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ChEMBL ligand: CHEMBL27759 (Entinostat, MS-27-275, MS-275, MS-275-27, SNDX-275) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
ChEMBL | Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
ChEMBL | Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
coagulation factor III, tissue factor/Coagulation factor III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4081] [GtoPdb: 3192] [UniProtKB: P13726] | ||||||||
ChEMBL | Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay | B | 5 | pIC50 | 10000 | nM | IC50 | J. Biol. Chem. (2007) 282: 28408-28418 [PMID:17675290] |
ChEMBL | Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay | B | 5.22 | pIC50 | 6000 | nM | IC50 | J. Biol. Chem. (2007) 282: 28408-28418 [PMID:17675290] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG by automated patch clamp assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2011) 21: 4909-4912 [PMID:21742496] |
ChEMBL | Inhibition of human ERG by automated Q-patch assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J. Med. Chem. (2011) 54: 4752-4772 [PMID:21650221] |
Histone deacetylase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7] | ||||||||
ChEMBL | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells | B | 6.03 | pIC50 | 940 | nM | IC50 | J. Med. Chem. (2009) 52: 2185-2187 [PMID:19317450] |
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
ChEMBL | Inhibition of human HDAC1 | B | 7.66 | pKi | 22 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
GtoPdb | - | - | 7.66 | pKi | 22 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | HDAC enzyme inhibitionAssay: HDAC enzyme inhibition assays were performed using purified HDACs 1-10 essentially as described in Beckers et al., 2007, Int. J. Cancer., 121:1138-48 and Perez-Balado et al., 2007, J. Med. Chem., 50:2497-2505. Inhibition assays using nuclear extract were performed essentially as described in Herman et al., 2006, Nat. Chem. Biol., 2:551-558. Briefly, the purified HDACs or nuclear extract were incubated with an acetylated substrate in the absence of the compound to be assayed and with increasing concentrations of the compound. The rate of substrate deacetylation was measured under each condition, and half-maximal inhibitory concentration with regard to each HDAC was determined by standard means. | B | 5.49 | pIC50 | 3200 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibitory activity on partially purified recombinant human Histone deacetylase 1 (HDAC-1) | B | 5.7 | pIC50 | 2000 | nM | IC50 | J. Med. Chem. (2003) 46: 820-830 [PMID:12593661] |
ChEMBL | Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method | B | 5.83 | pIC50 | 1480 | nM | IC50 | J. Med. Chem. (2016) 59: 1613-1633 [PMID:26681404] |
ChEMBL | Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay | B | 5.97 | pIC50 | 1070 | nM | IC50 | Eur J Med Chem (2018) 144: 612-625 [PMID:29289885] |
ChEMBL | Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1). | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2004) 14: 283-287 [PMID:14684344] |
ChEMBL | Inhibition of human HDAC1 | B | 6 | pIC50 | 1000 | nM | IC50 | J. Med. Chem. (2008) 51: 1505-1529 [PMID:18247554] |
ChEMBL | Inhibition of HDAC1 | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg. Med. Chem. Lett. (2011) 21: 110-116 [PMID:21145737] |
ChEMBL | Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay | B | 6.26 | pIC50 | 544 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of human recombinant HDAC1 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | B | 6.26 | pIC50 | 544 | nM | IC50 | Eur J Med Chem (2020) 196: 112291-112291 [PMID:32325365] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay | B | 6.26 | pIC50 | 544 | nM | IC50 | Eur J Med Chem (2021) 215: 113169-113169 [PMID:33588178] |
ChEMBL | Inhibition of recombinant human full-length C-terminal FLAG-His tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | B | 6.27 | pIC50 | 540 | nM | IC50 | Eur J Med Chem (2020) 192: 112158-112158 [PMID:32171161] |
ChEMBL | Inhibition of human recombinant HDAC1 | B | 6.27 | pIC50 | 540 | nM | IC50 | J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625] |
