quisinostat [Ligand Id: 7503] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2105763 (Quisinostat, JNJ-26481585, JNJ 26481585) |
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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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]
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