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BioAssay: AID 678570

Antagonist activity at LXRbeta in human HepG2 cells assessed as rightward shift in [3H]N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzenesulfonamide-induced triglyceride accumulation at 10 uM relative to control

The present report describes our efforts to convert an existing LXR agonist into an LXR antagonist using a structure-based approach. A series of benzenesulfonamides was synthesized based on structural modification of a known LXR agonist and was determined to be potent dual liver X receptor (LXR alpha/beta) ligands. Herein we report the identification of compound 54 as the first reported LXR antagonist that is suitable for pharmacological in vivo evaluation in rodents. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 678570
Data Source: ChEMBL (835709)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2014-08-26

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Oxysterols receptor LXR-beta; AltName: Full=Liver X receptor beta; AltName: Full=Nuclear receptor NER; AltName: Full=Nuclear receptor subfamily 1 group H member 2; AltName: Full=Ubiquitously-expressed nuclear receptor
Description ..   
Protein Family: The ligand binding domain of Liver X receptors, a family of nuclear receptors of ligand-activated transcription factors
Comment ..   

Gene:NR1H2     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Description:
Title: Discovery and optimization of a series of liver X receptor antagonists.

Abstract: The present report describes our efforts to convert an existing LXR agonist into an LXR antagonist using a structure-based approach. A series of benzenesulfonamides was synthesized based on structural modification of a known LXR agonist and was determined to be potent dual liver X receptor (LXR alpha/beta) ligands. Herein we report the identification of compound 54 as the first reported LXR antagonist that is suitable for pharmacological in vivo evaluation in rodents.
(PMID: 22901900)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Functional
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: HepG2
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1FC activity commentFC activity commentString
2FC standard flagFC standard flagInteger
3FC qualifierFC qualifierString
4FC published valueFC published valueFloat
5FC standard valueFC standard valueFloat

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