ChEMBL | Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate incubated for 90 mins by fluorescence assay | B | 6.28 | pIC50 | 519 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
ChEMBL | Inhibition of HADC1 (unknown origin) | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
ChEMBL | Inhibition of HDAC1 using Fluor de Lys as substrate by fluorescence analysis | B | 6.3 | pIC50 | 500 | nM | IC50 | Eur. J. Med. Chem. (2012) 53: 390-397 [PMID:22541394] |
ChEMBL | Inhibition of HDAC1 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg. Med. Chem. (2010) 18: 3925-3933 [PMID:20452226] |
ChEMBL | Inhibition of purified recombinant HDAC1 | B | 6.31 | pIC50 | 485 | nM | IC50 | Bioorg. Med. Chem. Lett. (2011) 21: 4909-4912 [PMID:21742496] |
ChEMBL | Inhibition of HDAC1 | B | 6.32 | pIC50 | 480 | nM | IC50 | Bioorg. Med. Chem. Lett. (2012) 22: 1926-1930 [PMID:22321215] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using deacetylase fluorogenic substrate pretreated for 5 mins followed by substrate addition after 30 mins by fluorescence assay | B | 6.39 | pIC50 | 410 | nM | IC50 | Eur J Med Chem (2017) 132: 42-62 [PMID:28340413] |
ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur. J. Med. Chem. (2015) 96: 1-13 [PMID:25874326] |
ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | B | 6.41 | pIC50 | 390 | nM | IC50 | Bioorg. Med. Chem. (2015) 23: 3457-3471 [PMID:25953722] |
ChEMBL | Inhibition of HDAC1 | B | 6.43 | pIC50 | 368 | nM | IC50 | Eur. J. Med. Chem. (2012) 53: 390-397 [PMID:22541394] |
ChEMBL | Inhibition of human recombinant HDAC1 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
ChEMBL | Inhibition of human recombinant His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS SIRT1 as substrate incubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2019) 173: 185-202 [PMID:31003060] |
ChEMBL | Inhibition of human recombinant HDAC1 using p53 residues 379-382 (RHKKAc) as substrate | B | 6.51 | pIC50 | 310 | nM | IC50 | Bioorg. Med. Chem. (2013) 21: 5339-5354 [PMID:23820574] |
ChEMBL | Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 2530-2535 [PMID:18381238] |
ChEMBL | Inhibition of HDAC1 by in vitro deacetylation assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Nat. Chem. Biol. (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay | B | 6.52 | pIC50 | <300 | nM | IC50 | J. Med. Chem. (2013) 56: 4816-4820 [PMID:23672185] |
ChEMBL | Inhibition of HDAC1 (unknown origin) preincubated for 5 mins followed by fluorogenic substrate addition measured after 30 mins by microplate reader analysis | B | 6.56 | pIC50 | 273 | nM | IC50 | Eur. J. Med. Chem. (2015) 100: 270-276 [PMID:26140961] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis | B | 6.57 | pIC50 | 271 | nM | IC50 | Bioorg Med Chem (2017) 25: 4123-4132 [PMID:28629630] |
ChEMBL | Inhibition of human recombinant C-terminal His/FLAG-tagged HDAC1 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 6.72 | pIC50 | 190 | nM | IC50 | Eur J Med Chem (2019) 177: 457-466 [PMID:31181405] |
ChEMBL | Inhibition of HDAC1 | B | 6.74 | pIC50 | 180 | nM | IC50 | J. Med. Chem. (2008) 51: 1505-1529 [PMID:18247554] |
ChEMBL | Inhibition of HDAC1 (unknown origin) by fluorescence based assay | B | 6.75 | pIC50 | 178.3 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay | B | 6.79 | pIC50 | 163 | nM | IC50 | Bioorg Med Chem (2017) 25: 2981-2994 [PMID:28511906] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2018) 61: 5304-5322 [PMID:29787262] |
ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) using of Fluor-de-Lys substrate incubated for 10 mins by fluorimetric assay | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 2931-2935 [PMID:27142751] |
ChEMBL | Inhibition of HDAC1 | B | 6.9 | pIC50 | 125 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 726-731 [PMID:18060775] |
ChEMBL | Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells | B | 6.92 | pIC50 | 120 | nM | IC50 | J. Med. Chem. (2009) 52: 3453-3456 [PMID:19441846] |
ChEMBL | Inhibition of HDAC1 by fluorogenic enzyme assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg. Med. Chem. Lett. (2009) 19: 3651-3656 [PMID:19457659] |
ChEMBL | Inhibition of HDAC1 | B | 6.92 | pIC50 | 120 | nM | IC50 | J. Med. Chem. (2008) 51: 2350-2353 [PMID:18370373] |
ChEMBL | Inhibition of HDAC1 in HEK293 cells | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563] |
