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ChEMBL ligand: CHEMBL2169919 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 human recombinant DOT1L (1 to 416 residues) using chicken erythrocyte oligonucleosomes as substrate and [3H]-SAM incubated for 120 mins by flashplate based assay | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4518-4522 [PMID:27485386] |
ChEMBL | Displacement of [3H]-SAM in recombinant human His-tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 120 mins by radioligand binding assay | B | 9.52 | pKi | 0.3 | nM | Ki | Eur J Med Chem (2020) 189: 112023-112023 [PMID:31978781] |
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 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 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 N-terminal GST-tagged DOT1L (1 to 420 residues) expressed in Escherichia coli BL21 (DE3) using histone as substrate incubated for 1 hr by MTase-glo based luminescence assay | B | 9.07 | pIC50 | 0.86 | nM | IC50 | Eur J Med Chem (2020) 189: 112023-112023 [PMID:31978781] |
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] |
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 (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] |
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: O14744, Q9BQA1] | ||||||||
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 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]