ChEMBL ligand: CHEMBL2018302 (Tubastatin A)
histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] histone deacetylase 1/Histone deacetylase 1 in Mouse [ChEMBL: CHEMBL4001] [GtoPdb: 2658] [UniProtKB: O09106] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 10/Histone deacetylase 10 in Human [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 11/Histone deacetylase 11 in Human [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 4/Histone deacetylase 4 in Human [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 5/Histone deacetylase 5 in Human [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] histone deacetylase 6/Histone deacetylase 6 in Mouse [ChEMBL: CHEMBL2878] [GtoPdb: 2618] [UniProtKB: Q9Z2V5] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 7/Histone deacetylase 7 in Human [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] There should be some charts here, you may need to enable JavaScript!
Histone deacetylase 8 in Schistosoma mansoni [ChEMBL: CHEMBL3797017] [UniProtKB: A5H660] histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 9/Histone deacetylase 9 in Human [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] There should be some charts here, you may need to enable JavaScript!
Polyamine deacetylase HDAC10 in Danio rerio [ChEMBL: CHEMBL4802002] [UniProtKB: F1QCV2] There should be some charts here, you may need to enable JavaScript!

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 HDAC1	B	5.42	pKi	3823.3	nM	Ki	Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL	Binding affinity to recombinant HDAC1 (unknown origin) assessed as inhibition constant using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	5.89	pKi	1280	nM	Ki	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2012) 55: 9891-9899 [PMID:23009203]
ChEMBL	Inhibition of N-terminal GST-tagged full length human HDAC1 expressed in baculovirus system using FTS as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based analysis	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875]
ChEMBL	Inhibition of human recombinant HDAC1 protein using RHKKAc from p53 as substrate	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL	Inhibition of human recombinant HDAC1 using RHKKAc as substrate	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of full length GST-tagged human HDAC1 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay	B	4.79	pIC50	16400	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2015) 96: 340-359 [PMID:25899338]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2018) 157: 447-461 [PMID:30103193]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of HDAC1 (unknown origin) using fluorogenic peptide RHKKAc-AMC as substrate by fluorescence-based assay	B	4.79	pIC50	16400	nM	IC50	Bioorg Med Chem Lett (2023) 81: 129148-129148 [PMID:36690041]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of human recombinant HDAC1 using RHKKAc as substrate	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2022) 65: 3080-3097 [PMID:35148101]
ChEMBL	Inhibition of HADC1 (unknown origin)	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL	Inhibition of human recombinant HDAC1 using RHKKAc peptide as substrate incubated for 5 to mins prior to substrate addition measured after 2 hrs	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2012) 55: 639-651 [PMID:22165909]
ChEMBL	Inhibition of recombinant human HDAC1 using RHKKAc fluorogenic peptide substrate	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL	Inhibition of human HDAC1 using p53 fluorogenic peptide (379 to 382 residues) RHKKAc as substrate by fluorescence-based assay	B	4.79	pIC50	16400	nM	IC50	Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060]
ChEMBL	Inhibition of HDAC1 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay	B	4.79	pIC50	16400	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of recombinant human HDAC1 using Fluor de Lys-SIRT1 as substrate incubated for 15 mins by fluorescence assay	B	4.84	pIC50	14350	nM	IC50	Eur J Med Chem (2016) 116: 126-135 [PMID:27060764]
GtoPdb	-	-	4.86	pIC50	13800	nM	IC50	US8748451. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.86	pIC50	13800	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells by using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504]
ChEMBL	Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf21 cells using RHKK(Ac) as substrate after 60 mins by fluorimetric method	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2017) 127: 115-127 [PMID:28038324]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	5.09	pIC50	8100	nM	IC50	J Med Chem (2020) 63: 10246-10262 [PMID:32815366]
ChEMBL	Inhibition of human HDAC1	B	5.09	pIC50	8100	nM	IC50	Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL	Inhibition of human full length recombinant HDAC1 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	5.1	pIC50	8000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay	B	5.12	pIC50	7582.5	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of recombinant human HDAC1 using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay	B	5.15	pIC50	7048	nM	IC50	Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778]
