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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 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]