panobinostat [Ligand Id: 7489] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL483254 (LBH589, Farydak, Panobinostat)
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • Histone deacetylase in Plasmodium falciparum [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
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  • 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: O15379Q9Y618]
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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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  • Human immunodeficiency virus type 1 Tat protein in Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1) [ChEMBL: CHEMBL4011] [UniProtKB: P04608]
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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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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Inhibition of BRD4 (unknown origin) B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013]
Histone deacetylase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
ChEMBL Inhibition of HDAC1 in Plasmodium falciparum 3D7 nuclear extract using Ac-RGK(Ac)-AMC fluorogenic peptide as substrate preincubated for 1 hr followed by substrate addition measured after 10 min by fluorescence assay B 8.48 pIC50 3.3 nM IC50 J Med Chem (2017) 60: 4780-4804 [PMID:28241112]
ChEMBL Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells B 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (2009) 52: 2185-2187 [PMID:19317450]
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 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Competitive inhibition of HDAC1 using KI-104 as substrate by fluorescence assay B 8.6 pKi 2.5 nM Ki J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of human HDAC1 B 9 pKi 1 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC1 B 9 pKi 1 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method B 9.27 pKi 0.54 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay B 6.52 pIC50 <300 nM IC50 J. Med. Chem. (2013) 56: 4816-4820 [PMID:23672185]
ChEMBL Inhibition of human recombinant HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by fluorescence based assay B 7.59 pIC50 26 nM IC50 Bioorg Med Chem Lett (2019) 29: 2581-2586 [PMID:31400937]
ChEMBL Inhibition of human KDAC1 using substrate A after 60 mins by fluorescence assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 127: 531-553 [PMID:28109947]
ChEMBL Inhibition of HADC1 (unknown origin) B 7.82 pIC50 <15 nM IC50 J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL Inhibition of recombinant His6/GST-tagged human HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence based assay B 8.15 pIC50 7.03 nM IC50 J Med Chem (2020) 63: 804-815 [PMID:31855601]
ChEMBL Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay B 8.17 pIC50 6.8 nM IC50 J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis B 8.6 pIC50 2.5 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting B 8.6 pIC50 2.5 nM IC50 Drug Metab. Dispos. (2012) 40: 1041-1050 [PMID:22344701]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) B 8.6 pIC50 2.5 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 90 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.67 pIC50 2.14 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.67 pIC50 2.12 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.74 pIC50 1.81 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.75 pIC50 1.78 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of HDAC1 (unknown origin) B 8.85 pIC50 1.4 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ChEMBL Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 8.9 pIC50 1.26 nM IC50 J. Med. Chem. (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. (2016) 24: 4008-4015 [PMID:27377864]
ChEMBL Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 9 pIC50 1 nM IC50 J. Med. Chem. (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay B 9.22 pIC50 0.6 nM IC50 Bioorg Med Chem Lett (2019) 29: 2136-2140 [PMID:31272794]
GtoPdb - - 8.52 pEC50 3 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 Competitive inhibition of HDAC10 using KI-104 as substrate by fluorescence assay B 7.51 pKi 31 nM Ki J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of human recombinant HDAC10 using fluorogenic HDAC substrate after 45 mins by fluorimetrc method B 8.29 pKi 5.1 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of recombinant human His6/GST-tagged HDAC10 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay B 7.99 pIC50 10.24 nM IC50 J Med Chem (2020) 63: 804-815 [PMID:31855601]
ChEMBL Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 8.35 pIC50 4.45 nM IC50 J. Med. Chem. (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of HDAC10 (unknown origin) B 8.68 pIC50 2.1 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
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 5.92 pKi 1200 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Competitive inhibition of HDAC11 using KI-104 as substrate by fluorescence assay B 8.46 pKi 3.5 nM Ki J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 5.39 pIC50 4112 nM IC50 J. Med. Chem. (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 5.39 pIC50 4112 nM IC50 J. Med. Chem. (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of recombinant human His6/GST-tagged HDAC11 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay B 6.92 pIC50 121 nM IC50 J Med Chem (2020) 63: 804-815 [PMID:31855601]
ChEMBL Inhibition of HDAC11 (unknown origin) B 8.8 pIC50 1.6 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
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 7.66 pKi 22 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay B 7.89 pKi 13 nM Ki Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL Competitive inhibition of HDAC2 using KI-104 as substrate by fluorescence assay B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of human HDAC2 B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human HDAC2 B 9.19 pKi 0.65 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay B 6.52 pIC50 <300 nM IC50 J. Med. Chem. (2013) 56: 4816-4820 [PMID:23672185]