ChEMBL	Inhibition of HDAC1 (unknown origin) measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of recombinant human HDAC1 using RHKKAc peptide as substrate	B	5.49	pIC50	3259	nM	IC50	Eur J Med Chem (2022) 229: 114090-114090 [PMID:34992037]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	5.49	pIC50	3200	nM	IC50	J Med Chem (2021) 64: 26-41 [PMID:33346659]
ChEMBL	Inhibition of HDAC1 (unknown origin)	B	5.52	pIC50	>3000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of human recombinant HDAC1 using fluorogenic substrate measured after 30 mins	B	5.53	pIC50	2980	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of human recombinant HDAC1 using fluorogenic substrate measured after 30 mins	B	5.53	pIC50	2977	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of recombinant human KDAC1 using acetylated p53 (379 to 382 residues) as substrate by fluorescence assay	B	5.54	pIC50	2870	nM	IC50	J Med Chem (2016) 59: 1613-1633 [PMID:26681404]
ChEMBL	Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA	B	5.57	pIC50	2700	nM	IC50	ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
ChEMBL	Inhibition of HDAC1 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method	B	5.57	pIC50	2700	nM	IC50	Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL	Inhibition of full length his6/FLAG-tagged human recombinant HDAC1(1 to 482 residues) expressed in Sf9 insect cells	B	5.57	pIC50	2700	nM	IC50	J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL	Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay	B	5.6	pIC50	2490	nM	IC50	Medchemcomm (2019) 10: 1109-1115 [PMID:31391882]
ChEMBL	Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis	B	5.6	pIC50	2490	nM	IC50	J Med Chem (2022) 65: 15457-15472 [PMID:36351184]
ChEMBL	Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay	B	5.6	pIC50	2490	nM	IC50	J Med Chem (2020) 63: 10339-10351 [PMID:32803970]
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 microplate reader analysis	B	5.65	pIC50	2240	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using MOCPAC as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis	B	5.7	pIC50	>2000	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925]
ChEMBL	Inhibition of full length C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using ZMAL as substrate incubated for 90 mins by fluorescence assay	B	5.72	pIC50	1910	nM	IC50	ACS Med Chem Lett (2020) 11: 2268-2276 [PMID:33214839]
ChEMBL	Inhibition of recombinant C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay	B	5.72	pIC50	1910	nM	IC50	J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL	Inhibition of recombinant human HDAC1 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay	B	5.72	pIC50	1910	nM	IC50	Eur J Med Chem (2022) 234: 114272-114272 [PMID:35306288]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.85	pIC50	1400	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis	B	5.95	pIC50	1109.7	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925]
ChEMBL	Inhibition of human HDAC1 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay	B	6.12	pIC50	752	nM	IC50	J Med Chem (2021) 64: 1116-1126 [PMID:33356256]
ChEMBL	Inhibition of HDAC1 (unknown origin) measured by fluorescence based assay	B	6.41	pIC50	392	nM	IC50	Bioorg Med Chem (2022) 73: 117028-117028 [PMID:36182802]
ChEMBL	Inhibition of HDAC1 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	6.84	pIC50	144	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
histone deacetylase 1/Histone deacetylase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4001] [GtoPdb: 2658] [UniProtKB: O09106]
ChEMBL	Inhibition of HDAC1 in mouse N2A cells	B	5.09	pIC50	8100	nM	IC50	ACS Med Chem Lett (2020) 11: 706-712 [PMID:32435374]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL	Inhibition of HDAC10 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL	Inhibition of human recombinant HDAC10 using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of N-terminal GST-tagged human HDAC10 (1 to 481 residues) using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC10 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC10 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC10 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of human recombinant HDAC10 protein using RHKKAc from p53 as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of HDAC10 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of human full length recombinant HDAC10 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	4.6	pIC50	25000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.43	pIC50	3710	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
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	7.9	pIC50	12.59	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	7.9	pIC50	12.59	nM	IC50	J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
