ChEMBL ligand: CHEMBL3109630
DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358] There should be some charts here, you may need to enable JavaScript!
enhancer of zeste 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800] There should be some charts here, you may need to enable JavaScript!
enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910] There should be some charts here, you may need to enable JavaScript!
DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3] There should be some charts here, you may need to enable JavaScript!
euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7] There should be some charts here, you may need to enable JavaScript!
euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1] There should be some charts here, you may need to enable JavaScript!
lysine methyltransferase 2A/Histone-lysine N-methyltransferase MLL in Human [ChEMBL: CHEMBL1293299] [GtoPdb: 2688] [UniProtKB: Q03164] There should be some charts here, you may need to enable JavaScript!
nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028] There should be some charts here, you may need to enable JavaScript!
Histone-lysine N-methyltransferase NSD3 in Human [ChEMBL: CHEMBL3108646] [UniProtKB: Q9BZ95] There should be some charts here, you may need to enable JavaScript!
SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6] There should be some charts here, you may need to enable JavaScript!
SET domain bifurcated histone lysine methyltransferase 1/Histone-lysine N-methyltransferase SETDB1 in Human [ChEMBL: CHEMBL2321646] [GtoPdb: 2705] [UniProtKB: Q15047] There should be some charts here, you may need to enable JavaScript!
Histone-lysine N-methyltransferase SMYD3 in Human [ChEMBL: CHEMBL2321643] [UniProtKB: Q9H7B4] There should be some charts here, you may need to enable JavaScript!
SUV39H2 histone lysine methyltransferase/Histone-lysine N-methyltransferase SUV39H2 in Human [ChEMBL: CHEMBL1795177] [GtoPdb: 2716] [UniProtKB: Q9H5I1] There should be some charts here, you may need to enable JavaScript!
lysine methyltransferase 5B/Histone-lysine N-methyltransferase SUV420H1 in Human [ChEMBL: CHEMBL2321645] [GtoPdb: 2717] [UniProtKB: Q4FZB7] There should be some charts here, you may need to enable JavaScript!
lysine methyltransferase 5C/Histone-lysine N-methyltransferase SUV420H2 in Human [ChEMBL: CHEMBL2321644] [GtoPdb: 2718] [UniProtKB: Q86Y97] There should be some charts here, you may need to enable JavaScript!
lysine methyltransferase 5A/N-lysine methyltransferase SETD8 in Human [ChEMBL: CHEMBL1795176] [GtoPdb: 2704] [UniProtKB: Q9NQR1] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 6/Protein arginine N-methyltransferase 6 in Human [ChEMBL: CHEMBL1275221] [GtoPdb: 1257] [UniProtKB: Q96LA8] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 8/Protein arginine N-methyltransferase 8 in Human [ChEMBL: CHEMBL3108648] [GtoPdb: 1259] [UniProtKB: Q9NR22] There should be some charts here, you may need to enable JavaScript!
spindlin 1/Spindlin-1 in Human [ChEMBL: CHEMBL4523509] [GtoPdb: 3274] [UniProtKB: Q9Y657] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b DNMT1	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
enhancer of zeste 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b EZH1	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b EZH2	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b DOT1L	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
ChEMBL	Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay	B	7.89	pIC50	13	nM	IC50	Bioorg Med Chem Lett (2019) 29: 2516-2524 [PMID:31350126]
ChEMBL	Inhibition of G9a (unknown origin) assessed as effect on H3K9 methylation by cell based assay	B	8.24	pIC50	5.8	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128858-128858 [PMID:35718104]
GtoPdb	-	-	8.48	pIC50	3.3	nM	IC50	A-366: a chemical Probe for G9a/GLP.. thesgc.org; ACS Med Chem Lett (2014) 5: 205-9 [PMID:24900801]
ChEMBL	Inhibition of G9a (unknown origin)	B	8.48	pIC50	3.3	nM	IC50	J Med Chem (2023) 66: 4059-4085 [PMID:36882960]
ChEMBL	Inhibition of G9a (unknown origin)	B	8.48	pIC50	3.3	nM	IC50	J Med Chem (2015) 58: 2569-2583 [PMID:25406944]
ChEMBL	Inhibition of G9a (unknown origin)	B	8.48	pIC50	3.3	nM	IC50	Bioorg Med Chem (2016) 24: 6102-6108 [PMID:27720557]
ChEMBL	Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assay	B	8.48	pIC50	3.3	nM	IC50	ACS Med Chem Lett (2014) 5: 205-209 [PMID:24900801]
ChEMBL	Inhibition of G9a (unknown origin)	B	8.52	pIC50	3	nM	IC50	J Med Chem (2019) 62: 8996-9007 [PMID:31260300]
ChEMBL	Inhibition of G9a (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assay	B	8.52	pIC50	3	nM	IC50	ACS Med Chem Lett (2014) 5: 205-209 [PMID:24900801]
ChEMBL	Affinity Biochemical interaction (Scintillation proximity assay (SPA)) EUB0000212b EHMT2/G9a	B	8.52	pIC50	3	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of G9a (unknown origin)	B	8.55	pIC50	2.8	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128858-128858 [PMID:35718104]
ChEMBL	Affinity Phenotypic Cellular interaction (In-Cell Western assay (H3K9Me2 antibody immunofluorescence in PC3 cells)) EUB0000212b EHMT2/G9a	B	5.52	pEC50	<3000	nM	EC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1]
ChEMBL	Inhibition of GLP (unknown origin)	B	6.93	pIC50	118.1	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128858-128858 [PMID:35718104]
