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ChEMBL ligand: CHEMBL1230640 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1] | ||||||||
ChEMBL | Inhibition of human hexahistidine-tagged full-length FTO expressed in Escherichia coli BL21 (DE3) using 3-methylthymidine as substrate assessed as inhibition of 3-methylthymidine conversion to thymidine after 1 hr by liquid chromatographic analysis | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2013) 56: 3680-3688 [PMID:23547775] |
egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9] | ||||||||
ChEMBL | Binding affinity to human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by NMR spectroscopic analysis | B | 4.22 | pKd | 60000 | nM | Kd | J Med Chem (2013) 56: 547-555 [PMID:23234607] |
GtoPdb | - | - | 4.48 | pIC50 | 33000 | nM | IC50 | ChemMedChem (2014) 9: 566-71 [PMID:24504543] |
ChEMBL | Inhibition of human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by NMR spectroscopic analysis | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2013) 56: 547-555 [PMID:23234607] |
ChEMBL | Inhibition of recombinant human PHD2 using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by LC-MS analysis | B | 4.84 | pIC50 | 14300 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
lysine demethylase 2A/Lysine-specific demethylase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938210] [GtoPdb: 2671] [UniProtKB: Q9Y2K7] | ||||||||
ChEMBL | Inhibition of KDM2A (unknown origin) | B | 4.8 | pIC50 | 15848.93 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
ChEMBL | Inhibition of recombinant FBXL11 (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2014) 57: 42-55 [PMID:24325601] |
lysine demethylase 3A/Lysine-specific demethylase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938209] [GtoPdb: 2673] [UniProtKB: Q9Y4C1] | ||||||||
ChEMBL | Inhibition of recombinant JMJD1A (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2014) 57: 42-55 [PMID:24325601] |
ChEMBL | Inhibition of KDM3A (unknown origin) | B | 6.8 | pIC50 | 158.49 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | ChemMedChem (2014) 9: 566-71 [PMID:24504543] |
lysine demethylase 4A/Lysine-specific demethylase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5896] [GtoPdb: 2675] [UniProtKB: O75164] | ||||||||
ChEMBL | Inhibition of Flag-tagged JMJD2A in human HeLa cells using H3K9me3 peptide as substrate by immunofluorescence assay | B | 4.06 | pIC50 | 86500 | nM | IC50 | Medchemcomm (2012) 3: 135-161 |
ChEMBL | Inhibition of recombinant human JMJD2A using biotinylated histone H3 as substrate by AlphaScreen assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | Eur J Med Chem (2015) 105: 145-155 [PMID:26491978] |
ChEMBL | Inhibition of JMJD2A catalytic domain by mass spectrophotometric analysis | B | 5.77 | pIC50 | 1700 | nM | IC50 | Eur J Med Chem (2012) 56: 179-194 [PMID:22975593] |
ChEMBL | Inhibition of human Flag-tagged KDM4A expressed in human HeLa cells assessed as increase in H3K9me3 level after 24 hrs by DAPI staining based immunofluorescence assay | B | 4.06 | pEC50 | 87000 | nM | EC50 | J Med Chem (2016) 59: 1308-1329 [PMID:26710088] |
lysine demethylase 4C/Lysine-specific demethylase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6175] [GtoPdb: 2677] [UniProtKB: Q9H3R0] | ||||||||
ChEMBL | Inhibition of KDM4C (unknown origin) | B | 6.2 | pIC50 | 630.96 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
GtoPdb | - | - | 6.22 | pIC50 | 600 | nM | IC50 | ChemMedChem (2014) 9: 566-71 [PMID:24504543] |
ChEMBL | Inhibition of recombinant JMJD2C (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2014) 57: 42-55 [PMID:24325601] |
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
ChEMBL | Inhibition of JMJD2E catalytic domain by mass spectrophotometric analysis | B | 5.62 | pIC50 | 2400 | nM | IC50 | Eur J Med Chem (2012) 56: 179-194 [PMID:22975593] |
ChEMBL | Inhibition of human N-terminal His6-tagged KDM4E catalytic domain (1 to 337 residues) expressed in Escherichia coli using ARK(me3)STGGK as substrate preincubated for 15 mins measured after 30 mins by MALDI-TOF mass spectrometric analysis | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2016) 59: 1308-1329 [PMID:26710088] |
ChEMBL | Inhibition of KDM4E (unknown origin) | B | 6.5 | pIC50 | 316.23 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
ChEMBL | Inhibition of recombinant JMJD2E (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2014) 57: 42-55 [PMID:24325601] |
ChEMBL | Inhibition of N-terminal His-6-tagged human JMJD2E (1 to 337 residues) expressed in Escherichia coli using ARK(me3)STGGK peptide as substrate by MALDI-TOF/MS analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | Medchemcomm (2012) 3: 135-161 |
ChEMBL | Inhibition of human N-terminal His6-tagged KDM4E catalytic domain (1 to 337 residues) expressed in Escherichia coli using ARK(me3)STGGK as substrate preincubated for 15 mins measured after 30 mins by FDH coupled enzyme assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2016) 59: 1308-1329 [PMID:26710088] |
lysine demethylase 5C/Lysine-specific demethylase 5C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
ChEMBL | Inhibition of KDM5C (unknown origin) | B | 4.6 | pIC50 | 25118.86 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
ChEMBL | Inhibition of recombinant JARID1C (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2014) 57: 42-55 [PMID:24325601] |
lysine demethylase 6B/Lysine-specific demethylase 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054] | ||||||||
GtoPdb | - | - | 5.8 | pIC50 | 1600 | nM | IC50 | ChemMedChem (2014) 9: 566-71 [PMID:24504543] |
ChEMBL | Inhibition of recombinant JMJD3 (unknown origin) incubated for 15 mins prior to substrate addition by AlphaScreen method | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2014) 57: 42-55 [PMID:24325601] |
ChEMBL | Inhibition of KDM6B (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
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 | 4.33 | pIC50 | 47200 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
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]