ChEMBL	Inhibition of HDAC11 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL	Inhibition of human recombinant HDAC11 using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of full length N-terminal GST-tagged human HDAC11 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC11 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of HDAC11 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC11 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC11 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of human recombinant HDAC11 protein using RHKKAc from p53 as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human full length recombinant HDAC11 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	4.8	pIC50	16000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of human recombinant HDAC11 using fluorogenic substrate measured after 30 mins	B	5.06	pIC50	8780	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of recombinant human HDAC11 measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of HDAC11 (unknown origin) measured by fluorescence based assay	B	5.3	pIC50	>5000	nM	IC50	Bioorg Med Chem (2022) 73: 117028-117028 [PMID:36182802]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.42	pIC50	3790	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
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	5.24	pKi	5770	nM	Ki	Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL	Inhibition of human recombinant HDAC2 using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2022) 65: 3080-3097 [PMID:35148101]
ChEMBL	Inhibition of human recombinant HDAC2 protein using RHKKAc from p53 as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL	Inhibition of human recombinant HDAC2 using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of full length C-terminal 6x-His tagged human HDAC2 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC2 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of human recombinant full-length C-terminal GST-tagged HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HADC2 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL	Inhibition of human HDAC2 using p53 fluorogenic peptide (379 to 382 residues) RHKKAc as substrate by fluorescence-based assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060]
ChEMBL	Inhibition of HDAC2 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC2 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of human full length recombinant HDAC2 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	4.72	pIC50	19000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of full length human recombinant C-terminal GST-tagged HDAC2 expressed in insect cells using RHKK(Ac) as substrate after 60 mins by fluorimetric method	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2017) 127: 115-127 [PMID:28038324]
ChEMBL	Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504]
ChEMBL	Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay	B	5.06	pIC50	8674.5	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.2	pIC50	6270	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of recombinant HDAC2 (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 microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC2 (unknown origin) measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of HDAC2 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method	B	5.41	pIC50	3900	nM	IC50	Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL	Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA	B	5.41	pIC50	3900	nM	IC50	ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
ChEMBL	Inhibition of full length C-terminal his6-tagged human recombinant HDAC2 (1 to 488 residues)	B	5.41	pIC50	3900	nM	IC50	J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL	Inhibition of recombinant human HDAC2 using RHKKAc peptide as substrate	B	5.45	pIC50	3575	nM	IC50	Eur J Med Chem (2022) 229: 114090-114090 [PMID:34992037]
ChEMBL	Inhibition of HDAC2 (unknown origin)	B	5.52	pIC50	>3000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of human recombinant HDAC2 using fluorogenic substrate measured after 30 mins	B	5.53	pIC50	2920	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of HDAC2 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	6.44	pIC50	360	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL	Inhibition of HDAC3 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of full length C-terminal 6x-His tagged human HDAC3 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC3 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of human recombinant full-length C-terminal GST-tagged HDAC3 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HADC3 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL	Inhibition of HDAC3 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC3 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of recombinant HDAC3 (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 microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC3 (unknown origin)	B	5.52	pIC50	>3000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA	B	5.54	pIC50	2900	nM	IC50	ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
ChEMBL	Inhibition of full length C-terminal his6/FLAG-tagged human recombinant HDAC3 (1 to 2383 residues) expressed in Sf9 insect cells	B	5.54	pIC50	2900	nM	IC50	J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL	Inhibition of HDAC3 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method	B	5.54	pIC50	2900	nM	IC50	Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL	Inhibition of HDAC3 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	6.81	pIC50	155	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618]
