BindingDB PrimarySearch

Found 17 hits Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase EZH2' and Ligand = 'BDBM50017293'
Target/Host (Institution)	Ligand	Target/Host Links	Ligand Links	Trg + Lig Links	Ki nM	ΔG° kJ/mole	IC50 nM	Kd nM	EC50/IC50 nM	k_off s^-1	k_on M^-1s^-1	pH	Temp °C
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human wild-type EZH2 assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 A677G mutant assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 A677G mutant assessed as H3K27me1 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 Y641F mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 Y641H mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 Y641N mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 Y641S mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	0.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					Assay Description Inhibition of human EZH2 Y641C mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM				J Med Chem 58: 1596-629 (2015) Article DOI: 10.1021/jm501234a BindingDB Entry DOI: 10.7270/Q28K7BS2
Icahn School of Medicine at Mount Sinai Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	1	n/a	n/a	n/a	n/a	n/a	n/a
Constellation Pharmaceuticals, Inc. Curated by ChEMBL					Assay Description Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method				Bioorg Med Chem Lett 25: 3644-9 (2015) Article DOI: 10.1016/j.bmcl.2015.06.056 BindingDB Entry DOI: 10.7270/Q2Q24205
Constellation Pharmaceuticals, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	2	n/a	n/a	n/a	n/a	n/a	n/a
Constellation Pharmaceuticals, Inc. Curated by ChEMBL					Assay Description Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count ba...				Bioorg Med Chem Lett 25: 3644-9 (2015) Article DOI: 10.1016/j.bmcl.2015.06.056 BindingDB Entry DOI: 10.7270/Q2Q24205
Constellation Pharmaceuticals, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	2.70	n/a	n/a	n/a	n/a	n/a	n/a
TBA					Assay Description Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated fo...				Citation and Details Article DOI: 10.1021/acs.jmedchem.0c02234 BindingDB Entry DOI: 10.7270/Q22V2M02
TBA					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	5.5	n/a	n/a	n/a	n/a	n/a	n/a
TBA					Assay Description Inhibition of EZH2 Y641F mutant (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay				Citation and Details Article DOI: 10.1021/acs.jmedchem.1c01154 BindingDB Entry DOI: 10.7270/Q2D79G73
TBA					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	9.90	n/a	n/a	n/a	n/a	n/a	n/a
TBA									Citation and Details Article DOI: 10.1016/j.ejmech.2022.114419 BindingDB Entry DOI: 10.7270/Q2PR80Z0
TBA					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	9.90	n/a	n/a	n/a	n/a	n/a	n/a
TBA									Citation and Details Article DOI: 10.1021/acs.jmedchem.2c00047 BindingDB Entry DOI: 10.7270/Q27D3059
TBA					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	10	n/a	n/a	n/a	n/a	n/a	n/a
TBA									Citation and Details Article DOI: 10.1021/acs.jmedchem.1c01208 BindingDB Entry DOI: 10.7270/Q25X2DZR
TBA					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	13	n/a	n/a	n/a	n/a	n/a	n/a
TBA					Assay Description Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay				Citation and Details Article DOI: 10.1021/acs.jmedchem.1c01154 BindingDB Entry DOI: 10.7270/Q2D79G73
TBA					More data for this Ligand-Target Pair				3D Structure (crystal)
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human))	BDBM50017293 (CHEMBL3287735 \| US10647700, Compound GSK126) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid PDB UniChem Similars	PDB Article PubMed	n/a	n/a	280	n/a	n/a	n/a	n/a	n/a	n/a
Constellation Pharmaceuticals, Inc. Curated by ChEMBL					Assay Description Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method				Bioorg Med Chem Lett 25: 3644-9 (2015) Article DOI: 10.1016/j.bmcl.2015.06.056 BindingDB Entry DOI: 10.7270/Q2Q24205
Constellation Pharmaceuticals, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair				3D Structure (crystal)