ChEMBL Inhibition of human recombinant HDAC2 pre-incubated for 30 mins before substrate addition and measured after 30 mins by fluorescence based assay B 6.87 pIC50 136 nM IC50 Bioorg Med Chem Lett (2019) 29: 2581-2586 [PMID:31400937]
ChEMBL Inhibition of recombinant human His6/GST-tagged HDAC2 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay B 7.64 pIC50 22.83 nM IC50 J Med Chem (2020) 63: 804-815 [PMID:31855601]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) B 7.88 pIC50 13.2 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis B 7.88 pIC50 13.2 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of flag-tagged HDAC2 (unknown origin) expressed in SF21 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting B 7.89 pIC50 13 nM IC50 Drug Metab. Dispos. (2012) 40: 1041-1050 [PMID:22344701]
ChEMBL Inhibition of HDAC2 (unknown origin) B 8.17 pIC50 6.8 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ChEMBL Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 8.48 pIC50 3.28 nM IC50 J. Med. Chem. (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. (2016) 24: 4008-4015 [PMID:27377864]
GtoPdb - - 8.52 pEC50 3 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]
ChEMBL Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate after 10 mins by spectrophotometric method B 8.62 pKi 2.4 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Competitive inhibition of HDAC3 using KI-104 as substrate by fluorescence assay B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of human HDAC3 B 8.96 pKi 1.1 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC3 B 8.96 pKi 1.1 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of HDAC3 (unknown origin) after 60 mins by fluorescence assay B 6.52 pIC50 <300 nM IC50 J. Med. Chem. (2013) 56: 4816-4820 [PMID:23672185]
ChEMBL Inhibition of human KDAC3 using FITC-labeled p53 acetylated peptide as substrate after 60 mins by fluorescence assay B 7.22 pIC50 60 nM IC50 Eur J Med Chem (2017) 127: 531-553 [PMID:28109947]
ChEMBL Inhibition of HADC3 (unknown origin) B 7.82 pIC50 <15 nM IC50 J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL Inhibition of recombinant His6/GST-tagged human HDAC3 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence based assay B 8.23 pIC50 5.83 nM IC50 J Med Chem (2020) 63: 804-815 [PMID:31855601]
ChEMBL Inhibition of HDAC3 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting B 8.68 pIC50 2.1 nM IC50 Drug Metab. Dispos. (2012) 40: 1041-1050 [PMID:22344701]
ChEMBL Inhibition of recombinant HDAC3 (unknown origin) B 8.68 pIC50 2.1 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition full length human recombinant HDAC3 expressed in baculovirus using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. (2016) 24: 4008-4015 [PMID:27377864]
ChEMBL Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of HDAC3 (unknown origin) B 8.82 pIC50 1.5 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
GtoPdb - - 8.4 pEC50 4 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: O15379Q9Y618]
ChEMBL Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 8.64 pIC50 2.27 nM IC50 J. Med. Chem. (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis B 8.68 pIC50 2.1 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 90 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.68 pIC50 2.1 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.69 pIC50 2.06 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.72 pIC50 1.93 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis B 8.78 pIC50 1.67 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
GtoPdb - - 8.4 pEC50 4 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 C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay B 6.19 pKi 640 nM Ki Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL Inhibition of human HDAC4 B 6.26 pKi 550 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC4 B 6.26 pKi 550 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method B 6.77 pKi 170 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Competitive inhibition of HDAC4 using KI-104 as substrate by fluorescence assay B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of recombinant human His6/GST-tagged HDAC4 expressed in baculovirus infected High5 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay B 4.98 pIC50 10390 nM IC50 J Med Chem (2020) 63: 804-815 [PMID:31855601]
ChEMBL Inhibition of N-terminal GST-tagged and C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues ) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay B 6.43 pIC50 373 nM IC50 Bioorg. Med. Chem. (2016) 24: 4008-4015 [PMID:27377864]
ChEMBL Inhibition of recombinant HDAC4 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 6.47 pIC50 338 nM IC50 J. Med. Chem. (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 6.47 pIC50 337.8 nM IC50 J. Med. Chem. (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of HDAC4 (unknown origin) after 60 mins by fluorescence assay B 6.52 pIC50 <300 nM IC50 J. Med. Chem. (2013) 56: 4816-4820 [PMID:23672185]
ChEMBL Inhibition of recombinant HDAC4 (unknown origin) B 6.69 pIC50 203 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of HDAC4 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting B 6.7 pIC50 200 nM IC50 Drug Metab. Dispos. (2012) 40: 1041-1050 [PMID:22344701]
ChEMBL Inhibition of HDAC4 (unknown origin) B 7.57 pIC50 26.7 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
GtoPdb - - 7.92 pEC50 12 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]
ChEMBL Inhibition of human HDAC5 B 7.1 pKi 80 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC5 B 7.1 pKi 80 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method