ChEMBL	Inhibition of HDAC3/NcoR2 (unknown origin) using RHKKAc as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of HDAC3/NcoR2 (unknown origin) using RHKKAc from p53 as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human full length recombinant HDAC3/ NcoR2 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	5.1	pIC50	8000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of recombinant human HDAC3/NcoR2 using RHKKAc peptide as substrate	B	5.31	pIC50	4948	nM	IC50	Eur J Med Chem (2022) 229: 114090-114090 [PMID:34992037]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.9	pIC50	1270	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of recombinant human KDAC3/NcoR2 using acetylated p53 (379 to 382 residues) as substrate by fluorescence assay	B	6.11	pIC50	770	nM	IC50	J Med Chem (2016) 59: 1613-1633 [PMID:26681404]
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	5.27	pKi	5380	nM	Ki	Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL	Inhibition of HDAC4 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of human recombinant HDAC4 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human recombinant HDAC4 using acetyl-Lys(trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of N-terminal GST-tagged human HDAC4 (627 to 1085 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC4 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of HDAC4 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC4 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC4 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.76	pIC50	17300	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of HDAC4 (unknown origin) measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of recombinant HDAC4 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of human recombinant HDAC4 using fluorogenic substrate measured after 30 mins	B	5.37	pIC50	4270	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of human full length recombinant HDAC4 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	5.52	pIC50	3000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of HDAC4 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	5.96	pIC50	1100	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
ChEMBL	Inhibition of HDAC5 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of human recombinant HDAC5 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human recombinant HDAC5 using acetyl-Lys(trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of C-terminal 6x-His tagged human HDAC5 (657 to 1123 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC5 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of HDAC5 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC5 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC5 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of recombinant HDAC5 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC5 (unknown origin) measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.47	pIC50	3350	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of HDAC5 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	5.64	pIC50	2300	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
ChEMBL	Inhibition of human full length recombinant HDAC5 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	6	pIC50	1000	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL	Inhibition of N-terminal GST-tagged recombinant human HDAC6 (1 to 1215 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	8	pKi	10	nM	Ki	Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL	Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus-infected Sf9 insect cells using RHKK(Ac)AMC as substrate after 90 mins by fluorimeter	B	8.12	pKi	7.56	nM	Ki	J Med Chem (2018) 61: 3454-3477 [PMID:29589441]
ChEMBL	Binding affinity to recombinant HDAC6 (unknown origin) assessed as inhibition constant using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	8.4	pKi	4	nM	Ki	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of human full-length recombinant HDAC6 expressed in baculovirus infected Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay	B	8.46	pKi	3.43	nM	Ki	J Med Chem (2019) 62: 857-874 [PMID:30525585]
ChEMBL	Inhibition of human HDAC6	B	8.48	pKi	3.3	nM	Ki	Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL	Inhibition of full length human HDAC6 using FAM-labeled acetylated peptide as substrate by electrophoretic mobility shift assay	B	4.82	pIC50	15000	nM	IC50	J Med Chem (2021) 64: 2691-2704 [PMID:33576627]
ChEMBL	Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay	B	5.6	pIC50	2500	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Inhibition of recombinant human HDAC8 using RHKKAc fluorogenic peptide substrate	B	6.07	pIC50	854	nM	IC50	J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL	Inhibition of HDAC6 (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 human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry	B	6.93	pIC50	118	nM	IC50	Eur J Med Chem (2021) 211: 113095-113095 [PMID:33360560]
