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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]