BML-281 [Ligand Id: 9664] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL511749
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 10/Histone deacetylase 10 in Human [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
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  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
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  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of recombinant human HDAC1 using Ac-RHKK(Ac)-ACC as substrate by fluorometric analysis B 5.45 pIC50 3567 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7067-7070 [PMID:20947351]
ChEMBL Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis B 6.47 pIC50 340 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7067-7070 [PMID:20947351]
ChEMBL Inhibition of HDAC1 after 17 hrs B 6.57 pIC50 271 nM IC50 J. Med. Chem. (2008) 51: 4370-4373 [PMID:18642892]
GtoPdb - - 7 pIC50 100 nM IC50 J. Med. Chem. (2008) 51: 4370-3 [PMID:18642892]
ChEMBL Inhibition of HDAC1 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay B 7.9 pIC50 12.7 nM IC50 J. Med. Chem. (2013) 56: 6297-6313 [PMID:23627282]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Inhibition of HDAC10 after 17 hrs B 7.04 pIC50 90.7 nM IC50 J. Med. Chem. (2008) 51: 4370-4373 [PMID:18642892]
GtoPdb - - 7.55 pIC50 28.2 nM IC50 J. Med. Chem. (2008) 51: 4370-3 [PMID:18642892]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of HDAC2 after 17 hrs B 6.6 pIC50 252 nM IC50 J. Med. Chem. (2008) 51: 4370-4373 [PMID:18642892]
GtoPdb - - 6.62 pIC50 238 nM IC50 J. Med. Chem. (2008) 51: 4370-3 [PMID:18642892]
ChEMBL Inhibition of HDAC2 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay B 7.03 pIC50 93 nM IC50 J. Med. Chem. (2013) 56: 6297-6313 [PMID:23627282]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of HDAC3 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay B 6.72 pIC50 190 nM IC50 J. Med. Chem. (2013) 56: 6297-6313 [PMID:23627282]
GtoPdb - - 8.7 pIC50 <2 nM IC50 J. Med. Chem. (2008) 51: 4370-3 [PMID:18642892]
ChEMBL Inhibition of HDAC3 after 17 hrs B 9.38 pIC50 0.42 nM IC50 J. Med. Chem. (2008) 51: 4370-4373 [PMID:18642892]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7067-7070 [PMID:20947351]
ChEMBL Inhibition of recombinant human HDAC6 using Ac-RHKK(Ac)-ACC as substrate by fluorometric analysis B 7.57 pIC50 27 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7067-7070 [PMID:20947351]
GtoPdb - - 8.7 pIC50 <2 nM IC50 J. Med. Chem. (2008) 51: 4370-3 [PMID:18642892]
ChEMBL Inhibition of HDAC6 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay B 9.49 pIC50 0.33 nM IC50 J. Med. Chem. (2013) 56: 6297-6313 [PMID:23627282]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
GtoPdb - - 5.09 pIC50 8104 nM IC50 J. Med. Chem. (2008) 51: 4370-3 [PMID:18642892]
ChEMBL Inhibition of HDAC8 after 17 hrs B 5.16 pIC50 6851 nM IC50 J. Med. Chem. (2008) 51: 4370-4373 [PMID:18642892]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]