BindingDB PrimarySearch

Found 29 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase EHMT2' and Ligand = 'BDBM50353128'

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

Ki: 3.70nMAssay Description:Competitive inhibition of G9a (unknown origin) by Morrison plot analysis in presence of histone H3 (1 to 25 residues)More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

Ki: 3.70nMAssay Description:Competitive inhibition of G9a by fluorescence polarization assay in presence of fluorescein-labeled H3 peptideMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

Ki: 18nMAssay Description:Inhibition of G9a (unknown origin) assessed as reduction in substrate methylation using histone H3 and SAM as substrate measured after 15 to 60 mins ...More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 2.5nMAssay Description:Inhibition of G9a (unknown origin) using [histone H3 1 to 25 residues] and SAM substrate by scintillation proximity assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 12nMAssay Description:Inhibition of G9a assessed as hydrolysis of S-adenosyl-L-homocysteine after 2 mins by SAHH-coupled fluorescence assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: <15nMAssay Description:Inhibition of G9a (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: <15nMAssay Description:Inhibition of G9a (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: <15nMAssay Description:Inhibition of EHMT2 (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: <15nMAssay Description:Inhibition of G9a (unknown origin) using histone H3 (1 to 25 residues) as substrate preincubated for 2 mins followed by substrate addition measured f...More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 15nMAssay Description:Inhibition G9a (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 15nMAssay Description:Inhibition G9a (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 25nMAssay Description:Inhibition of recombinant human G9a using biotinylated-Histone H3 peptide (1 to 21 residues) after 30 mins in presence of SAM by AlphaLISA assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 26nMAssay Description:Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as red...More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 30nMAssay Description:Inhibition of human G9a using core histone H3 as substrate incubated for 1 hr in presence of [3H]-SAM by filter binding methodMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 35nMAssay Description:Inhibition of N-terminal GST-tagged human recombinant G9a (785 to 1210 residues) expressed in baculovirus infected Sf9 cells incubated for 1 hr by Al...More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 48nMAssay Description:Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 55nMAssay Description:Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 55nMAssay Description:Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 59nMAssay Description:Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 70nMAssay Description:Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 81nMAssay Description:Inhibition of G9a in human MCF7 cells after 48 hrs by clonogenic assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 81nMAssay Description:Inhibition of G9a in human MDA-MB-231 cells after 48 hrs by clonogenic assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 81nMAssay Description:Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 81nMAssay Description:Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 81nMAssay Description:Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell We...More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 120nMAssay Description:Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 210nMAssay Description:Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

IC50: 610nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3 (1 to 21 residues)/S-adenosyl-methionine as substrate/methyl donor after 3 hrs by Al...More data for this Ligand-Target Pair

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3D Structure (crystal)

Histone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL

BDBM50353128(CHEMBL1231795)

Kd: 1.42E+3nMAssay Description:Binding affinity to human His-tagged G9a expressed in Escherichia coli Rosetta (DE3) after 30 mins by MST binding assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Filter my 29 hits

Targets 1▿
- Histone-lysine N-methyltransferase EHMT2 29
Publications 13▿
- J Med Chem 54: 6139-50 (2011) 8
- Bioorg Med Chem 24: 6102-6108 (2016) 3
- J Med Chem 62: 2666-2689 (2019) 3
- Eur J Med Chem 56: 179-194 (2012) 3
- J Med Chem 61: 6546-6573 (2018) 2
- Eur J Med Chem 184: (2019) 2
- Eur J Med Chem 237: (2022) 1
- Bioorg Med Chem Lett 29: 2516-2524 (2019) 1
- J Med Chem 56: 8931-42 (2013) 1
- J Med Chem 61: 6518-6545 (2018) 1
- Eur J Med Chem 179: 537-546 (2019) 1
- Bioorg Med Chem 25: 4579-4594 (2017) 1
- Medchemcomm 5: 1821-1828 (2014) 1
Institutions 12▿
- University Of North Carolina At Chapel Hill 9
- TBA 3
- The University Of Texas M.D. Anderson Cancer Center 3
- China Pharmaceutical University 3
- National University Of Singapore 2
- Wuxi Apptec (Tianjin) Co. 2
- Mercachem 1
- Fudan University 1
- Sapienza University Of Rome 1
- Universidad De Oviedo-Principado De Asturias 1
- Imperial College London 1
- Southern Medical University 1
Affinity: 2.5 to 1.4E+3 nM▿
- Ki 3
- IC50 25
- Kd 1
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1