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BioAssay: AID 653690

Antagonist activity at human LXRbeta-LBD expressed in HEK293 cells co-expressing GAL4-DBD assessed as inhibition of luciferase activity by beta-galactosidase reporter gene assay

Structural modification of a series of dual LXRalpha/beta agonists led to the identification of a new class of LXRbeta partial agonists. An X-ray co-crystal structure shows that a representative member of this series, pyrrole 5, binds to LXRbeta with a reversed orientation compared to 1. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 653690
Data Source: ChEMBL (810762)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    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..
BioActive Compound: 1
Description:
Title: Discovery of a new binding mode for a series of liver X receptor agonists.

Abstract: Structural modification of a series of dual LXRalpha/beta agonists led to the identification of a new class of LXRbeta partial agonists. An X-ray co-crystal structure shows that a representative member of this series, pyrrole 5, binds to LXRbeta with a reversed orientation compared to 1.
(PMID: 22406115)
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: HEK293
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

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