Bookmark and Share
BioAssay: AID 631006

Agonist activity at in mouse C2C12 cells ERRalpha assessed as increase in PDK4 protein level after 24 hrs by Western blot analysis

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
_
   
 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 631006
Data Source: ChEMBL (788454)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
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
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Assay Cell Type: C2C12

ChEMBL Target ID: 104376

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)
Classification
PageFrom: