Bookmark and Share
BioAssay: AID 260524

Repression of transcriptional activity in ERRgamma transfected HeLa cell luciferase assay at 1 uM

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity. ..more
_
   
 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 260524
Data Source: ChEMBL (333992)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
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 Compound:
Description:
Title: Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.

Abstract: The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.
(PMID: 16307879)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Functional
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
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)
Data Table ( Complete ):     View All Data
Classification
PageFrom: