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BioAssay: AID 271715

Binding affinity to human LRH1 relative to 3-(E-Oct-4-en-4-yl)-1-phenylamino-2-phenyl-cis-bicyclo[3.3.0]oct-2-ene by FRET-based peptide recruitment assay

We report the identification of substituted cis-bicyclo[3.3.0]-oct-2-enes as small molecule agonists of subfamily V orphan nuclear receptors (NR5A), liver receptor homolog-1 (LRH-1) and steroidogenic factor-1 (SF-1). Using fluorescence resonance energy transfer (FRET)-based biochemical assays, compound 5a (GSK8470) was identified as a high-affinity ligand for LRH-1 and SF-1. In liver cells, 5a more ..
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 Tested Compounds
 Tested Compounds
All(17)
 
 
Unspecified(17)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Unspecified(17)
 
 
 Related BioAssays
 Related BioAssays
AID: 271715
Data Source: ChEMBL (408054)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-11-18

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Nuclear receptor subfamily 5 group A member 2; AltName: Full=Alpha-1-fetoprotein transcription factor; AltName: Full=B1-binding factor; Short=hB1F; AltName: Full=CYP7A promoter-binding factor; AltName: Full=Hepatocytic transcription factor; AltName: Full=Liver receptor homolog 1; Short=LRH-1
Description ..   
Protein Family: The ligand binding domain of the liver receptor homolog-1, a member of nuclear receptor superfamily,
Comment ..   

Gene:NR5A2          More BioActivity Data..
Tested Compounds:
Description:
Title: Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.

Abstract: We report the identification of substituted cis-bicyclo[3.3.0]-oct-2-enes as small molecule agonists of subfamily V orphan nuclear receptors (NR5A), liver receptor homolog-1 (LRH-1) and steroidogenic factor-1 (SF-1). Using fluorescence resonance energy transfer (FRET)-based biochemical assays, compound 5a (GSK8470) was identified as a high-affinity ligand for LRH-1 and SF-1. In liver cells, 5a increased the expression of the LRH-1 target gene small heterodimer partner (SHP). Synthesis of analogues modified at three positions led to the development of compounds with functional selectivity between LRH-1 and SF-1.
(PMID: 17154495)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 100827

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Efficacy activity commentEfficacy activity commentString
2Efficacy standard flagEfficacy standard flagInteger
3Efficacy qualifierEfficacy qualifierString
4Efficacy published valueEfficacy published valueFloat%
5Efficacy standard valueEfficacy standard valueFloat%

Data Table (Concise)
Classification
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