Affinity DataKi: 0.400nM ΔG°: -53.6kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Affinity DataKi: 0.5nM ΔG°: -53.1kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Affinity DataKi: 0.800nM IC50: 4nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 1nM ΔG°: -51.4kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Affinity DataKi: 1.30nM IC50: 5nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 3nM IC50: 9nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataKi: 3.70nMAssay Description:Non-competitive inhibition of lysine methyltransferase G9a (unknown origin) using SAM as substrate by Michaelis-Menten kinetic assayMore data for this Ligand-Target Pair
Affinity DataKi: 4nM ΔG°: -47.9kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Affinity DataKi: 8nMAssay Description:Competitive inhibition of full length 6xHis-tagged SMYD2 (unknown origin) expressed in Escherichia coli using varying levels of Btn-Ahx-GSRAHSSHLKSKK...More data for this Ligand-Target Pair
Affinity DataKi: 11nM IC50: 30nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 16nMAssay Description:Inhibition of human PRMT6 pre-incubated for 1 to 30 mins using [3H]SAM as donor and [3H]methylated biotin-labeled peptide as substrate by scintillati...More data for this Ligand-Target Pair
Affinity DataKi: 17nM IC50: 42nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 23nM IC50: 83nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 28nMAssay Description:Uncompetitive inhibition of full length 6xHis-tagged SMYD2 (unknown origin) expressed in Escherichia coli using fixed levels of Btn-Ahx-GSRAHSSHLKSKK...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Entremed
Curated by ChEMBL
Entremed
Curated by ChEMBL
Affinity DataKi: 38nMAssay Description:Competitive inhibition of human recombinant DOT1L (1 to 420 amino acid residues) overexpressed in Escherichia coli BL21 (DE3) using [3H]-SAM as subst...More data for this Ligand-Target Pair
Affinity DataKi: 55nM IC50: 119nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
TargetSigma non-opioid intracellular receptor 1(Cavia porcellus (Guinea pig))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 64nMAssay Description:Displacement of [3H]pentazocine from guinea pig sigma1 receptorMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 87nMAssay Description:Displacement of [3H]alpha-methylhistamine from human histamine H3 receptor expressed HEK Flp-In cell membranesMore data for this Ligand-Target Pair
Affinity DataKi: 110nM IC50: 230nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 120nM IC50: 250nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 120nM IC50: 260nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Entremed
Curated by ChEMBL
Entremed
Curated by ChEMBL
Affinity DataKi: 300nMAssay Description:Competitive inhibition of human recombinant DOT1L (1 to 472 amino acid residues) expressed in Escherichia coli BL21 (DE3) using [3H]-SAM assessed as ...More data for this Ligand-Target Pair
Affinity DataKi: 550nM IC50: 1.10E+3nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 750nMAssay Description:Inhibition of recombinant full length human NNMT measured for 30 mins by SAHH-coupled fluorescence assayMore data for this Ligand-Target Pair
Affinity DataKi: 950nMAssay Description:Inhibition of DNMT1 (unknown origin) using [3H]-SAM assessed as inhibition of dsDNA methylation after 1 hr by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.15E+3nMAssay Description:Inhibition of PRMT5 (unknown origin) using [3H]SAM after 1 hr by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.15E+3nMAssay Description:Inhibition of PRMT3 (unknown origin) using [3H]SAM assessed as inhibition of biotinylated-H4 (1 to 24 amino acid residues) methylation after 1 hr by ...More data for this Ligand-Target Pair
Affinity DataKi: 1.20E+3nM ΔG°: -33.8kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Affinity DataKi: 1.50E+3nM IC50: 3.00E+3nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: 1.83E+3nM ΔG°: -32.7kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nM IC50: >2.00E+4nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: >3.75E+4nM IC50: >7.50E+4nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
Affinity DataKi: >5.00E+4nM IC50: >1.00E+5nMAssay Description:In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Entremed
Curated by ChEMBL
Entremed
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Competitive inhibition of human recombinant DOT1L (1 to 416 amino acid residues) using [3H]-SAM assessed as inhibition of nucleosome methylation incu...More data for this Ligand-Target Pair
TargetWD repeat-containing protein 5(Homo sapiens (Human))
Ontario Institute For Cancer Research
Curated by ChEMBL
Ontario Institute For Cancer Research
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of SUMO-His-tagged WDR5 (unknown origin) interaction with MLL1 assessed as displacement of fluorescence labelled Ac-ARA peptide substrate ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataIC50: 2nMAssay 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
Affinity DataIC50: 2nMAssay Description:Inhibition of human USP21 using ubiquitin rhodamine 110 110 as substrate preincubated for 15 to 20 mins followed by enzyme addition and measured afte...More data for this Ligand-Target Pair
Ligand Info
Affinity DataIC50: 2.80nMAssay Description:Inhibition of SMYD2 (unknown origin) using biotinylated GSRAHSSHLKSKKGQSTSRH as substrate assessed as incorporation of tritium labeled methyl group f...More data for this Ligand-Target Pair
TargetWD repeat-containing protein 5(Homo sapiens (Human))
Ontario Institute For Cancer Research
Curated by ChEMBL
Ontario Institute For Cancer Research
Curated by ChEMBL
Affinity DataIC50: 2.90nMAssay Description:Inhibition of N-terminal His-tagged WDR5 (24 to 334 residues) (unknown origin) interaction with MLL1 assessed as displacement of 5-Lys-FAM peptide su...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of G9a (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of lysine methyltransferase G9a (unknown origin) using [3H]-SAM as substrate after 0.25 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataIC50: 4nMAssay 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
Affinity DataIC50: 4nMAssay Description:Inhibition of PRMT8 (unknown origin) by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human PRMT1 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation prox...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human PRMT4 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation prox...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human PRMT3 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation prox...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataIC50: 4nMAssay 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
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina At Chapel Hill
Curated by ChEMBL
University Of North Carolina At Chapel Hill
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of lysine methyltransferase G9a (unknown origin) using [3H]-SAM as substrate after 0.25 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of human GLP catalytic domain (951 to 1235 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated H3 (1 to 25 residues) as ...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of human PRMT6 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation prox...More data for this Ligand-Target Pair