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ChEMBL ligand: CHEMBL511749 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
ChEMBL | Inhibition of recombinant human HDAC1 using Ac-RHKK(Ac)-ACC as substrate by fluorometric analysis | B | 5.45 | pIC50 | 3567 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of HDAC1 after 17 hrs | B | 6.57 | pIC50 | 271 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of recombinant human HDAC1 expressed in baculovirus expression system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2008) 51: 4370-3 [PMID:18642892] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay | B | 7.9 | pIC50 | 12.7 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
ChEMBL | Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
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 | 6.1 | pIC50 | 794.33 | 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 | 6.5 | pIC50 | 316.23 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
ChEMBL | Inhibition of HDAC10 after 17 hrs | B | 7.04 | pIC50 | 90.7 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
GtoPdb | - | - | 7.55 | pIC50 | 28.2 | nM | IC50 | J Med Chem (2008) 51: 4370-3 [PMID:18642892] |
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
ChEMBL | Inhibition of HDAC2 after 17 hrs | B | 6.6 | pIC50 | 252 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
GtoPdb | - | - | 6.62 | pIC50 | 238 | nM | IC50 | J Med Chem (2008) 51: 4370-3 [PMID:18642892] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay | B | 7.03 | pIC50 | 93 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
ChEMBL | Inhibition of recombinant human His-tagged HDAC3 expressed in baculovirus insect cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 6.12 | pIC50 | 760 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
ChEMBL | Inhibition of HDAC3 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
GtoPdb | - | - | 8.7 | pIC50 | <2 | nM | IC50 | J Med Chem (2008) 51: 4370-3 [PMID:18642892] |
ChEMBL | Inhibition of HDAC3 after 17 hrs | B | 9.38 | pIC50 | 0.42 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of recombinant human HDAC6 using Ac-RHKK(Ac)-ACC as substrate by fluorometric analysis | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of recombinant human N-terminal GST tagged HDAC6 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay | B | 7.86 | pIC50 | 13.8 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
GtoPdb | - | - | 8.7 | pIC50 | <2 | nM | IC50 | J Med Chem (2008) 51: 4370-3 [PMID:18642892] |
ChEMBL | Inhibition of HDAC6 (unknown origin) using carboxyfluorescein (FAM)-labeled acetylated peptide as substrate after 17 hrs by fluorescence-based electrophoretic assay | B | 9.49 | pIC50 | 0.33 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
GtoPdb | - | - | 5.09 | pIC50 | 8104 | nM | IC50 | J Med Chem (2008) 51: 4370-3 [PMID:18642892] |
ChEMBL | Inhibition of HDAC8 after 17 hrs | B | 5.16 | pIC50 | 6851 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of full length recombinant human C-terminal His tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-GlyLys (Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 5.21 | pIC50 | 6210 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
ChEMBL data shown on this page come from version 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]