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 - BioAssay Summary
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)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 426823
Data Source: ChEMBL (578167)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-05-11

Data Table (Complete):           Active    All
Target
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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
BioActive Compounds: 25
Description:
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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
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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: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 101592

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4Activity activity commentActivity activity commentString
5Activity standard flagActivity standard flagInteger
6Activity qualifierActivity qualifierString
7Activity published valueActivity published valueFloat%
8Activity standard valueActivity standard valueFloat%
9EC50 activity commentEC50 activity commentString
10EC50 standard flagEC50 standard flagInteger
11EC50 qualifierEC50 qualifierString
12EC50 published valueEC50 published valueFloatnM
13EC50 standard valueEC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
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Classification
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