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BioAssay: AID 263922

Transactivation of RXRbeta in CV1 cells by cotransfection assay

A new structurally simple series of potent lipophilic aza-retinoids RXR agonists has been developed. SAR studies for the N-alkyl-azadienoic acids described here demonstrate that the RXR activity profile is sensitive to the N-alkyl chain length. Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series. ..more
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 Tested Compounds
 Tested Compounds
All(21)
 
 
Active(15)
 
 
Inactive(6)
 
 
 Tested Substances
 Tested Substances
All(21)
 
 
Active(15)
 
 
Inactive(6)
 
 
AID: 263922
Data Source: ChEMBL (349698)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-08-25

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Retinoic acid receptor RXR-beta; AltName: Full=Nuclear receptor subfamily 2 group B member 2; AltName: Full=Retinoid X receptor beta
Description ..   
Protein Family: The ligand binding domain of the retinoid X receptor and Ultraspiracle, members of nuclear receptor superfamily
Comment ..   

Gene:RXRB     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 15
Description:
Title: Aza-retinoids as novel retinoid X receptor-specific agonists.

Abstract: A new structurally simple series of potent lipophilic aza-retinoids RXR agonists has been developed. SAR studies for the N-alkyl-azadienoic acids described here demonstrate that the RXR activity profile is sensitive to the N-alkyl chain length. Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series.
(PMID: 16364638)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
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
BAO: Assay Format: cell-based format
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2EC50 activity commentEC50 activity commentString
3EC50 standard flagEC50 standard flagInteger
4EC50 qualifierEC50 qualifierString
5EC50 published valueEC50 published valueFloatnM
6EC50 standard valueEC50 standard valueFloatnM
7EC50 binding domainsEC50 binding domainsString

* Activity Concentration.

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