ChEMBL ligand: CHEMBL2349526
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!
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!
nicotinamide N-methyltransferase/Nicotinamide N-methyltransferase in Human [ChEMBL: CHEMBL2346486] [GtoPdb: 3205] [UniProtKB: P40261] 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]
GtoPdb	-	-	6.02	pKi	950	nM	Ki	Bioorg Med Chem (2013) 21: 1787-94 [PMID:23433670]
ChEMBL	Inhibition of DNMT1 (unknown origin) using [3H]-SAM assessed as inhibition of dsDNA methylation after 1 hr by scintillation proximity assay	B	6.02	pKi	950	nM	Ki	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
ChEMBL	Inhibition of DNMT1 (unknown origin) using [3H]-SAM assessed as inhibition of dsDNA methylation after 1 hr by scintillation proximity assay	B	5.72	pIC50	1900	nM	IC50	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
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]
GtoPdb	-	-	7.42	pKi	38	nM	Ki	Bioorg Med Chem (2013) 21: 1787-94 [PMID:23433670]
ChEMBL	Competitive inhibition of human recombinant DOT1L (1 to 420 amino acid residues) overexpressed in Escherichia coli BL21 (DE3) using [3H]-SAM as substrate assessed as inhibition of nucleosome methylation incubated for 30 mins prior to substrate addition measured after 1 hr by scintillation counting analysis	B	7.42	pKi	38	nM	Ki	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
GtoPdb	-	-	7.11	pIC50	77	nM	IC50	Bioorg Med Chem (2013) 21: 1787-94 [PMID:23433670]
ChEMBL	Competitive inhibition of human recombinant DOT1L (1 to 420 amino acid residues) overexpressed in Escherichia coli BL21 (DE3) using [3H]-SAM as substrate assessed as inhibition of nucleosome methylation incubated for 30 mins prior to substrate addition measured after 1 hr by scintillation counting analysis	B	7.11	pIC50	77	nM	IC50	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
ChEMBL	Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor	B	7.11	pIC50	77	nM	IC50	J Med Chem (2013) 56: 8972-8983 [PMID:23879463]
nicotinamide N-methyltransferase/Nicotinamide N-methyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2346486] [GtoPdb: 3205] [UniProtKB: P40261]
ChEMBL	Inhibition of recombinant full length human NNMT measured for 30 mins by SAHH-coupled fluorescence assay	B	6.12	pKi	750	nM	Ki	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
ChEMBL	Inhibition of recombinant full length human NNMT measured for 30 mins by SAHH-coupled fluorescence assay	B	5.82	pIC50	1500	nM	IC50	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
ChEMBL	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 scintillation proximity assay	B	5.94	pKi	1150	nM	Ki	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
ChEMBL	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 scintillation proximity assay	B	5.64	pIC50	2300	nM	IC50	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
ChEMBL	Inhibition of PRMT5 (unknown origin) using [3H]SAM after 1 hr by scintillation proximity assay	B	5.94	pKi	1150	nM	Ki	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
ChEMBL	Inhibition of PRMT5 (unknown origin) using [3H]SAM after 1 hr by scintillation proximity assay	B	5.64	pIC50	2300	nM	IC50	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]

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]