bromo-deaza-SAH [Ligand Id: 7018] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2349526
  • DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358]
1 CHEMBL2349526_lig_chart_1 DNA (cytosine-5)-methyltransferase 1 Human
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  • DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3]
2 CHEMBL2349526_lig_chart_2 Histone-lysine N-methyltransferase, H3 lysine-79 specific Human
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  • Nicotinamide N-methyltransferase in Human [ChEMBL: CHEMBL2346486] [UniProtKB: P40261]
  • This target only has 1 pki data point
3 CHEMBL2349526_lig_chart_3 Nicotinamide N-methyltransferase Human
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  • protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
  • This target only has 1 pki data point
4 CHEMBL2349526_lig_chart_4 Protein arginine N-methyltransferase 3 Human
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  • protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
  • This target only has 1 pki data point
5 CHEMBL2349526_lig_chart_5 Protein arginine N-methyltransferase 5 Human
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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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2346486] [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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]