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BioAssay: AID 408887

Selectivity for HDAC10 over HDAC1

The discovery of the rules governing the inhibition of the various HDAC isoforms is likely to be key to identifying improved therapeutics that act as epigenetic modulators of gene transcription. Herein we present results on the modification of the CAP region of a set of triazolylphenyl-based HDACIs, and show that the nature of substitution on the phenyl ring plays a role in their selectivity for more ..
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 Tested Compounds
 Tested Compounds
All(17)
 
 
Unspecified(17)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Unspecified(17)
 
 
 Related BioAssays
 Related BioAssays
AID: 408887
Data Source: ChEMBL (556916)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-05-07

Data Table ( Complete ):           All
Tested Compounds:
Description:
Title: A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.

Abstract: The discovery of the rules governing the inhibition of the various HDAC isoforms is likely to be key to identifying improved therapeutics that act as epigenetic modulators of gene transcription. Herein we present results on the modification of the CAP region of a set of triazolylphenyl-based HDACIs, and show that the nature of substitution on the phenyl ring plays a role in their selectivity for HDAC1 versus HDAC6, with low to moderate selectivity (2-51-fold) being achieved. In light of the valuable selectivity and potency that were identified for the triazolylphenyl ligand 6b in the inhibition of HDAC6 (IC50 = 1.9 nM), this compound represents a valuable research tool and a candidate for further chemical modifications. Lastly, these new HDACIs were studied for both their anticancer and antimalarial activity, which serve to validate the superior activity of the HDACI 10c.
(PMID: 18494463)
Comment
Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ratio IC50 activity commentRatio IC50 activity commentString
2Ratio IC50 standard flagRatio IC50 standard flagInteger
3Ratio IC50 qualifierRatio IC50 qualifierString
4Ratio IC50 published valueRatio IC50 published valueFloat
5Ratio IC50 standard valueRatio IC50 standard valueFloat

Data Table (Concise)
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