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ChEMBL ligand: CHEMBL2349526 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 32:
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]