IOX2 [Ligand Id: 8229] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3186774 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9] | ||||||||
| ChEMBL | Inhibition of recombinant human PHD2 by alphascreen assay | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
| ChEMBL | Inhibition of human PHD2 | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2019) 62: 5725-5749 [PMID:30682255] |
| GtoPdb | - | - | 7.66 | pIC50 | 22 | nM | IC50 | ACS Chem Biol (2013) 8: 1488-96 [PMID:23683440] |
| 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 | 4 | pIC50 | >=100000 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| 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 | 4 | pIC50 | >=100000 | nM | IC50 | 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 | 4 | pIC50 | >=100000 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| 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 | 4 | pIC50 | >=100000 | nM | IC50 | 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 | 4 | pIC50 | >=100000 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| 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 | 4 | pIC50 | >=100000 | nM | IC50 | 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 | 5.07 | pIC50 | 8500 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
| lysine demethylase 2A in Human [GtoPdb: 2671] [UniProtKB: Q9Y2K7] | ||||||||
| GtoPdb | - | - | 7.28 | pIC50 | 52 | nM | IC50 | ACS Chem Biol (2013) 8: 1488-96 [PMID:23683440] |
| lysine demethylase 5C in Human [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
| GtoPdb | - | - | 6.8 | pIC50 | 159 | nM | IC50 | ACS Chem Biol (2013) 8: 1488-96 [PMID:23683440] |
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]
