ChEMBL ligand: CHEMBL3087498
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 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!
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!
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 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 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!

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	Inhibition of DNMT1 (unknown origin)	B	9.52	pIC50	0.3	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4518-4522 [PMID:27485386]
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 (radioactive enzyme assay)) EUB0000216b EZH2	B	4	pIC50	>100000	nM	IC50	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	Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysis	B	10.22	pKd	0.06	nM	Kd	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level	B	8.06	pIC50	8.8	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Affinity On-target Cellular interaction (Western Blot (reduction of H3K79 dimethylation in A431 cells by DOT1L)) EUB0000216b DOT1L	B	8.59	pIC50	2.6	nM	IC50	Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb	-	-	9.52	pIC50	0.3	nM	IC50	Nat Commun (2012) 3: 1288 [PMID:23250418]
ChEMBL	Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (2013) 56: 8972-8983 [PMID:23879463]
ChEMBL	Affinity Biochemical interaction (Radioactive enzyme assay) EUB0000216b DOT1L	B	9.52	pIC50	0.3	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assay	B	8.05	pEC50	9	nM	EC50	J Med Chem (2013) 56: 8972-8983 [PMID:23879463]
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	Selectivity interaction (Methyltransferase panel (radioactive enzyme assay)) EUB0000216b EHMT2	B	4	pIC50	>100000	nM	IC50	Selectivity 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	Selectivity interaction (Methyltransferase panel (radioactive enzyme assay)) EUB0000216b EHMT1	B	4	pIC50	>100000	nM	IC50	Selectivity 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 (radioactive enzyme assay)) EUB0000216b MLL	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b SETD7	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b SETDB1	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b SUV39H2	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b SUV420H2	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b SETD8	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b PRMT3	B	4	pIC50	>100000	nM	IC50	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 (radioactive enzyme assay)) EUB0000216b PRMT5	B	4	pIC50	>100000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3

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]