daminozide [Ligand Id: 7025] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2164243 (N-(Dimethylamino)Succinamic Acid)
  • egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9]
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  • PHD finger protein 8/Histone lysine demethylase PHF8 in Human [ChEMBL: CHEMBL1938212] [GtoPdb: 2698] [UniProtKB: Q9UPP1]
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  • Hypoxia-inducible factor 1-alpha inhibitor in Human [ChEMBL: CHEMBL5909] [UniProtKB: Q9NWT6]
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  • lysine demethylase 2A/Lysine-specific demethylase 2A in Human [ChEMBL: CHEMBL1938210] [GtoPdb: 2671] [UniProtKB: Q9Y2K7]
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  • lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
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  • lysine demethylase 5C/Lysine-specific demethylase 5C in Human [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229]
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  • lysine demethylase 6A/Lysine-specific demethylase 6A in Human [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550]
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  • lysine demethylase 6B/Lysine-specific demethylase 6B in Human [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054]
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  • lysine demethylase 7A/Lysine-specific demethylase 7 in Human [ChEMBL: CHEMBL2163177] [GtoPdb: 2686] [UniProtKB: Q6ZMT4]
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  • Prolyl 4-hydroxylase in Paramecium bursaria Chlorella virus 1 [ChEMBL: CHEMBL4523368] [UniProtKB: Q84406]
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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 human PHD2 expressed in Escherichia coli by fluorescence based assay B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
Gamma-butyrobetaine dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163175] [UniProtKB: O75936]
ChEMBL Inhibition of human BBOX1 by fluorescence based assay B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
PHD finger protein 8/Histone lysine demethylase PHF8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938212] [GtoPdb: 2698] [UniProtKB: Q9UPP1]
ChEMBL Inhibition of KDM7B (unknown origin) using H3K4me3K9me2 and 2-oxoglutarate as substrate after 1 hr by matrix-assisted laser desorption ionization time of flight mass spectrometry B 4.72 pIC50 19000 nM IC50 J Med Chem (2013) 56: 7222-7231 [PMID:23964788]
ChEMBL Inhibition of human PHF8 expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay B 6.26 pIC50 550 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
ChEMBL Inhibition of KDM7B (unknown origin) by alphascreen assay B 6.26 pIC50 550 nM IC50 J Med Chem (2013) 56: 7222-7231 [PMID:23964788]
GtoPdb - - 6.26 pIC50 550 nM IC50 J Med Chem (2012) 55: 6639-43 [PMID:22724510]
Hypoxia-inducible factor 1-alpha inhibitor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5909] [UniProtKB: Q9NWT6]
ChEMBL Inhibition of human FIH expressed in Escherichia coli by MALDI assay B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
lysine demethylase 2A/Lysine-specific demethylase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938210] [GtoPdb: 2671] [UniProtKB: Q9Y2K7]
ChEMBL Mixed type inhibition of human KDM2A expressed in Escherichia coli assessed inhibition constant for compound-enzyme-substrate complex using methyl lysine peptide substrate by enzyme kinetic assay B 4.07 pKi 85000 nM Ki J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
ChEMBL Competitive inhibition of human KDM2A expressed in Escherichia coli using 2-oxoglutarate by enzyme kinetic assay B 5.71 pKi 1970 nM Ki J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
GtoPdb - - 5.82 pIC50 1500 nM IC50 J Med Chem (2012) 55: 6639-43 [PMID:22724510]
ChEMBL Inhibition of human KDM2A expressed in Escherichia coli by formaldehyde dehydrogenase coupled assay B 5.82 pIC50 1500 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
ChEMBL Inhibition of human KDM2A expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay B 5.82 pIC50 1500 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
ChEMBL Inhibition of KDM2A (unknown origin) B 5.82 pIC50 1500 nM IC50 J Med Chem (2013) 56: 7222-7231 [PMID:23964788]
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
ChEMBL Inhibition of human KDM4E expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
lysine demethylase 5C/Lysine-specific demethylase 5C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229]
ChEMBL Inhibition of human KDM5C catalytic domain expressed in Sf9 cells using methyl lysine peptide substrate by AlphaScreen assay B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
lysine demethylase 6A/Lysine-specific demethylase 6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550]
ChEMBL Inhibition of human recombinant KDM6A after 1 hr B 4 pIC50 >100000 nM IC50 J Med Chem (2013) 56: 7222-7231 [PMID:23964788]
lysine demethylase 6B/Lysine-specific demethylase 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054]
ChEMBL Inhibition of human KDM6B catalytic domain expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
lysine demethylase 7A/Lysine-specific demethylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163177] [GtoPdb: 2686] [UniProtKB: Q6ZMT4]
ChEMBL Inhibition of human KDM7A catalytic domain expressed in Escherichia coli by MALDI assay B 5.68 pIC50 2100 nM IC50 J Med Chem (2012) 55: 6639-6643 [PMID:22724510]
GtoPdb - - 5.68 pIC50 2100 nM IC50 J Med Chem (2012) 55: 6639-43 [PMID:22724510]
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 pIC50 >100000 nM IC50 Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]

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]