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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on the storage and integration of epigenetic drug datasets that were obtained from laboratory experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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CPI360

Category:HMTi
Cas Number:N.A.
Molecular Formula:C25H31N3O4
Molecular Weight:437.53134 g/mol
Smiles:CC1=CC(=C(C(=O)N1)CNC(=O)C2=C(N(C3=CC=CC=C32)C(C)C4CCOCC4)C)OC
Description:Determination of the CPI-360 potency employing a biochemical assay with reconstituted PRC2 harboring WT EZH2 or Y641N-mutated EZH2 as the catalytic component and histone H3 peptides comprising residues 17–38 with either a monomethyl (WT) or dimethyl (Y641N) group on residue K27. Indicated half-maximal inhibitory concentration (IC50) values were calculated from the mean of three experiments ±SD. CPI-360 was found to be about 5-fold more potent on WT compared to the Y641N mutant EZH2.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (10.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex

Disease list

ConditionsDrug NameStatusNct NumberPhases
lymphomaCPI360
EPZ-6438
GSK126
Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
EZH2 inhibitor efficacy in non-Hodgkin lymphoma does not require suppression of H3K27 mono-methylation CPI360
EPZ-6438
GSK126
HMTihuman lymphoma cell line(Karpas422)25457180

Complex list

PDBIdDrug NameTargetmethodPubmedId

About

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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on integrating epigenetic drug studies based Omics data from high through experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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©2016 Group of Computational Epigenomics and Bioinformatics, College of Life Science, Jilin Normal University, China

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