibitory activity, especially for derivatives containing a phenyl (3d, IC(50) = 2.67 muM), pyrrolidine (3g, IC(50) = 1.72 muM), or sulfhydryl group (3e, IC(50)=3.02 muM). Several compounds (3a-3g) were tested in vivo using a xylene-induced ear edema mouse model. Three compounds (3d, 3f, and 3g) showed strong anti-inflammatory activities in vivo which were higher than that of Chlorzoxazone, a reference drug widely used in the clinic. Our investigation provided a novel type of sEH inhibitor and anti-inflammatory agent that may lead to the discovery of a potential candidate for clinical use.
(PMID: 23489630)
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)
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Classification
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