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BioAssay: AID 771528

Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay relative to dexamethasone

A series of heterocyclic glucocorticoid receptor (GR) modulators with 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core are described. Structure-activity relationships suggest a combination of H-bond acceptor and a 4-fluorophenyl moiety as being important structural components contributing to the glucocorticoid receptor binding and functional activity for this series of GR modulators. ..more
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 Tested Compounds
 Tested Compounds
All(15)
 
 
Unspecified(15)
 
 
 Tested Substances
 Tested Substances
All(15)
 
 
Unspecified(15)
 
 
 Related BioAssays
 Related BioAssays
AID: 771528
Data Source: ChEMBL (983186)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-24

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: Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.

Abstract: A series of heterocyclic glucocorticoid receptor (GR) modulators with 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core are described. Structure-activity relationships suggest a combination of H-bond acceptor and a 4-fluorophenyl moiety as being important structural components contributing to the glucocorticoid receptor binding and functional activity for this series of GR modulators.
(PMID: 24011644)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
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
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