ChEMBL | Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay | B | 6.93 | pIC50 | 118 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of HDAC1 (mean IC50) | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg. Med. Chem. Lett. (2006) 16: 5948-5952 [PMID:16987657] |
ChEMBL | Inhibition of HDAC1 in human HeLa cell lysate using KI-104 as substrate after 40 mins by fluorescence analysis | B | 7 | pIC50 | <100 | nM | IC50 | Bioorg. Med. Chem. (2012) 20: 4430-4436 [PMID:22705022] |
ChEMBL | Inhibition of recombinant human full length HDAC1 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 7 | pIC50 | 99 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | B | 7.27 | pIC50 | 53.89 | nM | IC50 | J Med Chem (2020) 63: 5501-5525 [PMID:32321249] |
ChEMBL | Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg. Med. Chem. Lett. (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of HDAC1 | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442] |
ChEMBL | Inhibition of recombinant human HDAC1 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
ChEMBL | Inhibition of human HDAC1 assessed as histone H4 acetylation in cell based assay | B | 6 | pEC50 | 1000 | nM | EC50 | J. Med. Chem. (2008) 51: 1505-1529 [PMID:18247554] |
GtoPdb | - | - | 6.74 | pEC50 | 181 | nM | EC50 | Biochem J (2008) 409: 581-9 [PMID:17868033] |
ChEMBL | Inhibition of recombinant human N-terminal GST/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 3 hrs by fluorescence assay | B | 6.74 | pEC50 | 180 | nM | EC50 | MedChemComm (2016) 7: 2184-2190 |
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
ChEMBL | Inhibition of HDAC10 | B | 4.3 | pIC50 | 50100 | nM | IC50 | Eur. J. Med. Chem. (2012) 53: 390-397 [PMID:22541394] |
ChEMBL | Inhibition of HDAC10 by in vitro deacetylation assay | B | 4.95 | pIC50 | 11100 | nM | IC50 | Nat. Chem. Biol. (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of HDAC10 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay | B | 5.5 | pIC50 | 3150 | nM | IC50 | Eur J Med Chem (2021) 215: 113169-113169 [PMID:33588178] |
ChEMBL | Inhibition of human recombinant HDAC10 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | B | 5.5 | pIC50 | 3150 | nM | IC50 | Eur J Med Chem (2020) 196: 112291-112291 [PMID:32325365] |
ChEMBL | Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
ChEMBL | Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM SAHA by fluorometric method | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2943-2945 [PMID:28501514] |
ChEMBL | Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2943-2945 [PMID:28501514] |
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
ChEMBL | Inhibition of human HDAC2 | B | 7.19 | pKi | 65 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
GtoPdb | - | - | 7.19 | pKi | 65 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HDAC2 | B | 5.82 | pIC50 | 1510 | nM | IC50 | Bioorg. Med. Chem. Lett. (2012) 22: 1926-1930 [PMID:22321215] |
ChEMBL | Inhibition of HDAC2 | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2011) 21: 110-116 [PMID:21145737] |
ChEMBL | Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay | B | 6.13 | pIC50 | 740 | nM | IC50 | Eur J Med Chem (2018) 144: 612-625 [PMID:29289885] |
ChEMBL | Inhibition of recombinant human full length HDAC2 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 6.13 | pIC50 | 740 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
ChEMBL | HDAC enzyme inhibitionAssay: HDAC enzyme inhibition assays were performed using purified HDACs 1-10 essentially as described in Beckers et al., 2007, Int. J. Cancer., 121:1138-48 and Perez-Balado et al., 2007, J. Med. Chem., 50:2497-2505. Inhibition assays using nuclear extract were performed essentially as described in Herman et al., 2006, Nat. Chem. Biol., 2:551-558. Briefly, the purified HDACs or nuclear extract were incubated with an acetylated substrate in the absence of the compound to be assayed and with increasing concentrations of the compound. The rate of substrate deacetylation was measured under each condition, and half-maximal inhibitory concentration with regard to each HDAC was determined by standard means. | B | 6.14 | pIC50 | 720 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of human recombinant His-tagged HDAC2 (1 to 582 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS Green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method | B | 6.17 | pIC50 | 670 | nM | IC50 | Eur J Med Chem (2019) 173: 185-202 [PMID:31003060] |
ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | B | 6.19 | pIC50 | 650 | nM | IC50 | Bioorg. Med. Chem. (2015) 23: 3457-3471 [PMID:25953722] |
ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | B | 6.19 | pIC50 | 650 | nM | IC50 | Eur. J. Med. Chem. (2015) 96: 1-13 [PMID:25874326] |
ChEMBL | Inhibition of human HDAC2 using RHKKAc as substrate by fluorescence assay | B | 6.21 | pIC50 | 613 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay | B | 6.21 | pIC50 | 613 | nM | IC50 | Eur J Med Chem (2021) 215: 113169-113169 [PMID:33588178] |
ChEMBL | Inhibition of human recombinant HDAC2 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis | B | 6.21 | pIC50 | 613 | nM | IC50 | Eur J Med Chem (2020) 196: 112291-112291 [PMID:32325365] |
ChEMBL | Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected insect cells using RHKKAc-AMC as substrate measured after 60 mins by fluorescence assay | B | 6.21 | pIC50 | 610 | nM | IC50 | Eur J Med Chem (2020) 192: 112158-112158 [PMID:32171161] |
ChEMBL | Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 90 mins by fluorescence assay | B | 6.3 | pIC50 | 505 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis | B | 6.3 | pIC50 | 505 | nM | IC50 | Bioorg Med Chem (2017) 25: 4123-4132 [PMID:28629630] |
ChEMBL | Inhibition of human recombinant HDAC2 | B | 6.3 | pIC50 | 500 | nM | IC50 | J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625] |
ChEMBL | Inhibition of HDAC2 by in vitro deacetylation assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Nat. Chem. Biol. (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of human recombinant HDAC2 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6.32 | pIC50 | 480 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
ChEMBL | Inhibition of human recombinant C-terminal FLAG-tagged HDAC2 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 6.39 | pIC50 | 410 | nM | IC50 | Eur J Med Chem (2019) 177: 457-466 [PMID:31181405] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2018) 61: 5304-5322 [PMID:29787262] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay | B | 6.4 | pIC50 | 396 | nM | IC50 | Bioorg Med Chem (2017) 25: 2981-2994 [PMID:28511906] |
ChEMBL | Inhibition of HDAC2 | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 726-731 [PMID:18060775] |
ChEMBL | Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay | B | 6.52 | pIC50 | <300 | nM | IC50 | J. Med. Chem. (2013) 56: 4816-4820 [PMID:23672185] |
ChEMBL | Inhibition of HDAC2 | B | 6.6 | pIC50 | 250 | nM | IC50 | J. Med. Chem. (2008) 51: 2350-2353 [PMID:18370373] |
ChEMBL | Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells | B | 6.6 | pIC50 | 250 | nM | IC50 | J. Med. Chem. (2009) 52: 3453-3456 [PMID:19441846] |
ChEMBL | Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay | B | 6.61 | pIC50 | 247 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | B | 6.97 | pIC50 | 108.2 | nM | IC50 | J Med Chem (2020) 63: 5501-5525 [PMID:32321249] |
ChEMBL | Inhibition of HDAC2 in human HeLa cell lysate using KI-104 as substrate after 40 mins by fluorescence analysis | B | 7 | pIC50 | <100 | nM | IC50 | Bioorg. Med. Chem. (2012) 20: 4430-4436 [PMID:22705022] |
ChEMBL | Inhibition of HDAC2 | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442] |
ChEMBL | Inhibition of recombinant human HDAC2 using pan-HDAC substrate incubated for 3 hrs by fluorescence method | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
ChEMBL | Inhibition of recombinant human N-terminal GST/flag-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells after 3 hrs by fluorescence assay | B | 5.92 | pEC50 | 1200 | nM | EC50 | MedChemComm (2016) 7: 2184-2190 |
GtoPdb | - | - | 5.94 | pEC50 | 1155 | nM | EC50 | Biochem J (2008) 409: 581-9 [PMID:17868033] |
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
GtoPdb | - | - | 6.44 | pKi | 360 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC3 | B | 6.44 | pKi | 360 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HADC3 (unknown origin) | B | 5.77 | pIC50 | 1700 | nM | IC50 |