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BioAssay: AID 304535

Effect on interaction between ERRgamma ligand binding domain and RIP140 by FRET assay

The estrogen-related receptor alpha (ERRalpha) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRalpha have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRgamma. The results suggest that ERRalpha may be intractable as a direct target for pharmacologic activation. ..more
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Inactive(18)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Inactive(18)
 
 
 Related BioAssays
 Related BioAssays
AID: 304535
Data Source: ChEMBL (452561)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-11-19

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Estrogen-related receptor gamma; AltName: Full=ERR gamma-2; AltName: Full=Estrogen receptor-related protein 3; AltName: Full=Nuclear receptor subfamily 3 group B member 3
Description ..   
Protein Family: The ligand binding domain of estrogen receptor-related nuclear receptors
Comment ..   

Gene:ESRRG     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.

Abstract: The estrogen-related receptor alpha (ERRalpha) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRalpha have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRgamma. The results suggest that ERRalpha may be intractable as a direct target for pharmacologic activation.
(PMID: 18052088)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 11255

ChEMBL Target Type: Target is a single protein chain

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)
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