tacedinaline [Ligand Id: 8367] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL235191 (Tacedinaline, GOE-5549, CI-994, PD-123654)
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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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]
GtoPdb - - 7.3 pKi 50 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC1 B 7.3 pKi 50 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of HDAC1 (unknown origin) by fluorimetric assay B 4.74 pIC50 18220 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919]
ChEMBL Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate by fluorometric assay B 5.79 pIC50 1620 nM IC50 Eur J Med Chem (2017) 134: 1-12 [PMID:28391133]
ChEMBL Inhibition of human recombinant HDAC1 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 5.79 pIC50 1620 nM IC50 Eur J Med Chem (2018) 143: 320-333 [PMID:29202397]
ChEMBL Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2017) 60: 7965-7983 [PMID:28885834]
ChEMBL Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay B 5.96 pIC50 1090 nM IC50 J Med Chem (2018) 61: 7245-7260 [PMID:30045621]
ChEMBL Inhibition of human recombinant HDAC1 B 6.05 pIC50 900 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
GtoPdb - - 6.24 pIC50 570 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 973-8 [PMID:18182289]
ChEMBL Inhibition of HDAC1 B 6.24 pIC50 570 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 973-978 [PMID:18182289]
ChEMBL Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate after 3 hrs by fluorescence assay B 7.22 pIC50 60 nM IC50 J Med Chem (2017) 60: 7965-7983 [PMID:28885834]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of human HDAC2 B 6.72 pKi 190 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 6.82 pKi 150 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of HDAC2 (unknown origin) by fluorimetric assay B 5.41 pIC50 3850 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919]
ChEMBL Inhibition of human recombinant HDAC2 using Fluor de Lys green as substrate by fluorometric assay B 5.92 pIC50 1200 nM IC50 Eur J Med Chem (2017) 134: 1-12 [PMID:28391133]
ChEMBL Inhibition of human recombinant HDAC2 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 5.92 pIC50 1200 nM IC50 Eur J Med Chem (2018) 143: 320-333 [PMID:29202397]
ChEMBL Inhibition of human recombinant HDAC2 B 6.05 pIC50 900 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of human HDAC3 B 6.26 pKi 550 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 6.26 pKi 550 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of HDAC3 (unknown origin) by fluorimetric assay B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919]
ChEMBL Inhibition of human recombinant HDAC3 B 5.92 pIC50 1200 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of HDAC6 (unknown origin) by fluorimetric assay B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919]
ChEMBL Inhibition of human recombinant HDAC6 using Fluor de Lys as substrate after 60 mins by fluorometric assay B 4.4 pIC50 >40000 nM IC50 Eur J Med Chem (2017) 134: 1-12 [PMID:28391133]
ChEMBL Inhibition of human recombinant HDAC6 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 4.4 pIC50 >40000 nM IC50 Eur J Med Chem (2018) 143: 320-333 [PMID:29202397]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Inhibition of human recombinant HDAC8 B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
Nicotinamide phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744525] [UniProtKB: P43490]
ChEMBL Inhibition of human recombinant NAMPT using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence assay B 5.7 pIC50 >2000 nM IC50 J Med Chem (2017) 60: 7965-7983 [PMID:28885834]

ChEMBL data shown on this page come from version 26:

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]