IOX1 [Ligand Id: 8230] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| Alpha-ketoglutarate-dependent dioxygenase AlkB in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5291506] [UniProtKB: P05050] | ||||||||
| ChEMBL | Inhibition of Escherichia coli AlkB DNA repair activity using 1-methyladenine with GC-1meA-AGGTCCCGTAGTGCG sequence as substrate by FDH coupled assay | B | 4.99 | pIC50 | 10200 | nM | IC50 | J Med Chem (2021) 64: 16974-17003 [PMID:34792334] |
| 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] |
| ChEMBL | Inhibition of FTO (unknown origin) | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2021) 64: 16974-17003 [PMID:34792334] |
| 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] |
| ChEMBL | Inhibition of KDM2A (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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 N-terminal His-tagged human KDM4A using ARK(me3)STGGK peptide as substrate preincubated for 15 mins followed by susbtrate addition measured by matrix-assisted laser desorption/ionization-time-of-flight (MALDI-TOF) mass spectrometry method | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2022) 65: 9564-9579 [PMID:35838529] |
| ChEMBL | Inhibition of KDM4A (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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 4B/Lysine-specific demethylase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313832] [GtoPdb: 2676] [UniProtKB: O94953] | ||||||||
| ChEMBL | Inhibition of KDM4B (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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] |
| ChEMBL | Inhibition of KDM4C (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| lysine demethylase 4D/Lysine-specific demethylase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6138] [GtoPdb: 2678] [UniProtKB: Q6B0I6] | ||||||||
| ChEMBL | Inhibition of KDM4D (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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] |
| ChEMBL | Inhibition of KDM4E (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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] |
| ChEMBL | Inhibition of KDM5C (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| lysine demethylase 6A/Lysine-specific demethylase 6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550] | ||||||||
| ChEMBL | Inhibition of KDM6A (unknown origin) expressed in Escherichia coli using Biotin-H3(14-34)K27me3 peptide and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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 KDM6B (unknown origin) expressed in Escherichia coli and measured after 1 hrs by alpha screen assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16609-16625 [PMID:34762429] |
| 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] |
| Methylcytosine dioxygenase TET1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523402] [UniProtKB: Q8NFU7] | ||||||||
| ChEMBL | Inhibition of N-terminal 3xFlag-tagged human TET1 catalytic domain (E1418 to V2136 residues) expressed in Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 30 mins by Alphascreen assay | B | 6.08 | pIC50 | 831.76 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human TET1 catalytic domain (1481 to 2136 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 4.99 | pEC50 | 10232.93 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human TET1 catalytic domain (1481 to 2136 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| Methylcytosine dioxygenase TET2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523344] [UniProtKB: Q6N021] | ||||||||
| ChEMBL | Inhibition of His10-FLAG tagged human TET2 catalytic domain (Q969 to I2002 residues) expressed in Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 10 mins by Alphascreen assay | B | 5.31 | pIC50 | 4897.79 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of N-terminal His6-tagged TET2 (unknown origin) expressed in Escherichia coli assessed as reduction in hmC and fC levels preincubated for 30 mins followed by Fe(II) addition and measured after 1 hrs using 5'-CACmCGGTG-3' palindromic oligonucleotide as substrate by MALDI-TOF MS analysis | B | 5.64 | pIC50 | 2270 | nM | IC50 | RSC Med Chem (2022) 13: 1540-1548 [PMID:36545435] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG tagged human TET2 catalytic domain (1129 to 2002 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 5.16 | pEC50 | 6918.31 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG tagged human TET2 catalytic domain (1129 to 2002 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 5.16 | pEC50 | 6900 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| Methylcytosine dioxygenase TET3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879414] [UniProtKB: O43151] | ||||||||
| ChEMBL | Inhibition of human TET3 catalytic domain (E824 to I1795 residues) expressed in mammalian cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 10 mins by Alphascreen assay | B | 5.57 | pIC50 | 2691.53 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG tagged human TET3 catalytic domain (824 to 1795 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 5.91 | pEC50 | 1230.27 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG tagged human TET3 catalytic domain (824 to 1795 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 5.92 | pEC50 | 1200 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| 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] |
| RNA demethylase ALKBH5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621037] [UniProtKB: Q6P6C2] | ||||||||
| ChEMBL | Inhibition of human ALKBH5 (74 to 294 residues) expressed in Escherichia coli BL21(DE3) V2R-pRARE cells using biotin labeled m6A-ss-RNA with UACACUCGAUCUGG(m6A)CUAAAGCUGCUC sequence as substrate incubated for 1 hr by TopCount scintillation counting method | B | 5.54 | pIC50 | 2900 | nM | IC50 | J Med Chem (2021) 64: 16974-17003 [PMID:34792334] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
