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 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]