Inhibition of GCN5 in human U937 cells at 50 uM - BioAssay Summary
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 331954
Data Source: ChEMBL (479980)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-05-07

Data Table (Complete):           All
Target
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Sequence: RecName: Full=Histone acetyltransferase KAT2A; AltName: Full=General control of amino acid synthesis protein 5-like 2; AltName: Full=Histone acetyltransferase GCN5; Short=HsGCN5; AltName: Full=Lysine acetyltransferase 2A; AltName: Full=STAF97
Description ..   
Protein Family: PCAF (P300/CBP-associated factor) N-terminal domain
Comment ..   

Gene:KAT2A     Related Protein 3D Structures
Tested Compound:
Description:
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Title: Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.

Abstract: Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs.
(PMID: 18434144)
Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 100876

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

Data Table (Concise)
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