Inverse agonist activity at human ERRalpha ligand binding domain expressed in human 293FT cells coexpressing with Gal4 DNA binding domain assessed as inhibition of transcritptional activity at 10 uM after 24 hrs by dual luciferase reporter gene assay - BioAssay Summary
The nuclear estrogen-related receptor ## (ERR##) 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 ERR##. The compounds potently elevated the mRNA levels and the protein levels of ERR## 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(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(2)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 630996
Data Source: ChEMBL (788444)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-05-15

Data Table (Complete):           Active    All
Target
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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
BioActive Compounds: 2
Description:
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Title: Identification of pyrido[1,2-##]pyrimidine-4-ones as new molecules improving the transcriptional functions of estrogen-related receptor ##.

Abstract: The nuclear estrogen-related receptor ## (ERR##) 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 ERR##. The compounds potently elevated the mRNA levels and the protein levels of ERR## downstream targets. Consequently, the compounds improved the glucose and fatty acid uptake in C2C12 muscle cells.
(PMID: 21958216)
Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 10133

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat

Data Table (Concise)
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Classification
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