givinostat [Ligand Id: 7490] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1213492 (Givinostat)
  • 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 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618]
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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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  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
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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 human HDAC1 B 8.7 pKi 2 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC1 B 8.7 pKi 2 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 8.7 pKi 2 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.88 pIC50 133 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL Inhibition of recombinant human C-terminal His-tagged HDAC1 expressed in Sf9 insect cells using Fluor de Lys deacetylase or Fluor de Lys Green deacetylase as substrate by fluorescent microplate reader assay B 7.15 pIC50 70 nM IC50 ACS Med Chem Lett (2021) 12: 1810-1817 [PMID:34795871]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis B 7.46 pIC50 35 nM IC50 J Med Chem (2022) 65: 15457-15472 [PMID:36351184]
GtoPdb - - 7.55 pEC50 28 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Inhibition of recombinant human HDAC10 (2 to 631 residues) expressed in baculovirus infected sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.48 pIC50 331 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
ChEMBL Inhibition of recombinant human HDAC11 expressed in baculovirus infected sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.54 pIC50 287 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
GtoPdb - - 8.52 pKi 3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC2 B 8.52 pKi 3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC2 B 8.52 pKi 3 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human HDAC2 expressed in Sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.53 pIC50 293 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
GtoPdb - - 7.25 pEC50 56 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
GtoPdb - - 8.52 pKi 3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC3 B 8.52 pKi 3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC3 B 8.52 pKi 3 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 7.68 pEC50 21 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618]
GtoPdb - - 8.52 pKi 3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human C-terminal His-tagged HDAC3 (1 to 428 residues)/human N-terminal GST-tagged NcoR2 (395 to 489 residues) expressed in sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.87 pIC50 136 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
GtoPdb - - 7.68 pEC50 21 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
ChEMBL Inhibition of human HDAC4 B 5.98 pKi 1050 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC4 B 5.98 pKi 1050 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 5.98 pKi 1050 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC4 expressed in baculovirus infected sf9 cells using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6 pIC50 >1000 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
GtoPdb - - 7.28 pEC50 52 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
GtoPdb - - 6.22 pKi 600 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC5 B 6.22 pKi 600 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC5 B 6.22 pKi 600 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human HDAC5 using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.27 pIC50 532 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of human HDAC6 B 8.38 pKi 4.2 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC6 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 recombinant human HDAC6 using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.51 pIC50 312 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method B 7.36 pIC50 44 nM IC50 J Med Chem (2019) 62: 10711-10739 [PMID:31710483]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 7.46 pIC50 35.02 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
ChEMBL Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in Sf9 insect cells using Fluor de Lys deacetylase or Fluor de Lys Green deacetylase substrate by fluorescent microplate reader assay B 7.64 pIC50 23 nM IC50 ACS Med Chem Lett (2021) 12: 1810-1817 [PMID:34795871]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis B 7.85 pIC50 14 nM IC50 J Med Chem (2022) 65: 15457-15472 [PMID:36351184]
GtoPdb - - 7.57 pEC50 27 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
ChEMBL Inhibition of human HDAC7 B 6.62 pKi 240 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC7 B 6.62 pKi 240 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 6.62 pKi 240 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected sf9 cells using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.28 pIC50 524 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
GtoPdb - - 6.79 pEC50 163 nM EC50 Biochem J (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Activity of human HDAC8 B 7.41 pKi 39 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC8 B 7.41 pKi 39 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 7.41 pKi 39 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of recombinant human C-terminal His-tagged HDAC8 expressed in baculovirus infected sf9 cells using Fluor-de-lys as substrate by fluorometric method B 6.08 pIC50 837 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
ChEMBL Inhibition of human HDAC9 B 6.41 pKi 390 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC9 B 6.41 pKi 390 nM Ki Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 6.41 pKi 390 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected sf9 cells using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method B 6.29 pIC50 512 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
Histone deacetylase HD1B in Zea mays (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3541] [UniProtKB: Q9ZTP8]
ChEMBL Inhibition of maize HD1B B 8.12 pIC50 7.5 nM IC50 Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
ChEMBL Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 1817-1828 [PMID:28218840]

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]