ChEMBL	Inhibition of dye-labeled tracer binding to HDAC6 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay	B	7	pIC50	100	nM	IC50	J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL	Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis	B	7.03	pIC50	94.3	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925]
ChEMBL	Inhibition of recombinant HDAC6 (unknown origin) 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	7.1	pIC50	78.74	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay	B	7.19	pIC50	64.04	nM	IC50	Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778]
ChEMBL	Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis	B	7.46	pIC50	34.9	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925]
ChEMBL	Inhibition of full length C-terminal FLAG-tagged human recombinant HDAC6 expressed inSf9 insect cells	B	7.51	pIC50	31	nM	IC50	J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL	Inhibition of HDAC6 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method	B	7.51	pIC50	31	nM	IC50	Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL	Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA	B	7.51	pIC50	31	nM	IC50	ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
ChEMBL	Inhibition of human recombinant N-terminal GST-tagged full length HDAC6 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay	B	7.52	pIC50	30.4	nM	IC50	Eur J Med Chem (2018) 157: 127-138 [PMID:30092367]
ChEMBL	Inhibition of full length N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using ZMAL as substrate incubated for 90 mins by fluorescence assay	B	7.52	pIC50	30.4	nM	IC50	ACS Med Chem Lett (2020) 11: 2268-2276 [PMID:33214839]
ChEMBL	Inhibition of recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay	B	7.52	pIC50	30	nM	IC50	J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL	Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 as substrate incubated for 15 mins by fluorescence assay	B	7.54	pIC50	28.88	nM	IC50	Eur J Med Chem (2016) 116: 126-135 [PMID:27060764]
ChEMBL	Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	7.54	pIC50	28.71	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of recombinant HDAC6 (unknown origin) 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	7.55	pIC50	28.28	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC6 (unknown origin) using Ac-LeuGlyLy-s(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence microtiter plate reader assay	B	7.56	pIC50	27.4	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of recombinant HDAC6 (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 microplate reader analysis	B	7.57	pIC50	27	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 0 min followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	7.58	pIC50	26.35	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 120 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	7.59	pIC50	25.76	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method	B	7.68	pIC50	21	nM	IC50	J Med Chem (2019) 62: 10711-10739 [PMID:31710483]
ChEMBL	Inhibition of recombinant human HDAC6 using fluorogenic HDAC substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence analysis	B	7.7	pIC50	20	nM	IC50	Bioorg Med Chem (2018) 26: 5718-5729 [PMID:30385227]
ChEMBL	Inhibition of N-terminal GST-tagged full-length human HDAC6 expressed in Sf9 infected baculovirus system using FTS as substrate preincubated for 10 mins followed by substrate addition and measured for 30 mins	B	7.72	pIC50	18.9	nM	IC50	Eur J Med Chem (2021) 218: 113383-113383 [PMID:33799069]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.74	pIC50	18	nM	IC50	J Med Chem (2021) 64: 26-41 [PMID:33346659]
ChEMBL	Inhibition of N-terminal GST-tagged full length human HDAC6 expressed in baculovirus system using FTS as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based analysis	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875]
ChEMBL	Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	B	7.82	pIC50	15	nM	IC50	J Med Chem (2012) 55: 9891-9899 [PMID:23009203]
ChEMBL	Inhibition of human recombinant HDAC6 protein using RHKKAc from p53 as substrate	B	7.82	pIC50	15	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate	B	7.82	pIC50	15	nM	IC50	J Med Chem (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL	Inhibition of human recombinant HDAC6 using RHKKAc as substrate	B	7.82	pIC50	15	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of recombinant human HDAC-6 using RHKKAc as substrate	B	7.82	pIC50	15	nM	IC50	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of recombinant N-GST-tagged HDAC6 (unknown origin) assessed as reduction in deacetylation of Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorescence assay	B	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2014) 24: 4826-4830 [PMID:25240614]
ChEMBL	Inhibition of recombinant human HDAC6 using RHKKAc as substrate by fluorescence assay	B	7.82	pIC50	15	nM	IC50	J Med Chem (2015) 58: 7611-7633 [PMID:26086931]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of human recombinant full-length HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2018) 150: 506-524 [PMID:29549837]
ChEMBL	Inhibition of human recombinant HDAC6 using RHKKAcAMC as substrate by fluorescence assay	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2018) 152: 329-357 [PMID:29738953]
