dacinostat [Ligand Id: 7497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL356066 (Dacinostat, NVP-LAQ824)
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  • 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 11/Histone deacetylase 11 in Human [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
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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 4/Histone deacetylase 4 in Human [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
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  • histone deacetylase 5/Histone deacetylase 5 in Human [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • histone deacetylase 7/Histone deacetylase 7 in Human [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
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  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
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  • histone deacetylase 9/Histone deacetylase 9 in Human [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells by automated patch clamp electrophysiology assay B 4.91 pIC50 12200 nM IC50 J. Med. Chem. (2010) 53: 2952-2963 [PMID:20205394]
ChEMBL Inhibition of human ERG by automated patch clamp assay B 4.99 pIC50 10300 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4909-4912 [PMID:21742496]
ChEMBL Inhibition of human ERG by radioligand binding assay B 4.99 pIC50 10300 nM IC50 J. Med. Chem. (2011) 54: 4752-4772 [PMID:21650221]
ChEMBL Inhibition of human ERG by patch clamp assay B 4.99 pIC50 10300 nM IC50 J. Med. Chem. (2011) 54: 4752-4772 [PMID:21650221]
ChEMBL Inhibition of human ERG by manual patch clamp assay B 4.99 pIC50 10300 nM IC50 J. Med. Chem. (2011) 54: 4752-4772 [PMID:21650221]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of human HDAC1 B 9.22 pKi 0.6 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human HDAC1 B 9.26 pKi 0.55 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 9.26 pKi 0.55 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of purified recombinant HDAC1 B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4909-4912 [PMID:21742496]
ChEMBL Inhibition of HDAC1 B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2011) 54: 4752-4772 [PMID:21650221]
ChEMBL Inhibition of FLAG-tagged HDAC1 expressed in HEK293 cells by fluorescent assay B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2010) 53: 2952-2963 [PMID:20205394]
ChEMBL Inhibition of human recombinant HDAC1 B 8.1 pIC50 8 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
ChEMBL Inhibition of recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus after 10 mins by fluorimetric analysis B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of C-terminal FLAG-tagged full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells after 3 hrs by FDL assay B 8.3 pIC50 5 nM IC50 MedChemComm (2017) 8: 767-770
ChEMBL Inhibition of human HDAC1 by fluorimetric assay B 8.49 pIC50 3.23 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of HDAC1 in HEK293 cells B 8.59 pIC50 2.6 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Inhibition of human HDAC10 by fluorimetric assay B 8.08 pIC50 8.41 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
ChEMBL Inhibition of human HDAC11 by fluorimetric assay B 8.25 pIC50 5.58 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
GtoPdb - - 8.85 pKi 1.4 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC2 B 8.85 pKi 1.4 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC2 B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human HDAC2 by fluorimetric assay B 7.8 pIC50 15.7 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus after 10 mins by fluorimetric analysis B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of human recombinant HDAC2 B 8.15 pIC50 7 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
ChEMBL Inhibition of C-terminal FLAG-tagged full length recombinant human HDAC2 expressed in baculovirus infected Sf9 insect cells after 3 hrs by FDL assay B 8.3 pIC50 5 nM IC50 MedChemComm (2017) 8: 767-770
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of human HDAC3 B 8.38 pKi 4.2 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC3 B 8.38 pKi 4.2 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 8.38 pKi 4.2 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC3 by fluorimetric assay B 7.98 pIC50 10.5 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of human recombinant HDAC3 B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
ChEMBL Inhibition of HDAC3 in HEK293 cells B 8.44 pIC50 3.6 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of flag-tagged HDAC3 B 9.4 pIC50 0.4 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
ChEMBL Inhibition of human HDAC4 B 5.65 pKi 2250 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC4 B 5.65 pKi 2250 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 5.65 pKi 2250 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human recombinant N-terminal FLAG-tagged HDAC4 (612-1034) expressed in baculovirus after 10 mins by fluorimetric analysis B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of wild type HDAC4 expressed in Escherichia coli B 6.38 pIC50 420 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of human HDAC4 by fluorimetric assay B 8.24 pIC50 5.82 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of HDAC4 H976Y mutant expressed in Escherichia coli B 8.36 pIC50 4.4 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of flag-tagged HDAC4 by pull-down assay B 8.4 pIC50 4 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of flag-tagged HDAC4 expressed in HEK293 cells by Biomol assay B 8.52 pIC50 3 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of HDAC4 catalytic domain expressed in HEK293 cells by Biomol assay B 8.6 pIC50 2.5 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of flag-tagged HDAC4 B 8.92 pIC50 1.2 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of flag-tagged HDAC4 by Biomol assay B 9 pIC50 1 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
ChEMBL Inhibition of human HDAC5 B 6.38 pKi 420 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC5 B 6.38 pKi 420 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 6.38 pKi 420 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human recombinant N-terminal FLAG-tagged HDAC5 (620-1122) expressed in baculovirus after 10 mins by fluorimetric analysis B 6.72 pIC50 190 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of human HDAC5 by fluorimetric assay B 8.25 pIC50 5.58 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
GtoPdb - - 8.02 pKi 9.5 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC6 B 8.02 pKi 9.5 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC6 B 8.02 pKi 9.5 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of HDAC6 in HEK293 cells B 8.08 pIC50 8.3 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of human HDAC6 by fluorimetric assay B 8.23 pIC50 5.93 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
GtoPdb - - 5.02 pKi 9500 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC7 B 5.02 pKi 9500 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC7 B 5.02 pKi 9500 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human recombinant N-terminal FLAG-tagged HDAC7 (438-915) expressed in baculovirus after 10 mins by fluorimetric analysis B 5.65 pIC50 2240 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of human HDAC7 by fluorimetric assay B 8.21 pIC50 6.11 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Activity of human HDAC8 B 6.47 pKi 340 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC8 B 6.47 pKi 340 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 6.47 pKi 340 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human recombinant HDAC8 B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625]
ChEMBL Inhibition of human HDAC8 by fluorimetric assay B 8.42 pIC50 3.84 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
ChEMBL Inhibition of human HDAC9 B 5.05 pKi 9000 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC9 B 5.05 pKi 9000 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 5.05 pKi 9000 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC9 by fluorimetric assay B 8.08 pIC50 8.24 nM IC50 J. Med. Chem. (2010) 53: 8387-8399 [PMID:21073160]

ChEMBL data shown on this page come from version 28:

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]