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Found 757 with Last Name = 'schapira' and Initial = 'm'
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataKi:  0.300nMAssay Description:Inhibition of human recombinant DOT1L (1 to 416 residues) using chicken erythrocyte oligonucleosomes as substrate and [3H]-SAM incubated for 120 mins...More data for this Ligand-Target Pair
TargetProtein arginine N-methyltransferase 6(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
TargetProtein arginine N-methyltransferase 8(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 6(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178102(N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-py...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 8(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178102(N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-py...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50431676(CHEMBL2349526)
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
TargetProtein arginine N-methyltransferase 3 [N508S](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(Cavia porcellus (Guinea pig))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50194756(CHEMBL3961701)
Affinity DataKi:  64nMAssay Description:Displacement of [3H]pentazocine from guinea pig sigma1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50194756(CHEMBL3961701)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 6(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178101(N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178102(N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-py...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178102(N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-py...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50396981(CHEMBL2171174)
Affinity DataKi:  290nMAssay Description:Inhibition of recombinant human DOT1L (1 to 472 residues) preincubated for 10 mins prior addition of [3H]SAM measured after 30 mins by Beckman LS-650...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50396981(CHEMBL2171174)
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
TargetProtein arginine N-methyltransferase 3 [N508S](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178102(N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-py...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNicotinamide N-methyltransferase(Homo sapiens (Human))
Entremed

Curated by ChEMBL
LigandPNGBDBM50431676(CHEMBL2349526)
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
In DepthDetails ArticlePubMed
TargetDNA (cytosine-5)-methyltransferase 1(Homo sapiens (Human))
Entremed

Curated by ChEMBL
LigandPNGBDBM50431676(CHEMBL2349526)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 3 [N508S](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM50431676(CHEMBL2349526)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Entremed

Curated by ChEMBL
LigandPNGBDBM50431676(CHEMBL2349526)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 8(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178101(N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178101(N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178101(N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 3 [N508S](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178101(N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDNA (cytosine-5)-methyltransferase 1(Homo sapiens (Human))
Entremed

Curated by ChEMBL
LigandPNGBDBM50443016(CHEMBL3087498)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of DNMT1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
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
LigandPNGBDBM50164787(CHEMBL3798088)
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
In DepthDetails ArticlePubMed
TargetWD repeat-containing protein 5(Homo sapiens (Human))
Ontario Institute For Cancer Research

Curated by ChEMBL
LigandPNGBDBM200712(US9233086, 10A)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDNA (cytosine-5)-methyltransferase 1(Homo sapiens (Human))
Entremed

Curated by ChEMBL
LigandPNGBDBM50396980(CHEMBL2171169)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of DNMT1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 6(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PRMT6 (unknown origin) by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PRMT4 (unknown origin) by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 3(Homo sapiens)
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PRMT3 (unknown origin) by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 1(Homo sapiens)
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PRMT1 (unknown origin) by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 6(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
TargetProtein arginine N-methyltransferase 3 [N508S](Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 8(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of PRMT8 (unknown origin) by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 8(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM178103(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human PRMT8 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
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50519299(CHEMBL4536230)
Affinity DataIC50:  6nMAssay Description:Inhibition of recombinant human SMYD2 (1 to 433 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-p53 peptide (361 to 3...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50519300(CHEMBL4520134)
Affinity DataIC50:  8nMAssay Description:Inhibition of recombinant human SMYD2 (1 to 433 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-p53 peptide (361 to 3...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetProtein arginine N-methyltransferase 3(Homo sapiens)
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50247381(CHEMBL4079503)
Affinity DataIC50:  10nMAssay Description:Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50536666(CHEMBL4588797)
Affinity DataIC50:  13nMAssay Description:Inhibition of human recombinant DOT1L (1 to 420 amino acids) expressed in Escherichia coliMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM50194730(CHEMBL3906680)
Affinity DataIC50:  14nMAssay Description:Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with pr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM50194766(CHEMBL3938938)
Affinity DataIC50:  15nMAssay Description:Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with pr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM50194785(CHEMBL3956007)
Affinity DataIC50:  15nMAssay Description:Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with pr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50519300(CHEMBL4520134)
Affinity DataIC50:  16nMAssay Description:Inhibition of recombinant human SMYD2 (1 to 433 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-p53 peptide (361 to 3...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetHistone-arginine methyltransferase CARM1(Homo sapiens (Human))
University of Toronto

LigandPNGBDBM50194780(CHEMBL3911620)
Affinity DataIC50:  16nMAssay Description:Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with pr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 3(Homo sapiens)
Icahn School Of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50247397(CHEMBL4076640)
Affinity DataIC50:  17nMAssay Description:Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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