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BioAssay: AID 271722

Binding affinity to human SF1 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(23)
 
 
Active(16)
 
 
Unspecified(7)
 
 
 Tested Substances
 Tested Substances
All(23)
 
 
Active(16)
 
 
Unspecified(7)
 
 
 Related BioAssays
 Related BioAssays
AID: 271722
Data Source: ChEMBL (408061)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-11-18

Data Table ( Complete ):           Active    All
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..
BioActive Compounds: 16
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)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 100828

ChEMBL Target Type: Target is a single protein chain

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6EC50 activity commentEC50 activity commentString
7EC50 standard flagEC50 standard flagInteger
8EC50 qualifierEC50 qualifierString
9EC50 published valueEC50 published valueFloatμM
10EC50 standard valueEC50 standard valueFloatnM
11EC50 binding domainsEC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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