ChEMBL	Inhibition of HADC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL	Inhibition of human HDAC6 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2019) 162: 321-333 [PMID:30448419]
ChEMBL	Inhibition of recombinant human HDAC6 using RHKKAc fluorogenic peptide substrate	B	7.82	pIC50	15	nM	IC50	J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL	Inhibition of human HDAC6 using fluorogenic HDAC substrate	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL	Inhibition of human HDAC6 using p53 fluorogenic peptide (379 to 382 residues) RHKKAc as substrate by fluorescence-based assay	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2021) 47: 128204-128204 [PMID:34139324]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of recombiant human HDAC6 using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence microplate reader assay	B	7.82	pIC50	15	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of HDAC6 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay	B	7.82	pIC50	15	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of recombinant human HDAC6 using RHKKAc peptide as substrate	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2022) 229: 114090-114090 [PMID:34992037]
ChEMBL	Inhibition of human recombinant HDAC6 using RHKKAc as substrate	B	7.82	pIC50	15	nM	IC50	J Med Chem (2022) 65: 3080-3097 [PMID:35148101]
ChEMBL	Inhibition of human HDAC6	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2021) 226: 113874-113874 [PMID:34619465]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2022) 76: 129015-129015 [PMID:36208870]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL	Inhibition of human HDAC6	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2021) 225: 113815-113815 [PMID:34479038]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2018) 157: 447-461 [PMID:30103193]
ChEMBL	Inhibition of human recombinant HDAC6 using RHKKAc peptide as substrate incubated for 5 to mins prior to substrate addition measured after 2 hrs	B	7.82	pIC50	15	nM	IC50	J Med Chem (2012) 55: 639-651 [PMID:22165909]
ChEMBL	Inhibition of HDAC6 (unknown origin) using fluorogenic peptide RHKKAc-AMC as substrate by fluorescence-based assay	B	7.84	pIC50	14.3	nM	IC50	Bioorg Med Chem Lett (2023) 81: 129148-129148 [PMID:36690041]
GtoPdb	-	-	7.85	pIC50	14	nM	IC50	US8748451. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay	B	7.85	pIC50	14	nM	IC50	Medchemcomm (2019) 10: 1109-1115 [PMID:31391882]
ChEMBL	Inhibition of recombinant human KDAC6 using acetylated p53 (379 to 382 residues) as substrate by fluorescence assay	B	7.85	pIC50	14	nM	IC50	J Med Chem (2016) 59: 1613-1633 [PMID:26681404]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	7.85	pIC50	14	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay	B	7.85	pIC50	14	nM	IC50	J Med Chem (2020) 63: 10339-10351 [PMID:32803970]
ChEMBL	Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis	B	7.85	pIC50	14	nM	IC50	J Med Chem (2022) 65: 15457-15472 [PMID:36351184]
ChEMBL	Inhibition of human HDAC6 using fluorogenic-(RHKKAc) as substrate by fluorescence assay	B	7.86	pIC50	13.7	nM	IC50	Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504]
ChEMBL	Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using RHKK(Ac) as substrate after 90 mins by fluorimetric method	B	7.86	pIC50	13.7	nM	IC50	Eur J Med Chem (2017) 127: 115-127 [PMID:28038324]
ChEMBL	Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay	B	7.89	pIC50	13	nM	IC50	Eur J Med Chem (2018) 150: 506-524 [PMID:29549837]
ChEMBL	Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay	B	7.95	pIC50	11.14	nM	IC50	Bioorg Med Chem (2019) 27: 3408-3420 [PMID:31235266]
ChEMBL	Inhibition of human recombinant HDAC6 using fluorogenic substrate measured after 30 mins	B	7.95	pIC50	11.14	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of human recombinant HDAC6 using fluorogenic substrate measured after 30 mins	B	7.95	pIC50	11.1	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate by fluorescence assay	B	7.96	pIC50	11	nM	IC50	J Med Chem (2016) 59: 8233-8262 [PMID:27541357]
ChEMBL	Inhibition of HDAC6 (unknown origin) measured by fluorescence based assay	B	8.03	pIC50	9.4	nM	IC50	Bioorg Med Chem (2022) 73: 117028-117028 [PMID:36182802]
ChEMBL	Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate	B	8.13	pIC50	7.44	nM	IC50	HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
ChEMBL	Inhibition of HDAC6 (unknown origin)	B	8.36	pIC50	4.4	nM	IC50	J Med Chem (2020) 63: 10246-10262 [PMID:32815366]
ChEMBL	Inhibition of human full length recombinant HDAC6 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	8.4	pIC50	4	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of human HDAC6	B	8.4	pIC50	4	nM	IC50	Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	8.4	pIC50	4	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHKKAc as substrate in presence of ATP	B	8.46	pIC50	3.5	nM	IC50	J Med Chem (2017) 60: 8336-8357 [PMID:28953386]
ChEMBL	Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay	B	8.46	pIC50	3.5	nM	IC50	J Med Chem (2016) 59: 8233-8262 [PMID:27541357]
