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BioAssay: AID 426823

Transcriptional activation of HSF1 in heat shock stress-induced human HeLa cells assessed as granule formation treated 1 hr before heat shock challenge measured after 2 hrs by immunocytochemical staining

Chloro-oxime derivatives were investigated as novel small molecule chaperone amplifiers. Lead optimization led to the discovery of compounds that displayed potent HSF1 activation activity, significant cytoprotection in MG-132 stress, ER stress and PolyQ stress cell models (EC(50)<10 microM). ..more
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 Tested Compounds
 Tested Compounds
All(44)
 
 
Active(25)
 
 
Inactive(15)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(44)
 
 
Active(25)
 
 
Inactive(15)
 
 
Unspecified(4)
 
 
AID: 426823
Data Source: ChEMBL (578167)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Heat shock factor protein 1; Short=HSF 1; AltName: Full=Heat shock transcription factor 1; Short=HSTF 1
Description ..   
Protein Family: Vertebrate heat shock transcription factor
Comment ..   

Gene:HSF1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 25
Description:
Title: Chloro-oxime derivatives as novel small molecule chaperone amplifiers.

Abstract: Chloro-oxime derivatives were investigated as novel small molecule chaperone amplifiers. Lead optimization led to the discovery of compounds that displayed potent HSF1 activation activity, significant cytoprotection in MG-132 stress, ER stress and PolyQ stress cell models (EC(50)<10 microM).
(PMID: 19398333)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

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
Assay Cell Type: HeLa
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Activity activity commentActivity activity commentString
7Activity standard flagActivity standard flagInteger
8Activity qualifierActivity qualifierString
9Activity published valueActivity published valueFloat%
10Activity standard valueActivity standard valueFloat%
11EC50 activity commentEC50 activity commentString
12EC50 standard flagEC50 standard flagInteger
13EC50 qualifierEC50 qualifierString
14EC50 published valueEC50 published valueFloatμM
15EC50 standard valueEC50 standard valueFloatnM

* Activity Concentration.

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