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ChEMBL ligand: CHEMBL2018302 (Tubastatin A) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
ChEMBL | Inhibition of human 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 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) | B | 4.79 | pIC50 | 16400 | nM | IC50 | Eur J Med Chem (2018) 157: 447-461 [PMID:30103193] |
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) 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 HADC1 (unknown origin) | B | 4.79 | pIC50 | 16400 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
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 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 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 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 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 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 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 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 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 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 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 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 |