Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-stimulated IL-8 production at 1 uM relative to prednisolone - BioAssay Summary
The prednisolone C-21 heteroaryl thioethers have been synthesized and evaluated in cell based transrepression and transactivation assays. Most of the compounds demonstrated weak transactivational activity in both human and rat tyrosineaminotransferase functional assay while keeping potent anti-inflammatory activity. The benzimidazole thioether 7 exhibited comparable anti-inflammatory activity and improved safety profile compared to the classical oral steroid prednisolone. ..more
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 Tested Compounds
 Tested Compounds
All(26)
 
 
Unspecified(26)
 
 
 Tested Substances
 Tested Substances
All(26)
 
 
Unspecified(26)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 640509
Data Source: ChEMBL (797957)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-05-16

Data Table (Complete):           All
Target
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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
Tested Compounds:
Description:
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Title: Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).

Abstract: The prednisolone C-21 heteroaryl thioethers have been synthesized and evaluated in cell based transrepression and transactivation assays. Most of the compounds demonstrated weak transactivational activity in both human and rat tyrosineaminotransferase functional assay while keeping potent anti-inflammatory activity. The benzimidazole thioether 7 exhibited comparable anti-inflammatory activity and improved safety profile compared to the classical oral steroid prednisolone.
(PMID: 22197391)
Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 25

ChEMBL target type: Target is a single protein chain

Result Definitions
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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)
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Classification
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