ChEMBL	Inhibition of GLP (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assay	B	7.42	pIC50	38	nM	IC50	ACS Med Chem Lett (2014) 5: 205-209 [PMID:24900801]
ChEMBL	Affinity Biochemical interaction (Scintillation proximity assay (SPA)) EUB0000212b EHMT1/GLP	B	7.42	pIC50	38	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of GLP (unknown origin)	B	7.42	pIC50	38	nM	IC50	J Med Chem (2023) 66: 4059-4085 [PMID:36882960]
ChEMBL	Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay	B	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2019) 29: 2516-2524 [PMID:31350126]
GtoPdb	-	-	8.52	pIC50	38	nM	IC50	A-366: a chemical Probe for G9a/GLP.. thesgc.org; ACS Med Chem Lett (2014) 5: 205-9 [PMID:24900801]
ChEMBL	Affinity Phenotypic Cellular interaction (In-Cell Western assay (H3K9Me2 antibody immunofluorescence in PC3 cells)) EUB0000212b EHMT1/GLP	B	5.52	pEC50	<3000	nM	EC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
lysine methyltransferase 2A/Histone-lysine N-methyltransferase MLL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293299] [GtoPdb: 2688] [UniProtKB: Q03164]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b MLL	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b NSD2	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
Histone-lysine N-methyltransferase NSD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108646] [UniProtKB: Q9BZ95]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b NSD3	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SETD7	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
SET domain bifurcated histone lysine methyltransferase 1/Histone-lysine N-methyltransferase SETDB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321646] [GtoPdb: 2705] [UniProtKB: Q15047]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SETDB1	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
Histone-lysine N-methyltransferase SMYD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321643] [UniProtKB: Q9H7B4]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SMYD3	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
SUV39H2 histone lysine methyltransferase/Histone-lysine N-methyltransferase SUV39H2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795177] [GtoPdb: 2716] [UniProtKB: Q9H5I1]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SUV39H2	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
lysine methyltransferase 5B/Histone-lysine N-methyltransferase SUV420H1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321645] [GtoPdb: 2717] [UniProtKB: Q4FZB7]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SUV420H1	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
lysine methyltransferase 5C/Histone-lysine N-methyltransferase SUV420H2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321644] [GtoPdb: 2718] [UniProtKB: Q86Y97]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SUV420H2	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
lysine methyltransferase 5A/N-lysine methyltransferase SETD8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795176] [GtoPdb: 2704] [UniProtKB: Q9NQR1]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b SETD8	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b PRMT1	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b PRMT3	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b PRMT5	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
protein arginine methyltransferase 6/Protein arginine N-methyltransferase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1275221] [GtoPdb: 1257] [UniProtKB: Q96LA8]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b PRMT6	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
protein arginine methyltransferase 8/Protein arginine N-methyltransferase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108648] [GtoPdb: 1259] [UniProtKB: Q9NR22]
ChEMBL	Selectivity interaction (Methyltransferase panel (Scintillation proximity assay (SPA))) EUB0000212b PRMT8	B	4.3	pEC50	>50000	nM	EC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
spindlin 1/Spindlin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523509] [GtoPdb: 3274] [UniProtKB: Q9Y657]
ChEMBL	Binding affinity to recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry	B	6.41	pKd	393	nM	Kd	J Med Chem (2019) 62: 9008-9025 [PMID:31550156]
ChEMBL	Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry	B	6.74	pKd	180	nM	Kd	J Med Chem (2019) 62: 9008-9025 [PMID:31550156]
ChEMBL	Inhibition of H3(1-12)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by FTSA assay	B	6.96	pKd	110	nM	Kd	J Med Chem (2019) 62: 8996-9007 [PMID:31260300]
ChEMBL	Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen method	B	5.82	pIC50	1500	nM	IC50	J Med Chem (2019) 62: 9008-9025 [PMID:31550156]
ChEMBL	Inhibition of FL-H3K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 30 mins by fluorescence polarization displacement assay	B	6.68	pIC50	207	nM	IC50	J Med Chem (2019) 62: 8996-9007 [PMID:31260300]
ChEMBL	Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by AlphaLISA assay	B	6.73	pIC50	186	nM	IC50	J Med Chem (2019) 62: 9008-9025 [PMID:31550156]
ChEMBL	Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assay	B	7.14	pIC50	72	nM	IC50	J Med Chem (2019) 62: 8996-9007 [PMID:31260300]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]