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BioAssay: AID 271716

Binding affinity to human SF1 relative to 3-Hexyl-1-phenylamino-2-phenyl-cis-bicyclo[3.3.0]oct-2-ene1 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(15)
 
 
Unspecified(15)
 
 
 Tested Substances
 Tested Substances
All(15)
 
 
Unspecified(15)
 
 
 Related BioAssays
 Related BioAssays
AID: 271716
Data Source: ChEMBL (408055)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Steroidogenic factor 1; Short=SF-1; Short=STF-1; AltName: Full=Adrenal 4-binding protein; AltName: Full=Fushi tarazu factor homolog 1; AltName: Full=Nuclear receptor subfamily 5 group A member 1; AltName: Full=Steroid hormone receptor Ad4BP
Description ..   
Protein Family: The ligand binding domain of nuclear receptor steroidogenic factor 1, a member of nuclear receptor superfamily
Comment ..   

Gene:NR5A1     Related Protein 3D Structures     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 - 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
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)
Data Table ( Complete ):     View All Data
Classification
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