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BioAssay: AID 630922

Agonist activity at human ERRalpha ligand binding domain expressed in human 293FT cells coexpressing Gal4 DNA binding domain assessed as increased transcriptional activity at 10 uM after 24 hrs by dual luciferase reporter gene assay relative to control

The nuclear estrogen-related receptor alpha (ERRalpha) plays a central role in the regulation of expression of the genes involved in mitochondrial biogenesis and oxidative metabolism. We have successfully identified a series of pyrido[1,2-a]pyrimidin-4-ones as new agonists enhancing the transcriptional functions of ERRalpha. The compounds potently elevated the mRNA levels and the protein levels of ERRalpha downstream targets. Consequently, the compounds improved the glucose and fatty acid uptake in C2C12 muscle cells. ..more
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 Tested Compounds
 Tested Compounds
All(9)
 
 
Active(1)
 
 
Inactive(5)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Active(1)
 
 
Inactive(5)
 
 
Unspecified(3)
 
 
AID: 630922
Data Source: ChEMBL (788370)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Steroid hormone receptor ERR1; AltName: Full=Estrogen receptor-like 1; AltName: Full=Estrogen-related receptor alpha; Short=ERR-alpha; AltName: Full=Nuclear receptor subfamily 3 group B member 1
Description ..   
Protein Family: The ligand binding domain of estrogen receptor-related nuclear receptors
Comment ..   

Gene:ESRRA     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Identification of pyrido[1,2-alpha]pyrimidine-4-ones as new molecules improving the transcriptional functions of estrogen-related receptor alpha.

Abstract: The nuclear estrogen-related receptor alpha (ERRalpha) plays a central role in the regulation of expression of the genes involved in mitochondrial biogenesis and oxidative metabolism. We have successfully identified a series of pyrido[1,2-a]pyrimidin-4-ones as new agonists enhancing the transcriptional functions of ERRalpha. The compounds potently elevated the mRNA levels and the protein levels of ERRalpha downstream targets. Consequently, the compounds improved the glucose and fatty acid uptake in C2C12 muscle cells.
(PMID: 21958216)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: cell-based format

Target Type: Target is a single protein chain

Result Definitions
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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
6FC activity commentFC activity commentString
7FC standard flagFC standard flagInteger
8FC qualifierFC qualifierString
9FC published valueFC published valueFloat
10FC standard valueFC standard valueFloat

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