quisinostat [Ligand Id: 7503] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105763 (Quisinostat, JNJ-26481585, JNJ 26481585)
  • 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 in Schistosoma mansoni [ChEMBL: CHEMBL3797017] [UniProtKB: A5H660]
  • 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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  • sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
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  • sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
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  • sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
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  • sirtuin 7/NAD-dependent protein deacetylase sirtuin-7 in Human [ChEMBL: CHEMBL2163184] [GtoPdb: 2713] [UniProtKB: Q9NRC8]
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  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum 3D7 [GtoPdb: 3072] [UniProtKB: Q7K6A1]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum Dd2 [GtoPdb: 3072]
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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 recombinant HDAC1 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method B 8.14 pKi 7.3 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method B 9.32 pKi 0.48 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC1 B 10.52 pKi 0.03 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay B 9.21 pIC50 0.62 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
GtoPdb - - 9.96 pIC50 0.11 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Inhibition of human recombinant HDAC10 using fluorogenic HDAC substrate after 45 mins by fluorimetrc method B 8.36 pKi 4.4 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC10 B 10.3 pKi 0.05 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay B 7.4 pIC50 39.81 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay B 8 pIC50 10 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay B 8.71 pIC50 1.96 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
GtoPdb - - 9.34 pIC50 0.46 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
ChEMBL Inhibition of human recombinant HDAC11 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method B 5.89 pKi 1300 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC11 B 10.15 pKi 0.07 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 9.43 pIC50 0.37 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of human recombinant HDAC2 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method B 7.51 pKi 31 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC2 B 10.22 pKi 0.06 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay B 8.67 pIC50 2.16 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
GtoPdb - - 9.48 pIC50 0.33 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate after 10 mins by spectrophotometric method B 8.37 pKi 4.3 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC3 B 8.68 pKi 2.1 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 8.31 pIC50 4.86 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
ChEMBL Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method B 8.17 pKi 6.7 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC4 B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay B 8.34 pIC50 4.61 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
GtoPdb - - 9.19 pIC50 0.64 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
ChEMBL Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method B 8.37 pKi 4.3 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC5 B 8.68 pKi 2.1 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay B 8.23 pIC50 5.95 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
GtoPdb - - 8.43 pIC50 3.69 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate after 30 mins by fluorimetrc method B 6.46 pKi 350 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC6 B 7.77 pKi 16.9 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 7.11 pIC50 76.8 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
ChEMBL Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis B 7.11 pIC50 76.8 nM IC50 J Med Chem (2016) 59: 8967-9004 [PMID:27606546]
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
ChEMBL Inhibition of human HDAC7 B 7.18 pKi 66.6 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2a after 45 mins by fluorimetrc method B 8.77 pKi 1.7 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
GtoPdb - - 6.92 pIC50 119 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
ChEMBL Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay B 8.39 pIC50 4.04 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
Histone deacetylase 8 in Schistosoma mansoni (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797017] [UniProtKB: A5H660]
ChEMBL Binding affinity to Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method B 7.55 pKd 28.4 nM Kd J Med Chem (2018) 61: 10000-10016 [PMID:30347148]
ChEMBL Inhibition of Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method B 6.52 pIC50 303.4 nM IC50 J Med Chem (2018) 61: 10000-10016 [PMID:30347148]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Binding affinity to human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method B 7.64 pKd 22.7 nM Kd J Med Chem (2018) 61: 10000-10016 [PMID:30347148]
ChEMBL Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC8 B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method B 6.66 pIC50 217 nM IC50 J Med Chem (2018) 61: 10000-10016 [PMID:30347148]
ChEMBL Inhibition of human His-thioredoxin-tagged HDAC8 mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method B 6.77 pIC50 169 nM IC50 J Med Chem (2018) 61: 10000-10016 [PMID:30347148]
ChEMBL Inhibition of human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method B 7.19 pIC50 64.4 nM IC50 J Med Chem (2018) 61: 10000-10016 [PMID:30347148]
GtoPdb - - 8.37 pIC50 4.26 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
ChEMBL Inhibition of human recombinant HDAC9 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method B 8.28 pKi 5.3 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human HDAC9 B 8.42 pKi 3.8 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 7.49 pIC50 32.1 nM IC50 Clin Cancer Res (2009) 15: 6841-51 [PMID:19861438]
ChEMBL Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay B 8.17 pIC50 6.7 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
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]
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
ChEMBL Inhibition of human recombinant SIRT1 using fluorogenic HDAC substrate after 20 mins by fluorimetrc method B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Inhibition of human recombinant SIRT2 using fluoro-lysine sirtuin 2 deacetylase substrate after 60 mins by fluorimetrc method B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
ChEMBL Inhibition of human recombinant SIRT3 using fluoro-lysine sirtuin 2 deacetylase substrate after 45 mins by fluorimetrc method B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
sirtuin 7/NAD-dependent protein deacetylase sirtuin-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163184] [GtoPdb: 2713] [UniProtKB: Q9NRC8]
ChEMBL Inhibition of SIRT7 (unknown origin) B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum 3D7 [GtoPdb: 3072] [UniProtKB: Q7K6A1]
GtoPdb Parasite growth inhibition assay - 8.28 pEC50 5.2 nM EC50 Cell Discov (2020) 6: 93 [PMID:33311461]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum Dd2 [GtoPdb: 3072]
GtoPdb Parasite growth inhibition assay - 8.15 pEC50 7.1 nM EC50 Cell Discov (2020) 6: 93 [PMID:33311461]

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]