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ChEMBL ligand: CHEMBL3188597 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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lysine demethylase 3A/Lysine-specific demethylase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938209] [GtoPdb: 2673] [UniProtKB: Q9Y4C1] | ||||||||
ChEMBL | Inhibition of KDM3A (unknown origin) | B | 4.4 | pIC50 | 39810.72 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
ChEMBL | Inhibition of KDM4E (unknown origin) | B | 4.7 | pIC50 | 19952.62 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
lysine demethylase 5A/Lysine-specific demethylase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424504] [GtoPdb: 2680] [UniProtKB: P29375] | ||||||||
ChEMBL | Binding affinity to KDM5A ARID/PhD1 domain deletion mutant (1 to 588 residues) (unknown origin) by ITC assay | B | 4.92 | pKd | 12000 | nM | Kd | J Med Chem (2018) 61: 10588-10601 [PMID:30392349] |
GtoPdb | - | - | 5.17 | pIC50 | 6800 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
lysine demethylase 6A/Lysine-specific demethylase 6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550] | ||||||||
ChEMBL | Inhibition of KDM6A (880 to 1401 residues) (unknown origin) using H3 ( 21 to 44 residues) K27me3 as substrate preincubated for 15 min followed by substrate addition measured after 15 mins by FDH-coupled demethylase assay | B | 4.16 | pIC50 | 69000 | nM | IC50 | J Med Chem (2018) 61: 10588-10601 [PMID:30392349] |
GtoPdb | - | - | 7.28 | pIC50 | 53 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
lysine demethylase 6B/Lysine-specific demethylase 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054] | ||||||||
ChEMBL | Inhibition of JMJD3 (unknown origin) using biotinylated H3K27me3 peptide as substrate after 1 hr by AlphaLISA assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 721-725 [PMID:26776360] |
ChEMBL | Inhibition of KDM6B (unknown origin) | B | 7.2 | pIC50 | 63.1 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
GtoPdb | - | - | 7.55 | pIC50 | 28 | nM | IC50 |
Nature (2012) 488: 404-8 [PMID:22842901]; Nature (2014) 514: E1-2 [PMID:25279926] |
ChEMBL | Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured after 1 hr by AlphaScreen assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1173-1176 [PMID:30928196] |
Prolyl 4-hydroxylase in Paramecium bursaria Chlorella virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523368] [UniProtKB: Q84406] | ||||||||
ChEMBL | Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-incubated for 5 mins before 2OG as substrate and Fe2 as co-factor addition in presence of L-ascorbate and measured after 5 mins MALDI TOF MS analysis | B | 4.8 | pIC50 | 15900 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
lysine demethylase 5B in Human [GtoPdb: 2681] [UniProtKB: Q9UGL1] | ||||||||
GtoPdb | - | - | 6.77 | pIC50 | 170 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
lysine demethylase 5C in Human [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
GtoPdb | - | - | 6.26 | pIC50 | 550 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
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]