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BioAssay: AID 659501

Transactivation activity at glucocorticoid receptor in rat H4II-E cells assessed as induction of tyrosine aminotransferase relative to control

The introduction of A ring pyrazole modification to the hydrocortisone C-21 heteroaryl thioethers generated compounds with excellent transrepression potency (IL-8 inhibition) compared to their hydrocortisone analogs. However, the transcriptional transactivation activity of these compounds were considerably higher than the corresponding hydrocortisone analogs. Among all the compounds evaluated, a quinoxaline thioether modification demonstrated the best overall in vitro separation. ..more
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 Tested Compounds
 Tested Compounds
All(38)
 
 
Inconclusive(7)
 
 
Unspecified(31)
 
 
 Tested Substances
 Tested Substances
All(38)
 
 
Inconclusive(7)
 
 
Unspecified(31)
 
 
 Related BioAssays
 Related BioAssays
AID: 659501
Data Source: ChEMBL (816573)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Glucocorticoid receptor; Short=GR; AltName: Full=Nuclear receptor subfamily 3 group C member 1
Description ..   
Protein Family: Ligand binding domain of the glucocorticoid receptor, a member of the nuclear receptor superfamily
Comment ..   

Gene:NR3C1     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).

Abstract: The introduction of A ring pyrazole modification to the hydrocortisone C-21 heteroaryl thioethers generated compounds with excellent transrepression potency (IL-8 inhibition) compared to their hydrocortisone analogs. However, the transcriptional transactivation activity of these compounds were considerably higher than the corresponding hydrocortisone analogs. Among all the compounds evaluated, a quinoxaline thioether modification demonstrated the best overall in vitro separation.
(PMID: 22465636)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: ADME
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
1Efficacy activity commentEfficacy activity commentString
2Efficacy standard flagEfficacy standard flagInteger
3Efficacy qualifierEfficacy qualifierString
4Efficacy published valueEfficacy published valueFloat%
5Efficacy standard valueEfficacy standard valueFloat%

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