Transactivation activity at glucocorticoid receptor in human HepG2 cells expressing luciferase-taggged GRE gene at 1 uM by luciferase reporter gene assay relative to control - BioAssay Summary
A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function. ..more
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 Tested Compounds
 Tested Compounds
All(10)
 
 
Unspecified(10)
 
 
 Tested Substances
 Tested Substances
All(10)
 
 
Unspecified(10)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 630007
Data Source: ChEMBL (787455)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-05-15

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 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.

Abstract: A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function.
(PMID: 21944381)
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
1Emax activity commentEmax activity commentString
2Emax standard flagEmax standard flagInteger
3Emax qualifierEmax qualifierString
4Emax published valueEmax published valueFloat%
5Emax standard valueEmax standard valueFloat%

Data Table (Concise)
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Classification
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