ChEMBL ligand: CHEMBL1230640
Alpha-ketoglutarate-dependent dioxygenase FTO in Human [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1] There should be some charts here, you may need to enable JavaScript!
egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 2A/Lysine-specific demethylase 2A in Human [ChEMBL: CHEMBL1938210] [GtoPdb: 2671] [UniProtKB: Q9Y2K7] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 3A/Lysine-specific demethylase 3A in Human [ChEMBL: CHEMBL1938209] [GtoPdb: 2673] [UniProtKB: Q9Y4C1] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 4A/Lysine-specific demethylase 4A in Human [ChEMBL: CHEMBL5896] [GtoPdb: 2675] [UniProtKB: O75164] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 4C/Lysine-specific demethylase 4C in Human [ChEMBL: CHEMBL6175] [GtoPdb: 2677] [UniProtKB: Q9H3R0] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 5C/Lysine-specific demethylase 5C in Human [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 6B/Lysine-specific demethylase 6B in Human [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054] There should be some charts here, you may need to enable JavaScript!
Prolyl 4-hydroxylase in Paramecium bursaria Chlorella virus 1 [ChEMBL: CHEMBL4523368] [UniProtKB: Q84406] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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]