ChEMBL	Inhibition of human HDAC6 using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate	B	8.46	pIC50	3.5	nM	IC50	Bioorg Med Chem Lett (2018) 28: 2636-2640 [PMID:29945795]
ChEMBL	Inhibition of HDAC6 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	8.7	pIC50	2	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
ChEMBL	Inhibition of human HDAC6 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay	B	8.72	pIC50	1.9	nM	IC50	J Med Chem (2021) 64: 1116-1126 [PMID:33356256]
ChEMBL	Inhibition of HDAC6 in human RPMI-8226 cells assessed as increase in tubulin acetylation incubated for 6 hrs by Western blot analysis	B	5.96	pEC50	1090	nM	EC50	J Med Chem (2021) 64: 4810-4840 [PMID:33830764]
histone deacetylase 6/Histone deacetylase 6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2878] [GtoPdb: 2618] [UniProtKB: Q9Z2V5]
ChEMBL	Inhibition of HDAC6 in mouse N2A cells	B	8.36	pIC50	4.4	nM	IC50	ACS Med Chem Lett (2020) 11: 706-712 [PMID:32435374]
ChEMBL	Inhibition of HDAC6 in mouse N2A cells assessed as increase in alpha tubulin acetylation	B	6.84	pEC50	145	nM	EC50	ACS Med Chem Lett (2020) 11: 706-712 [PMID:32435374]
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
ChEMBL	Inhibition of HDAC7 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of human recombinant HDAC7 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of human recombinant HDAC7 using acetyl-Lys(trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC7 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of HDAC7 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC7 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC7 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.01	pIC50	9700	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of recombinant HDAC7 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC7 (unknown origin) measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of HDAC7 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	6.42	pIC50	379	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
ChEMBL	Inhibition of human full length recombinant HDAC7 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	6.51	pIC50	306	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
Histone deacetylase 8 in Schistosoma mansoni (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797017] [UniProtKB: A5H660]
ChEMBL	Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay	B	5.83	pIC50	1479.11	nM	IC50	Bioorg Med Chem (2017) 25: 2105-2132 [PMID:28259528]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL	Inhibition of C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in 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	4.91	pKi	12300	nM	Ki	Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL	Inhibition of human HDAC8	B	7.02	pKi	96.2	nM	Ki	Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL	Inhibition of recombinant HDAC8 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	Inhibition of HDAC8 (unknown origin) measured by fluorescence based assay	B	5.3	pIC50	>5000	nM	IC50	Bioorg Med Chem (2022) 73: 117028-117028 [PMID:36182802]
ChEMBL	Inhibition of recombinant human KDAC8 using diacetylated p53 (379 to 382 residues) as substrate by fluorescence assay	B	5.63	pIC50	2340	nM	IC50	J Med Chem (2016) 59: 1613-1633 [PMID:26681404]
ChEMBL	Inhibition of HDAC8 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay	B	5.72	pIC50	1899	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of human recombinant HDAC8 using fluorogenic substrate measured after 30 mins	B	5.87	pIC50	1350	nM	IC50	Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.9	pIC50	1270	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of HDAC8 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	6.07	pIC50	854	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HADC8 (unknown origin)	B	6.07	pIC50	854	nM	IC50	J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL	Inhibition of human recombinant HDAC8 protein using RHKAcKAc from p53 as substrate	B	6.07	pIC50	854	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Inhibition of HDAC8 (unknown origin)	B	6.07	pIC50	854	nM	IC50	Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL	Inhibition of HDAC8 (unknown origin)	B	6.07	pIC50	854	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate	B	6.07	pIC50	854	nM	IC50	J Med Chem (2013) 56: 6775-6791 [PMID:23905680]
ChEMBL	Inhibition of human recombinant HDAC8 using RHKAcKAc as substrate	B	6.07	pIC50	854	nM	IC50	J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL	Inhibition of full length C-terminal 6x-His tagged human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay	B	6.07	pIC50	854	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL	Inhibition of HDAC8 (unknown origin)	B	6.07	pIC50	854	nM	IC50	Bioorg Med Chem Lett (2014) 24: 4826-4830 [PMID:25240614]
ChEMBL	Inhibition of N-terminal GST-tagged full length human HDAC8 expressed in baculovirus system using FTS as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based analysis	B	6.07	pIC50	854	nM	IC50	Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875]
