Transactivation of glucocorticoid receptor in rat H42E cells assessed as induction of TAT measuring degradation of tyrosine to p-hydroxy phenyl pyruvate - 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(10)
 
 
Active(9)
 
 
Inconclusive(1)
 
 
 Tested Substances
 Tested Substances
All(10)
 
 
Active(9)
 
 
Inconclusive(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 640510
Data Source: ChEMBL (797958)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-05-16

Data Table (Complete):           Active    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
BioActive Compounds: 9
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)
Comment
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Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
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ChEMBL Assay Type: ADMET

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 12104

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatnM
6IC50 standard valueIC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
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Classification
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