EPZ004777 [Ligand Id: 7377] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2169919
  • DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3]
1 CHEMBL2169919_lig_chart_1 Histone-lysine N-methyltransferase, H3 lysine-79 specific Human
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  • protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744Q9BQA1]
  • This target only has 0 pki data point
2 CHEMBL2169919_lig_chart_2 PRMT5/MEP50 complex Human
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  • protein arginine methyltransferase 7 /Protein arginine N-methyltransferase 7 in Human [ChEMBL: CHEMBL3562175] [GtoPdb: 1258] [UniProtKB: Q9NVM4]
  • This target only has 0 pki data point
3 CHEMBL2169919_lig_chart_3 Protein arginine N-methyltransferase 7 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 9.6 pKd 0.25 nM Kd J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human recombinant DOT1L using [3H]-SAM as substrate after 30 mins B 6.52 pKi 300 nM Ki Eur. J. Med. Chem. (2012) 56: 179-194 [PMID:22975593]
ChEMBL Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2013) 56: 8972-8983 [PMID:23879463]
ChEMBL Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containing B 9.52 pKi 0.3 nM Ki MedChemComm (2013) 4: 822-826 [PMID:23795283]
ChEMBL Inhibition of human DOT1L using oligo-nucleosome/[3H]-SAM as substrate preincubated for 30 mins followed by substrate addition measured after 120 mins by Morrison plot analysis B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Binding affinity to human DOT1L after 120 mins B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of DOT1L in human MOLM13 cells assessed as downregulation of HOXA9/MEIS1 mRNA expression after 6 days by real-time PCR analysis B 6.15 pIC50 700 nM IC50 MedChemComm (2012) 3: 135-161
ChEMBL Inhibition of DOT1L in human MV4-11 cells assessed as downregulation of HOXA9/MEIS1 mRNA expression after 6 days by real-time PCR analysis B 6.15 pIC50 700 nM IC50 MedChemComm (2012) 3: 135-161
ChEMBL Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level B 7.08 pIC50 84 nM IC50 J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of recombinant human DOT1L (1 to 416) using [3H]-SAM, SAM and nucleosome as substrate assessed as incorporation of radioactivity into nucleosome preincubated for 30 mins followed by substrate addition measured after 120 mins by flash plate assay B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human recombinant DOT1L using [3H]-SAM as substrate after 30 mins B 9.4 pIC50 0.4 nM IC50 Eur. J. Med. Chem. (2012) 56: 179-194 [PMID:22975593]
ChEMBL Inhibition of recombinant human DOT1L using chicken erythrocyte oligonucleosomes/[3H]-SAM as substrate assessed as incorporation of radioactivity into oligonucleosome preincubated for 30 mins followed by substrate addition measured after 120 mins B 9.4 pIC50 0.4 nM IC50 MedChemComm (2012) 3: 135-161
ChEMBL Competitive inhibition of human recombinant DOT1L (1 to 416 amino acid residues) using [3H]-SAM assessed as inhibition of nucleosome methylation incubated for 30 mins prior to substrate addition measured after 120 mins B 9.4 pIC50 0.4 nM IC50 Bioorg. Med. Chem. (2013) 21: 1787-1794 [PMID:23433670]
GtoPdb - - 9.4 pIC50 0.4 nM IC50 Cancer Cell (2011) 20: 53-65 [PMID:21741596]
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]
protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744Q9BQA1]
ChEMBL Inhibition of human full length PRMT5-MEP50 complex expressed in Sf9 cells B 4.7 pIC50 >20000 nM IC50 ACS Med. Chem. Lett. (2015) 6: 408-412 [PMID:25893041]
protein arginine methyltransferase 7 /Protein arginine N-methyltransferase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562175] [GtoPdb: 1258] [UniProtKB: Q9NVM4]
ChEMBL Inhibition of human full length PRMT7 expressed in Sf9 cells B 5.12 pIC50 7500 nM IC50 ACS Med. Chem. Lett. (2015) 6: 408-412 [PMID:25893041]

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]