ChEMBL	Inhibition of HDAC8 (unknown origin)	B	6.07	pIC50	854	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC8 (unknown origin) measured after 30 mins by fluorescence microplate reader assay	B	6.07	pIC50	854	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of HDAC8 (unknown origin) using RHKAcKAc fluorogenic-diacyl peptide as substrate by fluorescence assay	B	6.07	pIC50	854	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of recombinant human HDAC8 using RHKAcKAc peptide as substrate	B	6.07	pIC50	854	nM	IC50	Eur J Med Chem (2022) 229: 114090-114090 [PMID:34992037]
ChEMBL	Inhibition of human recombinant HDAC8 using RHKAcKAc as substrate	B	6.07	pIC50	850	nM	IC50	J Med Chem (2022) 65: 3080-3097 [PMID:35148101]
ChEMBL	Inhibition of HDAC8 (unknown origin)	B	6.07	pIC50	850	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	6.09	pIC50	814	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
GtoPdb	-	-	6.09	pIC50	814	nM	IC50	US8748451. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of human HDAC8	B	6.12	pIC50	760	nM	IC50	Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL	Inhibition of human full length recombinant HDAC8 using p53 (379 to 382 residues) (RHK(Ac)K(Ac)AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	6.12	pIC50	755	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of human recombinant HDAC8 expressed in Escherichia coli using Fluor de Lys substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay	B	6.16	pIC50	695	nM	IC50	ACS Med Chem Lett (2020) 11: 2268-2276 [PMID:33214839]
ChEMBL	Inhibition of recombinant human HDAC8 expressed in baculovirus expression system using fluorogenic Arg-His-Lys(Ac)-Lys(Ac) as substrate incubated for 90 mins by fluorescence assay	B	6.16	pIC50	695	nM	IC50	J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL	Inhibition of HDAC8 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	6.17	pIC50	681	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
ChEMBL	Inhibition of full length C-terminal his-tagged human recombinant HDAC8 expressed in Sf9 insect cells	B	6.48	pIC50	333	nM	IC50	J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL	Inhibition of human recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 mins by fluorimetric method	B	6.48	pIC50	330	nM	IC50	Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL	Inhibition of full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA	B	6.48	pIC50	330	nM	IC50	ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
ChEMBL	Inhibition of HDAC9 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of human recombinant HDAC9 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2013) 56: 6297-6313 [PMID:23627282]
ChEMBL	Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at room temperature in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	4.52	pIC50	>30000	nM	IC50	US-8748451-B2. HDAC inhibitors and therapeutic methods of using same (2014)
ChEMBL	Inhibition of HDAC9 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL	Inhibition of HDAC9 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL	Inhibition of HDAC9 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL	Inhibition of HDAC9 (unknown origin)	B	4.52	pIC50	>30000	nM	IC50	Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL	Inhibition of recombinant human HDAC9 measured after 30 mins by fluorescence microplate reader assay	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL	Inhibition of recombinant HDAC9 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (2022) 65: 12140-12162 [PMID:36073117]
ChEMBL	HDAC Activity Assay: HDAC assay is performed using fluorescently-labeled acetylated substrate, which comprises an acetylated lysine side chain. After incubation with HDAC, deacetylation of the substrate sensitizes the substrate such that, in a second step, treatment with the detection enzyme produces a fluorophore. HDACs 1 and 6 were expressed as full length fusion proteins. Purified proteins were incubated with 50 μM fluorescently-labeled acetylated peptide substrate and test compound for 2 hours at RT in HDAC assay buffer containing 50 mM Tris-HCl (pH 8.0), 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1% DMSO, and 1% BSA. Reactions were terminated by the addition of the Developer after 2 hours, and the development of fluorescence signal, which was relative to the amount of deacetylated peptide, was monitored by time-course measurement of EnVision (PerkinElmer). The HDAC activity was estimated from the slope of time-course measurement of the fluorescence intensity.	B	5.37	pIC50	4310	nM	IC50	US-9249087-B2. HDAC inhibitors and therapeutic methods using the same (2016)
ChEMBL	Inhibition of human full length recombinant HDAC9 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method	B	6.13	pIC50	739	nM	IC50	J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL	Inhibition of HDAC9 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay	B	6.21	pIC50	621	nM	IC50	J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
Polyamine deacetylase HDAC10 in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4802002] [UniProtKB: F1QCV2]
ChEMBL	Inhibition of zebra fish HDAC10 using Ac-spermidine-AMC as substrate incubated for 25 mins and measured by fluorescence assay	B	6.66	pIC50	220	nM	IC50	Eur J Med Chem (2022) 234: 114272-114272 [PMID:35306288]

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]