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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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UNC0224

Category:HMTi
Cas Number:1197196-48-7
Molecular Formula:C26H43N7O2
Molecular Weight:485.66532 g/mol
Smiles:CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C)OC)OCCCN(C)C
Description:UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in the G9a Thioglo assay.IC50 value: 15 nM [1]Target: G9aUNC0224 (Compound 8) also potently inhibited GLP with an IC50 of 20 nM and 58 nM in the Thioglo assay and and AlphaScreen, respectively. 8 was more than 1000-fold selective for G9a over SET7/9 (a H3K4 HMT) and SET8/PreSET7 (a H4K20 HMT) in Thioglo-based biochemical assays
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (9.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
1445 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)
1446 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)20614940
1447 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)19891491
1448 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)19891491
1449 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)20614940
1450 UNC0224Histone-lysine N-methyltransferase SETD7 (Homo sapiens)20614940
1451 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)21316248
1452 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)21780790
1453 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)21780790
1454 UNC0224N-lysine methyltransferase SETD8 (Homo sapiens)20614940
1455 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)20614940
1456 UNC0224Protein arginine methyltransferase 3 (PRMT3) (Homo sapiens (Human))20614940
1457 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)20614940
1458 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)20614940
1459 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)19891491
1460 UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)19891491

Disease list

ConditionsDrug NameStatusNct NumberPhases

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID

Complex list

PDBIdDrug NameTargetmethodPubmedId
3K5K UNC0224Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)X-RAY DIFFRACTION19891491

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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