Inhibition of human JMJD2A by FDH coupled assay - BioAssay Summary
The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling. ..more
 _
   
 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 344925
Data Source: ChEMBL (492954)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-05-11

Data Table (Complete):           Active    All
Target
Helptop of page
Sequence: RecName: Full=Lysine-specific demethylase 4A; AltName: Full=JmjC domain-containing histone demethylation protein 3A; AltName: Full=Jumonji domain-containing protein 2A
Description ..   
Protein Family: PHD-zinc-finger like domain
Comment ..   

Gene:KDM4A     Related Protein 3D Structures
BioActive Compound: 1
Description:
Helptop of page
Title: Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

Abstract: The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.
(PMID: 18942826)
Comment
Helptop of page
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Helptop of page
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 101373

ChEMBL target type: Target is a single protein chain

Result Definitions
Helptop of page
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4IC50 activity commentIC50 activity commentString
5IC50 standard flagIC50 standard flagInteger
6IC50 qualifierIC50 qualifierString
7IC50 published valueIC50 published valueFloatnM
8IC50 standard valueIC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
Helptop of page
Classification
PageFrom: