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ChEMBL ligand: CHEMBL99 (A-300-I, ANTIBIOTIC A-300, GNF-Pf-1011, Trichostatin, Trichostatin(s)) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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coagulation factor III, tissue factor/Coagulation factor III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4081] [GtoPdb: 3192] [UniProtKB: P13726] | ||||||||
ChEMBL | Inhibition of LPS-induced tissue factor activity in human PBMC preincubated for 4 hrs assessed after 5 hrs of LPS challenge by one stage clotting assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Biol Chem (2007) 282: 28408-28418 [PMID:17675290] |
ChEMBL | Inhibition of IL-1-beta-induced tissue factor activity in human PBMC preincubated for 4 hrs assessed after 5 hrs of IL1-beta challenge by one stage clotting assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Biol Chem (2007) 282: 28408-28418 [PMID:17675290] |
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 | 7.52 | pIC50 | 30 | 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Biol Chem (2007) 282: 28408-28418 [PMID:17675290] |
ChEMBL | Inhibition of IL-1-beta-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of IL1-beta challenge by one stage clotting assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Biol Chem (2007) 282: 28408-28418 [PMID:17675290] |
ChEMBL | Inhibition of HOSCN-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of HOSCN challenge by one stage clotting assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Biol Chem (2007) 282: 28408-28418 [PMID:17675290] |
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 | 9.22 | pIC50 | 0.6 | 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 | Binding affinity to human HDAC1 assessed as dissociation constant | B | 7.82 | pKd | 15 | nM | Kd | J Med Chem (2023) 66: 11672-11700 [PMID:37651268] |
ChEMBL | Inhibition of human recombinant HDAC1 by Michaelis-Menten equation analysis | B | 9.06 | pKi | 0.87 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
ChEMBL | Inhibition of recombinant HDAC1 | B | 9.64 | pKi | 0.23 | nM | Ki | Eur J Med Chem (2010) 45: 2095-2116 [PMID:20223566] |
ChEMBL | Inhibition of human HDAC1 | B | 9.7 | pKi | 0.2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC1 | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 9.7 | pKi | 0.2 | nM | Ki | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
GtoPdb | - | - | 9.7 | pKi | 0.2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibitory activity on partially purified recombinant human Histone deacetylase 1 (HDAC-1) | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2003) 46: 820-830 [PMID:12593661] |
ChEMBL | Inhibition of HDAC1 by fluorescence assay | B | 5.41 | pIC50 | 3900 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1218-1221 [PMID:21256006] |
ChEMBL | Inhibition of HDAC1 expressed in 293T cells | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem (2008) 16: 437-445 [PMID:17900911] |
ChEMBL | Inhibition of human full-length recombinant HDAC1 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 7.21 | pIC50 | 62 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
ChEMBL | Inhibition of human HDAC1 expressed in 293T cells | B | 7.44 | pIC50 | 36.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2982-2984 [PMID:18397826] |
ChEMBL | Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2019) 162: 321-333 [PMID:30448419] |
ChEMBL | Inhibition of HDAC1 | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1558-1561 [PMID:17257837] |
ChEMBL | Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay | B | 7.6 | pIC50 | 24.9 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of human HDAC1 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem (2014) 22: 3850-3855 [PMID:24997578] |
ChEMBL | Inhibition of HDAC1 by fluorimetric assay | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
ChEMBL | Inhibition of recombinant human HDAC1 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay | B | 7.64 | pIC50 | 23 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of HDAC1 | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 997-999 [PMID:20045316] |
ChEMBL | Inhibition of HDAC1 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5222-5228 [PMID:27717544] |
ChEMBL | Inhibition of human recombinant HDAC1 expressed in NIH3T3 cells | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2007) 50: 5425-5438 [PMID:17929798] |
ChEMBL | Inhibition of HDAC1 | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2006) 49: 4809-4812 [PMID:16884291] |
ChEMBL | Inhibition of human histone deacetylase 1 prepared from 293T cells | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5343-5346 [PMID:15454224] |
ChEMBL | Inhibitory concentration against histone deacetylase 1 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4427-4431 [PMID:16137884] |
ChEMBL | Inhibition of recombinant human HDAC1 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins in presence of DTT by fluorescence assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2018) 26: 1920-1928 [PMID:29519604] |
ChEMBL | Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis | B | 7.73 | pIC50 | 18.8 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925] |
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 | 7.75 | pIC50 | 17.9 | nM | IC50 | Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504] |
ChEMBL | Inhibition of HDAC1 by fluorescent activity assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5735-5738 [PMID:21875796] |
ChEMBL | Inhibition of human HDAC1 | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4895-4900 [PMID:17588744] |
ChEMBL | Inhibition of recombinant full length human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorimetric assay | B | 7.8 | pIC50 | 15.8 | nM | IC50 | Eur J Med Chem (2020) 187: 111915-111915 [PMID:31838329] |
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 | 7.8 | pIC50 | 15.7 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925] |
ChEMBL | Inhibition of human KDAC1 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic peptide as the substrate containing residues 379-382 of p53 pre-incubated for 15 mins followed by substrate addition incubated for 30 mins by multimode plate reader | B | 7.85 | pIC50 | 14.14 | nM | IC50 | Bioorg Med Chem (2023) 93: 117444-117444 [PMID:37611334] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control | B | 7.9 | pIC50 | 12.5 | nM | IC50 | Eur J Med Chem (2019) 168: 110-122 [PMID:30802729] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | B | 7.91 | pIC50 | 12.44 | nM | IC50 | Eur J Med Chem (2018) 143: 2005-2014 [PMID:29150335] |
ChEMBL | Inhibition of human HDAC1 by ELISA | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2018) 148: 73-85 [PMID:29454918] |
ChEMBL | Inhibition of human HDAC1 using RHKKAc peptide as substrate | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2018) 61: 7087-7102 [PMID:30028616] |
ChEMBL | Inhibition of human HDAC1 after 30 mins by fluorescence assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Nat Prod (2012) 75: 285-289 [PMID:22276693] |
ChEMBL | Inhibition of HDAC1 by fluorometric assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6200-6204 [PMID:22932316] |
ChEMBL | Inhibition of human HDAC1 by fluorescence assay | B | 7.96 | pIC50 | 10.9 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
ChEMBL | Inhibition of recombinant human HDAC1 using RHK-K(Ac) as substrate by homogeneous fluorescence release assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2019) 161: 277-291 [PMID:30366254] |
ChEMBL | Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of recombinant human full-length C-terminal Flag-His6-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry | B | 8 | pIC50 | <10 | nM | IC50 | Bioorg Med Chem (2022) 56: 116599-116599 [PMID:35041998] |
ChEMBL | Inhibition of HDAC1 | B | 8 | pIC50 | 9.9 | nM | IC50 | Bioorg Med Chem (2010) 18: 3925-3933 [PMID:20452226] |
ChEMBL | Inhibition of full length recombinant C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence plate reader assay | B | 8.02 | pIC50 | 9.59 | nM | IC50 | Bioorg Med Chem (2021) 50: 116454-116454 [PMID:34634618] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 8.04 | pIC50 | 9.2 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
ChEMBL | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of recombinant human HDAC1 by fluorimetry | B | 8.07 | pIC50 | 8.5 | nM | IC50 | J Med Chem (2016) 59: 655-670 [PMID:26705137] |
ChEMBL | Inhibition of HDAC1 (unknown origin) using Fluor de lys as substrate by fluorescence based analysis | B | 8.08 | pIC50 | 8.41 | nM | IC50 | Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013] |
ChEMBL | Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 8.09 | pIC50 | 8.22 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay | B | 8.11 | pIC50 | 7.7 | nM | IC50 | ACS Med Chem Lett (2017) 8: 510-515 [PMID:28523102] |
ChEMBL | Inhibition of HDAC1 (unknown origin) after 15 mins by fluorescence assay | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5497-5501 [PMID:25455492] |
ChEMBL | Inhibition of human HDAC1 by fluorimetric assay | B | 8.15 | pIC50 | 7.12 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate | B | 8.15 | pIC50 | 7.12 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC1 | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of recombinant human C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorimetry analysis | B | 8.16 | pIC50 | 6.96 | nM | IC50 | Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238] |
ChEMBL | Inhibition of human HDAC1 using RHKK(Ac) as substrate | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Eur J Med Chem (2018) 150: 667-677 [PMID:29567459] |
ChEMBL | Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect cells using [RHKK(Ac)] fluorogenic substrate | B | 8.16 | pIC50 | 6.89 | nM | IC50 | Eur J Med Chem (2021) 217: 113338-113338 [PMID:33744690] |
ChEMBL | Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay | B | 8.16 | pIC50 | 6.89 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
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 | 8.17 | pIC50 | 6.7 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 8.18 | pIC50 | 6.57 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of human HDAC1 | B | 8.2 | pIC50 | 6.3 | nM | IC50 | Eur J Med Chem (2023) 248: 115054-115054 [PMID:36630883] |
ChEMBL | Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | B | 8.21 | pIC50 | 6.22 | nM | IC50 | Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059] |
ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2022) 65: 3080-3097 [PMID:35148101] |
ChEMBL | Inhibition of HADC1 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
ChEMBL | Inhibition of HDAC1 in human NIH3T3 cells by radiometric histone deacetylation assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
ChEMBL | Inhibition of human HDAC1 | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127023-127023 [PMID:32067866] |
ChEMBL | Inhibition of HDAC1 | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1926-1930 [PMID:22321215] |
ChEMBL | Inhibition of human recombinant HDAC1 using fluorogenic substrate incubated for 30 mins by fluorescence based assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | ACS Med Chem Lett (2020) 11: 713-719 [PMID:32435375] |
ChEMBL | Inhibition against partially purified human histone deacetylase 1 (HDAC-1) | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2002) 45: 2877-2885 [PMID:12061890] |
ChEMBL | In vitro inhibition of partially purified recombinant human Histone deacetylase 1 | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2847-2850 [PMID:11597413] |
ChEMBL | Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2013) 56: 6775-6791 [PMID:23905680] |
ChEMBL | Inhibitory concentration against recombinant human Histone deacetylase 1 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
ChEMBL | Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
ChEMBL | Inhibition of human recombinant HDAC1 using p53 residues 379-382 (RHKKAc) as substrate | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem (2013) 21: 5339-5354 [PMID:23820574] |
ChEMBL | Inhibition of HDAC1 (unknown origin) after 30 mins by fluorometric analysis | B | 8.37 | pIC50 | 4.3 | nM | IC50 | Bioorg Med Chem (2013) 21: 4201-4209 [PMID:23719282] |
ChEMBL | Inhibition of HDAC1 | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
ChEMBL | Inhibition of HDAC1 after 17 hrs | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
ChEMBL | Inhibition of human recombinant HDAC1 using fluorogenic substrate measured after 30 mins | B | 8.45 | pIC50 | 3.51 | nM | IC50 | Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952] |
ChEMBL | Inhibition of human recombinant HDAC1 after 30 mins by fluorimetric assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | J Med Chem (2009) 52: 7836-7846 [PMID:19705846] |
ChEMBL | Inhibition of human HDAC1 using rhodamine as substrate after 1 hrs by fluorescence assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2011) 19: 4626-4634 [PMID:21723733] |
ChEMBL | Inhibition of HDAC1 by in vitro deacetylation assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of human HDAC1 in presence of dithiothreitol by HDAC fluorescent assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2012) 52: 111-122 [PMID:22465091] |
ChEMBL | Inhibition of HDAC1 (unknown origin) by colorimetric method | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522] |
ChEMBL | Inhibition of recombinant full-length human HDAC1 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 8.67 | pIC50 | 2.14 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of HDAC1 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem (2015) 23: 6785-6793 [PMID:26481659] |
ChEMBL | Inhibition of human HDAC1 expressed in baculovirus expression system in Sf9 cells using RHKKAc (379 to 382 residues) fluorogenic peptide as substrate and measured after 2 hrs by fluorescence based analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2023) 66: 10528-10557 [PMID:37463500] |
ChEMBL | Inhibition of human HDAC1 expressed in 293T cells | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem (2007) 15: 7830-7839 [PMID:17881232] |
ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Eur J Med Chem (2023) 254: 115327-115327 [PMID:37098307] |
ChEMBL | Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
ChEMBL | Inhibition of recombinant full-length human HDAC1 using FITC-H3K27(Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
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 | 9.17 | pIC50 | 0.68 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of HDAC1 | B | 9.82 | pIC50 | 0.15 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
ChEMBL | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells. | B | 5.22 | pEC50 | 6000 | nM | EC50 | J Med Chem (2003) 46: 4826-4829 [PMID:14584932] |
ChEMBL | Concentration of compound required for acetylation of histone-4 in human T24 cancer cells | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2847-2850 [PMID:11597413] |
histone deacetylase 1/Histone deacetylase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4001] [GtoPdb: 2658] [UniProtKB: O09106] | ||||||||
ChEMBL | Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi) | B | 8.97 | pKi | 1.07 | nM | Ki | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
ChEMBL | Inhibitory activity against histone deacetylases (HDAC1) prepared from mouse melanoma B16/BL6 cells | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2427-2431 [PMID:15109626] |
ChEMBL | In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
ChEMBL | Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
ChEMBL | Inhibition of mouse HDAC1 | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
ChEMBL | Inhibition of mouse HDAC1 | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2006) 49: 6046-6056 [PMID:17004718] |
ChEMBL | Inhibition of mouse liver HDAC1 | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
ChEMBL | Inhibition of HDAC10 | B | 8.15 | pKi | 7 | nM | Ki | Eur J Med Chem (2010) 45: 2095-2116 [PMID:20223566] |
ChEMBL | Inhibition of human HDAC10 using RHKKAc as substrate by fluorescence assay | B | 7.15 | pIC50 | 71 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of HDAC10 (unknown origin) using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of recombinant human HDAC10 using fluorogenic substrate by fluorescence assay | B | 7.42 | pIC50 | 38.1 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
ChEMBL | Inhibition of recombinant full-length human HDAC10 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 7.42 | pIC50 | 37.9 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of human recombinant HDAC10 using RHK-K(Ac)-AMC as substrate | B | 7.46 | pIC50 | 34.81 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of human HDAC10 using RHKKAc peptide as substrate | B | 7.46 | pIC50 | 34.5 | nM | IC50 | J Med Chem (2018) 61: 7087-7102 [PMID:30028616] |
ChEMBL | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2018) 143: 2005-2014 [PMID:29150335] |
ChEMBL | Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
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 | 7.64 | pIC50 | 22.8 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.7 | pIC50 | 20.1 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC10 by fluorimetric assay | B | 7.7 | pIC50 | 20.1 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC10 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of human recombinant HDAC10 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 7.95 | pIC50 | 11.3 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2013) 56: 6775-6791 [PMID:23905680] |
ChEMBL | Inhibition of HDAC10 by in vitro deacetylation assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of HDAC10 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
ChEMBL | Inhibition of HDAC10 after 17 hrs | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
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 | 8.79 | pIC50 | 1.61 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of recombinant full-length human HDAC10 using FITC-H3K27(Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
ChEMBL | Inhibition of human full length HDAC11 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 4.96 | pIC50 | 10900 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
ChEMBL | Inhibition of recombinant full-length human HDAC11 using FAM-RHKK (trifluor-Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 5.04 | pIC50 | 9080 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of HDAC11 (unknown origin) using fluorogenic peptide 382 RHKK(Ac)AM as substrate and measured by fluorescence assay | B | 5.17 | pIC50 | 6830 | nM | IC50 | Eur J Med Chem (2022) 228: 113971-113971 [PMID:34772529] |
ChEMBL | Inhibition of human recombinant N-terminal Streptavidin2-tagged HDAC11 (1 to 347 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay | B | 5.46 | pIC50 | 3470 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of recombinant human HDAC11 using fluorogenic substrate by fluorescence assay | B | 5.68 | pIC50 | 2110 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
ChEMBL | Inhibition of human HDAC11 by fluorescence assay | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
ChEMBL | Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate | B | 7.76 | pIC50 | 17.3 | nM | IC50 | J Med Chem (2013) 56: 6775-6791 [PMID:23905680] |
ChEMBL | Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.82 | pIC50 | 15.2 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC11 by fluorimetric assay | B | 7.82 | pIC50 | 15.15 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC11 | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of recombinant C-terminal His-tagged human HDAC11 (1 to 347 residues) expressed in Baculovirus infected insect cells using RHKK-Ac as substrate by fluorimetric assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2019) 162: 321-333 [PMID:30448419] |
ChEMBL | Inhibition of human recombinant HDAC11 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 7.86 | pIC50 | 13.9 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of human recombinant N-terminal His-tagged HDAC11 (1 to 347 residues) expressed in insect cells/baculovirus expression system using RHK-K(Ac)-AMC as substrate by fluorescence assay | B | 7.94 | pIC50 | 11.37 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of recombinant full-length human HDAC11 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 7.97 | pIC50 | 10.6 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
ChEMBL | Binding affinity to C-terminal His-tagged human HDAC2 (2 to 488 residues) in transfected in baculovirus infected Sf9 cells assessed as dissociation constant | B | 7.92 | pKd | 12 | nM | Kd | J Med Chem (2023) 66: 11672-11700 [PMID:37651268] |
ChEMBL | Inhibition of human recombinant HDAC2 by Michaelis-Menten equation analysis | B | 8.97 | pKi | 1.06 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
ChEMBL | Inhibition of recombinant HDAC2 | B | 9.12 | pKi | 0.76 | nM | Ki | Eur J Med Chem (2010) 45: 2095-2116 [PMID:20223566] |
ChEMBL | Inhibition of human HDAC2 | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
ChEMBL | Inhibition of human HDAC2 | B | 9.19 | pKi | 0.65 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
GtoPdb | - | - | 9.19 | pKi | 0.65 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system using fluorogenic peptide RHKK(Ac) as substrate by fluorescence assay | B | 4.59 | pIC50 | 25800 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
ChEMBL | Inhibition of HDAC2 by fluorescence assay | B | 5.12 | pIC50 | 7600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1218-1221 [PMID:21256006] |
ChEMBL | Inhibition of human full-length recombinant HDAC2 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 7.02 | pIC50 | 96 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
ChEMBL | Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 7.17 | pIC50 | 68 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of recombinant human HDAC2 by fluorimetry | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2016) 59: 655-670 [PMID:26705137] |
ChEMBL | Inhibition of human HDAC2 using RHKKAc peptide as substrate | B | 7.33 | pIC50 | 46.6 | nM | IC50 | J Med Chem (2018) 61: 7087-7102 [PMID:30028616] |
ChEMBL | Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry assay | B | 7.4 | pIC50 | 39.5 | nM | IC50 | Eur J Med Chem (2020) 187: 111915-111915 [PMID:31838329] |
ChEMBL | Inhibition of human HDAC2 using RHKKAc as substrate by fluorescence assay | B | 7.41 | pIC50 | 39.1 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibitory concentration against histone deacetylase 2 | B | 7.41 | pIC50 | 39 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4427-4431 [PMID:16137884] |
ChEMBL | Inhibition of human HDAC2 by fluorescence assay | B | 7.49 | pIC50 | 32.1 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
ChEMBL | Inhibition of full length recombinant C-terminal GST-fusion-tagged human HDAC2 expressed in insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence plate reader assay | B | 7.54 | pIC50 | 28.6 | nM | IC50 | Bioorg Med Chem (2021) 50: 116454-116454 [PMID:34634618] |
ChEMBL | Inhibition of HDAC2 (unknown origin) after 15 mins by fluorescence assay | B | 7.55 | pIC50 | 28.2 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5497-5501 [PMID:25455492] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of HDAC2 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5222-5228 [PMID:27717544] |
ChEMBL | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | B | 7.63 | pIC50 | 23.6 | nM | IC50 | Eur J Med Chem (2018) 143: 2005-2014 [PMID:29150335] |
ChEMBL | Inhibition of human HDAC2 by ELISA | B | 7.64 | pIC50 | 23 | nM | IC50 | Eur J Med Chem (2018) 148: 73-85 [PMID:29454918] |
ChEMBL | Inhibition of human HDAC2 | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of human HDAC2 by fluorimetric assay | B | 7.64 | pIC50 | 22.95 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC2 | B | 7.67 | pIC50 | 21.5 | nM | IC50 | Eur J Med Chem (2023) 248: 115054-115054 [PMID:36630883] |
ChEMBL | Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay | B | 7.69 | pIC50 | 20.5 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
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 | 7.73 | pIC50 | 18.7 | nM | IC50 | Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504] |
ChEMBL | Inhibition of HDAC2 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1926-1930 [PMID:22321215] |
ChEMBL | Inhibition of recombinant full-length human HDAC2 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
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 | 7.83 | pIC50 | 14.8 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of HDAC2 (unknown origin) after 30 mins by fluorometric analysis | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem (2013) 21: 4201-4209 [PMID:23719282] |
ChEMBL | Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
ChEMBL | Inhibition of HDAC2 | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
ChEMBL | Inhibition of HDAC2 after 17 hrs | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of full length human recombinant C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.98 | pIC50 | 10.51 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of human recombinant histone deacetylase 2 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 688-692 [PMID:19111466] |
ChEMBL | Inhibition of HDAC2 by in vitro deacetylation assay | B | 8 | pIC50 | 10 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of HDAC2 (unknown origin) by colorimetric method | B | 8.22 | pIC50 | 6.08 | nM | IC50 | Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522] |
ChEMBL | Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2013) 56: 6775-6791 [PMID:23905680] |
ChEMBL | Inhibition of human HDAC2 using rhodamine as substrate after 1 hrs by fluorescence assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2011) 19: 4626-4634 [PMID:21723733] |
ChEMBL | Inhibition of recombinant full-length human HDAC2 using FITC-H3K27(Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
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 | 8.56 | pIC50 | 2.74 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of HDAC2 in human HeLa cell nuclear extracts in presence of dithiothreitol by HDAC fluorescent assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Eur J Med Chem (2012) 52: 111-122 [PMID:22465091] |
ChEMBL | Inhibition of HDAC2 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
ChEMBL | Inhibition of recombinant HDAC3 | B | 9.24 | pKi | 0.58 | nM | Ki | Eur J Med Chem (2010) 45: 2095-2116 [PMID:20223566] |
GtoPdb | - | - | 9.3 | pKi | 0.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC3 | B | 9.3 | pKi | 0.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC3 | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
ChEMBL | Inhibition of HDAC3 by fluorescence assay | B | 5.28 | pIC50 | 5200 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1218-1221 [PMID:21256006] |
ChEMBL | Inhibition of human HDAC3 using RHKKAc peptide as substrate | B | 7.28 | pIC50 | 52.5 | nM | IC50 | J Med Chem (2018) 61: 7087-7102 [PMID:30028616] |
ChEMBL | Inhibition of human recombinant HDAC3 using [RHKK(Ac)] fluorogenic substrate | B | 7.43 | pIC50 | 37.5 | nM | IC50 | Eur J Med Chem (2021) 217: 113338-113338 [PMID:33744690] |
ChEMBL | Inhibition of recombinant human HDAC3 using fluorogenic substrate by fluorescence assay | B | 7.43 | pIC50 | 37.5 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
ChEMBL | Inhibition of HDAC3 (unknown origin) by ELISA | B | 7.51 | pIC50 | 31 | nM | IC50 | Eur J Med Chem (2018) 148: 73-85 [PMID:29454918] |
ChEMBL | Inhibition of human full-length recombinant HDAC3 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
ChEMBL | Inhibition of human HDAC3 using RHKKAc as substrate by fluorescence assay | B | 7.58 | pIC50 | 26.2 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of HDAC3 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of human KDAC3 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
ChEMBL | Inhibition of recombinant full length human C-terminal His-tagged HDAC3 (1 to 428 residues) expressed in baculovirus infected insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of HDAC3 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5222-5228 [PMID:27717544] |
ChEMBL | Inhibition of human recombinant HDAC3 after 30 mins by fluorimetric assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2009) 52: 7836-7846 [PMID:19705846] |
ChEMBL | Inhibition of recombinant human HDAC3 using RHK-K(Ac)-AMC as substrate by fluorescence based assay | B | 7.98 | pIC50 | 10.4 | nM | IC50 | Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238] |
ChEMBL | Inhibition of human HDAC3 using RHKK(Ac) as substrate | B | 7.98 | pIC50 | 10.4 | nM | IC50 | Eur J Med Chem (2018) 150: 667-677 [PMID:29567459] |
ChEMBL | Inhibition of human HDAC3 by fluorimetric assay | B | 7.99 | pIC50 | 10.32 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC3 complexed with NCOR2 using fluorogenic tetrapeptide RHKKAc as susbtrate | B | 7.99 | pIC50 | 10.3 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC3 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
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 | 8.02 | pIC50 | 9.6 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of HDAC3 by in vitro deacetylation assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of HDAC3 (unknown origin) by colorimetric method | B | 8.4 | pIC50 | 4.01 | nM | IC50 | Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522] |
ChEMBL | Inhibition of recombinant full-length human HDAC3 using FAM-RHKK(Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of HDAC3 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
ChEMBL | Inhibition of HDAC3 after 17 hrs | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of HDAC3 | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
ChEMBL | Inhibition of HDAC3 | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
histone deacetylase 3/Histone deacetylase 3/NCoR1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038484] [GtoPdb: 2617] [UniProtKB: O15379, O75376] | ||||||||
ChEMBL | Inhibition of recombinant human HDAC3/NCOR1 complex expressed in insect cells assessed as residual enzyme activity preincubated for 1 hr followed by addition of fluorogenic Ac-LGK-ac-AMC as substrate for 30 mins by fluorescence analysis | B | 9.27 | pKi | 0.54 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
GtoPdb | - | - | 9.3 | pKi | 0.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
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 full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged recombinant human NCOR2 (395 to 489 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter | B | 9.08 | pKi | 0.84 | nM | Ki | J Med Chem (2018) 61: 3454-3477 [PMID:29589441] |
GtoPdb | - | - | 9.3 | pKi | 0.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay | B | 9.59 | pKi | 0.26 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminaL GST-tagged human recombinant NCOR2 (395 to 489 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry analysis | B | 7.6 | pIC50 | 25.3 | nM | IC50 | Eur J Med Chem (2020) 187: 111915-111915 [PMID:31838329] |
ChEMBL | Inhibition of recombinant full-length human HDAC3/NCOR2 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 7.8 | pIC50 | 15.7 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2019) 162: 321-333 [PMID:30448419] |
ChEMBL | Inhibition of full length human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/human recombinant N-terminal GST-tagged NCOR2 expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.96 | pIC50 | 11.07 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry | B | 8 | pIC50 | <10 | nM | IC50 | Bioorg Med Chem (2022) 56: 116599-116599 [PMID:35041998] |
ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
ChEMBL | Inhibition of human recombinant HDAC4 by Michaelis-Menten equation analysis | B | 4.84 | pKi | 14547 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
GtoPdb | - | - | 5.85 | pKi | 1400 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC4 | B | 5.85 | pKi | 1400 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 5.85 | pKi | 1400 | nM | Ki | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of N-terminal GST-tagged recombinant human HDAC4 assessed as hydrolase activity using fluorogenic Ac-AC-LGK-tfa-AMC-AMC as substrate measured after 60 mins by fluorescence analysis | B | 6.01 | pKi | 980 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
ChEMBL | Inhibition of human HDAC4 | B | 6.4 | pKi | 400 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | B | 5.04 | pIC50 | 9100 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of human HDAC4 by fluorescence assay | B | 5.07 | pIC50 | 8439 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
ChEMBL | Inhibition of HDAC4 by fluorescence assay | B | 5.11 | pIC50 | 7690 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1218-1221 [PMID:21256006] |
ChEMBL | Inhibition of recombinant full-length human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | B | 5.18 | pIC50 | 6600 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of recombinant human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by homogeneous fluorescence release assay | B | 5.42 | pIC50 | 3800 | nM | IC50 | Eur J Med Chem (2019) 161: 277-291 [PMID:30366254] |
ChEMBL | Inhibition of recombinant full-length human HDAC4 using FAM-RHKK (trifluor-Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 5.92 | pIC50 | 1210 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of HDAC4 expressed in 293T cells | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2008) 16: 437-445 [PMID:17900911] |
ChEMBL | Inhibition of human recombinant HDAC4 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 6.91 | pIC50 | 122 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of human recombinant HDAC4 using p53 residues 379-382 (RHKKAc) as substrate | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem (2013) 21: 5339-5354 [PMID:23820574] |
ChEMBL | Inhibition of human HDAC4 expressed in 293T cells | B | 7.2 | pIC50 | 62.9 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2982-2984 [PMID:18397826] |
ChEMBL | Inhibition of HDAC4 | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 997-999 [PMID:20045316] |
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 | 7.46 | pIC50 | 34.8 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of HDAC4 by fluorimetric assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
ChEMBL | Inhibition of HDAC4 | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2006) 49: 4809-4812 [PMID:16884291] |
ChEMBL | Inhibition of human recombinant HDAC4 expressed in 293 cells | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2007) 50: 5425-5438 [PMID:17929798] |
ChEMBL | Inhibition of human HDAC4 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem (2014) 22: 3850-3855 [PMID:24997578] |
ChEMBL | Inhibition of recombinant human HDAC4 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of human HDAC4 | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4895-4900 [PMID:17588744] |
ChEMBL | Inhibition of human histone deacetylase 4 prepared from 293T cells | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5343-5346 [PMID:15454224] |
ChEMBL | Inhibition of HDAC4 in human HeLa cells incubated for 1 hr by mass spectrometry method | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem (2021) 52: 116510-116510 [PMID:34826681] |
ChEMBL | Inhibition of human HDAC4 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.92 | pIC50 | 12.1 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC4 by fluorimetric assay | B | 7.92 | pIC50 | 12.07 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC4 | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of HDAC4 by in vitro deacetylation assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of human HDAC4 expressed in 293T cells | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem (2007) 15: 7830-7839 [PMID:17881232] |
ChEMBL | Inhibition of acetylation of histone-4 in human T-24 cancer cells | F | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
ChEMBL | Inhibition of acetylation of histone-4 in human T-24 cancer cells | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
ChEMBL | Inhibition of human recombinant HDAC5 by Michaelis-Menten equation analysis | B | 5.39 | pKi | 4120 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
ChEMBL | Inhibition of human HDAC5 | B | 6.59 | pKi | 260 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC5 | B | 6.59 | pKi | 260 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
GtoPdb | - | - | 6.59 | pKi | 260 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC5 by fluorescence assay | B | 5.21 | pIC50 | 6155 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
ChEMBL | Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of recombinant full-length human HDAC5 using FAM-RHKK (trifluor-Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of recombinant full-length human HDAC5 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | B | 5.96 | pIC50 | 1090 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay | B | 6.11 | pIC50 | 776 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of human HDAC5 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.78 | pIC50 | 16.5 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC5 by fluorimetric assay | B | 7.78 | pIC50 | 16.48 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC5 | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
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 | 7.9 | pIC50 | 12.5 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of human recombinant HDAC5 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 8.09 | pIC50 | 8.08 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of HDAC5 by in vitro deacetylation assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
histone deacetylase 5/Histone deacetylase 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2768] [GtoPdb: 2660] [UniProtKB: Q9Z2V6] | ||||||||
ChEMBL | Inhibitory activity against histone deacetylase (HDAC4) prepared from mouse melanoma B16/BL6 cells | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2427-2431 [PMID:15109626] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Inhibition of human recombinant HDAC6 by Michaelis-Menten equation analysis | B | 8.52 | pKi | 3.02 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC6 | B | 9 | pKi | 1 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC6 | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
ChEMBL | Inhibition of recombinant HDAC6 | B | 9 | pKi | 0.99 | nM | Ki | Eur J Med Chem (2010) 45: 2095-2116 [PMID:20223566] |
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 | 9.24 | pKi | 0.58 | nM | Ki | J Med Chem (2018) 61: 3454-3477 [PMID:29589441] |
ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay | B | 9.89 | pKi | 0.13 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
ChEMBL | Inhibition of human HDAC6 using fluorogenic-(RHKKAc) as substrate by fluorescence assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504] |
ChEMBL | Inhibition of human HDAC6 using RHKK(Ac) as substrate | B | 5.59 | pIC50 | 2600 | nM | IC50 | Eur J Med Chem (2018) 150: 667-677 [PMID:29567459] |
ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 5.92 | pIC50 | 1210 | nM | IC50 | Eur J Med Chem (2018) 150: 506-524 [PMID:29549837] |
ChEMBL | Inhibition of HDAC6 by fluorescence assay | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1218-1221 [PMID:21256006] |
ChEMBL | Inhibition of HDAC6 expressed in 293T cells | B | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem (2008) 16: 437-445 [PMID:17900911] |
ChEMBL | Inhibitory concentration against histone deacetylase 6 | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4427-4431 [PMID:16137884] |
ChEMBL | Inhibition of human HDAC6 expressed in 293T cells | B | 7.08 | pIC50 | 83.3 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2982-2984 [PMID:18397826] |
ChEMBL | Inhibition of HDAC6 | B | 7.09 | pIC50 | 81 | nM | IC50 | J Med Chem (2006) 49: 4809-4812 [PMID:16884291] |
ChEMBL | Inhibition of HDAC6 by fluorimetric assay | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
ChEMBL | Inhibition of HDAC6 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem (2015) 23: 6785-6793 [PMID:26481659] |
ChEMBL | Inhibition of HDAC6 | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 997-999 [PMID:20045316] |
ChEMBL | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
ChEMBL | Inhibition of human HDAC6 | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4895-4900 [PMID:17588744] |
ChEMBL | Inhibition of human HDAC6 using rhodamine as substrate after 1 hrs by fluorescence assay | B | 7.29 | pIC50 | 51 | nM | IC50 | Bioorg Med Chem (2011) 19: 4626-4634 [PMID:21723733] |
ChEMBL | Inhibition of human KDAC6 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
ChEMBL | Inhibition of human recombinant histone deacetylase 6 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 688-692 [PMID:19111466] |
ChEMBL | Inhibition of human histone deacetylase 6 prepared from 293T cells | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5343-5346 [PMID:15454224] |
ChEMBL | Inhibition of HDAC6 (unknown origin) measured by fluorometry assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2022) 240: 114573-114573 [PMID:35797900] |
ChEMBL | Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay | B | 7.77 | pIC50 | 16.8 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay | B | 7.77 | pIC50 | 16.8 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
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 | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925] |
ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins using fluorogenic substrate by fluorimetric assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2018) 61: 6574-6591 [PMID:30004697] |
ChEMBL | Inhibition of human full-length recombinant HDAC6 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
ChEMBL | Inhibition of HDAC6 | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.95 | pIC50 | 11.1 | nM | IC50 | Eur J Med Chem (2021) 226: 113874-113874 [PMID:34619465] |
ChEMBL | Inhibition of human HDAC6 using fluorogenic HDAC substrate | B | 8.03 | pIC50 | 9.3 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2022) 65: 3080-3097 [PMID:35148101] |
ChEMBL | Inhibition of recombinant human HDAC6 by fluorimetry | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2016) 59: 655-670 [PMID:26705137] |
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 | 8.05 | pIC50 | 8.92 | 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 | 8.05 | pIC50 | 8.92 | nM | IC50 | Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952] |
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 8.06 | pIC50 | 8.73 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
ChEMBL | Inhibition of HADC6 (unknown origin) | B | 8.07 | pIC50 | 8.6 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
ChEMBL | Inhibition of N-terminal GST-tagged recombinant human HDAC6 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay | B | 8.07 | pIC50 | 8.5 | nM | IC50 | J Med Chem (2018) 61: 10299-10309 [PMID:30365892] |
ChEMBL | Inhibition of HDAC6 (unknown origin) after 15 mins by fluorescence assay | B | 8.09 | pIC50 | 8.2 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5497-5501 [PMID:25455492] |
ChEMBL | Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4955-4959 [PMID:27650925] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorimetry analysis | B | 8.21 | pIC50 | 6.12 | nM | IC50 | Eur J Med Chem (2020) 187: 111915-111915 [PMID:31838329] |
ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins by fluorimetric assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2009) 52: 7836-7846 [PMID:19705846] |
ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in Baculovirus infected insect cells using RHKK-Ac as substrate by fluorimetric assay | B | 8.23 | pIC50 | 5.9 | nM | IC50 | Eur J Med Chem (2019) 162: 321-333 [PMID:30448419] |
ChEMBL | Inhibition of HDAC6 (unknown origin) using Fluor de lys as substrate by fluorescence based analysis | B | 8.25 | pIC50 | 5.56 | nM | IC50 | Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013] |
ChEMBL | Inhibition of human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHKKAc as substrate | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2020) 63: 295-308 [PMID:31793776] |
ChEMBL | Inhibition of human HDAC6 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127023-127023 [PMID:32067866] |
ChEMBL | Inhibition of HDAC6 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5222-5228 [PMID:27717544] |
ChEMBL | Inhibition of recombinant human HDAC6 using fluorogenic substrate by fluorescence assay | B | 8.34 | pIC50 | 4.53 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
ChEMBL | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using [RHKK(Ac)] fluorogenic substrate | B | 8.34 | pIC50 | 4.53 | nM | IC50 | Eur J Med Chem (2021) 217: 113338-113338 [PMID:33744690] |
ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorescence assay | B | 8.45 | pIC50 | 3.55 | nM | IC50 | J Med Chem (2018) 61: 905-917 [PMID:29304284] |
ChEMBL | Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay | B | 8.45 | pIC50 | 3.55 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of human HDAC6 using RHKKAc peptide as substrate | B | 8.46 | pIC50 | 3.49 | nM | IC50 | J Med Chem (2018) 61: 7087-7102 [PMID:30028616] |
ChEMBL | Inhibition of human recombinant HDAC6 using RHKKAcAMC as substrate by fluorescence assay | B | 8.5 | pIC50 | 3.13 | nM | IC50 | Eur J Med Chem (2018) 152: 329-357 [PMID:29738953] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1125 residues) expressed in baculovirus infected insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of recombinant human HDAC6 using RHK-K(Ac)-AMC as substrate by fluorescence based assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238] |
ChEMBL | Inhibition of human recombinant HDAC6 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 8.64 | pIC50 | 2.31 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | ACS Med Chem Lett (2017) 8: 510-515 [PMID:28523102] |
ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Eur J Med Chem (2023) 254: 115327-115327 [PMID:37098307] |
ChEMBL | Inhibition of full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHK-K(Ac)-AMC as substrate measured after 90 mins by fluorescence plate reader assay | B | 8.68 | pIC50 | 2.11 | nM | IC50 | Bioorg Med Chem (2021) 50: 116454-116454 [PMID:34634618] |
ChEMBL | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | B | 8.68 | pIC50 | 2.09 | nM | IC50 | Eur J Med Chem (2018) 143: 2005-2014 [PMID:29150335] |
ChEMBL | Inhibition of human HDAC6 | B | 8.69 | pIC50 | 2.05 | nM | IC50 | Eur J Med Chem (2023) 248: 115054-115054 [PMID:36630883] |
ChEMBL | Inhibition of recombinant human HDAC6 using RHK-K(Ac) as substrate by homogeneous fluorescence release assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2019) 161: 277-291 [PMID:30366254] |
ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
ChEMBL | Inhibition of recombinant full-length human HDAC6 using FAM-RHKK(Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of human HDAC6 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | B | 8.71 | pIC50 | 1.94 | nM | IC50 | Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059] |
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 incubated for 90 mins by fluorescence assay | B | 8.77 | pIC50 | 1.72 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of human recombinant HDAC6 using p53 residues 379-382 (RHKKAc) as substrate | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem (2013) 21: 5339-5354 [PMID:23820574] |
ChEMBL | Inhibition of recombinant full-length human HDAC6 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 8.81 | pIC50 | 1.56 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of recombinant human full-length N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected Sf9 insect cells using RHKK(Ac)AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2021) 35: 116085-116085 [PMID:33668008] |
ChEMBL | Inhibition of human HDAC6 by fluorescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
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 | 8.85 | pIC50 | 1.4 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
ChEMBL | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of HDAC6 (unknown origin) by colorimetric method | B | 8.97 | pIC50 | 1.07 | nM | IC50 | Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522] |
ChEMBL | Inhibition of HDAC6 | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
ChEMBL | Inhibition of human HDAC6 expressed in baculovirus expression system in Sf9 cells using RHKKAc (379 to 382 residues) fluorogenic peptide as substrate and measured after 2 hrs by fluorescence based analysis | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2023) 66: 10528-10557 [PMID:37463500] |
ChEMBL | Inhibition of HDAC6 after 17 hrs | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
ChEMBL | Inhibition of HDAC6 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
ChEMBL | Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2013) 56: 6775-6791 [PMID:23905680] |
ChEMBL | Inhibition of HDAC6 by in vitro deacetylation assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of human HDAC6 by fluorimetric assay | B | 9.38 | pIC50 | 0.42 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate | B | 9.38 | pIC50 | 0.42 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC6 | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA | B | 8.28 | pEC50 | 5.2 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919] |
histone deacetylase 6/Histone deacetylase 6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2878] [GtoPdb: 2618] [UniProtKB: Q9Z2V5] | ||||||||
ChEMBL | Inhibition of mouse recombinant HDAC6 expressed in 293 cells | B | 7.09 | pIC50 | 81 | nM | IC50 | J Med Chem (2007) 50: 5425-5438 [PMID:17929798] |
ChEMBL | Inhibition of mouse HDAC6 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem (2014) 22: 3850-3855 [PMID:24997578] |
ChEMBL | Inhibition of recombinant mouse HDAC6 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay | B | 7.19 | pIC50 | 65 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibitory activity against histone deacetylase 6 prepared from mouse melanoma B16/BL6 cells | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2427-2431 [PMID:15109626] |
ChEMBL | Inhibition of recombinant mouse HDAC6 expressed in HEK293T cells co-expressing mouse HDA2 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins in presence of DTT by fluorescence assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem (2018) 26: 1920-1928 [PMID:29519604] |
ChEMBL | Inhibition of mouse HDAC6 expressed in 293T cells | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem (2007) 15: 7830-7839 [PMID:17881232] |
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
ChEMBL | Inhibition of N-terminal 6His-tagged recombinant human HDAC7 assessed as hydrolase activity using fluorogenic AC-LGK-tfa-AMC as substrate measured after 60 mins by fluorescence analysis | B | 6.52 | pKi | 300 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
ChEMBL | Inhibition of human HDAC7 | B | 6.71 | pKi | 195 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC7 | B | 6.71 | pKi | 195 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
GtoPdb | - | - | 6.71 | pKi | 195 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of recombinant full-length human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | B | 5.38 | pIC50 | 4170 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of HDAC7 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay | B | 6.32 | pIC50 | 482 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
ChEMBL | Inhibition of recombinant full-length human HDAC7 using FAM-RHKK (trifluor-Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of HDAC7 by in vitro deacetylation assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
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 | 6.71 | pIC50 | 197 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of human recombinant HDAC7 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 6.86 | pIC50 | 139 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of human recombinant HDAC7 using ArgHisLysLys(Ac) as substrate by fluorescence based analysis | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2023) 66: 7698-7729 [PMID:37276138] |
ChEMBL | Inhibition of human HDAC7 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.65 | pIC50 | 22.5 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC7 by fluorimetric assay | B | 7.65 | pIC50 | 22.46 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC7 | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
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 | 5.44 | pIC50 | 3620 | 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 recombinant human HDAC8 expressed in Escherichia coli assessed as hydrolase activity using fluorogenic AC-LGK-tfa-AMC as substrate measured after 60 mins by fluorescence analysis | B | 6.7 | pKi | 200 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
ChEMBL | Inhibition of recombinant HDAC8 | B | 6.89 | pKi | 130 | nM | Ki | Eur J Med Chem (2010) 45: 2095-2116 [PMID:20223566] |
ChEMBL | Inhibition of human recombinant HDAC8 by Michaelis-Menten equation analysis | B | 7.16 | pKi | 69.65 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
ChEMBL | Activity of human HDAC8 | B | 7.35 | pKi | 45 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC8 | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
ChEMBL | Inhibition of C-terminal His-tagged human recombinant full-length HDAC8 expressed in baculovirus expression system assessed as reduction in 7-amino-4-methylcoumarin by fluorescence based assay | B | 7.35 | pKi | 45 | nM | Ki | Eur J Med Chem (2017) 141: 188-196 [PMID:29031066] |
GtoPdb | - | - | 8.35 | pKi | 4.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HDAC8 by fluorescence assay | B | 4.14 | pIC50 | 73100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1218-1221 [PMID:21256006] |
ChEMBL | Inhibition of human KDAC8 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | B | 5.34 | pIC50 | 4550 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
ChEMBL | Inhibition of HDAC8 | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
ChEMBL | Inhibition of HDAC8 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
ChEMBL | Inhibition of HDAC8 (unknown origin) after 30 mins by fluorometric analysis | B | 5.87 | pIC50 | 1360 | nM | IC50 | Bioorg Med Chem (2013) 21: 4201-4209 [PMID:23719282] |
ChEMBL | Inhibition of HDAC8 (unknown origin) using Fluor de lys as substrate by fluorescence based analysis | B | 5.94 | pIC50 | 1160 | nM | IC50 | Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013] |
ChEMBL | Inhibition of human HDAC8 using RHKAcKAc as substrate | B | 5.99 | pIC50 | 1020 | nM | IC50 | Eur J Med Chem (2018) 150: 667-677 [PMID:29567459] |
ChEMBL | Inhibition of recombinant C-terminal His-tagged human HDAC8 (1 to 377 residues) expressed in Baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay | B | 6 | pIC50 | 990 | nM | IC50 | Eur J Med Chem (2019) 162: 321-333 [PMID:30448419] |
ChEMBL | Inhibition of N terminal hexahistidine-tagged human HDAC8 expressed in Sf9 cells after 1 hr by fluorescence assay | B | 6.02 | pIC50 | 960 | nM | IC50 | Bioorg Med Chem (2011) 19: 4626-4634 [PMID:21723733] |
ChEMBL | Inhibition of recombinant C-terminal His-tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | B | 6.03 | pIC50 | 944 | nM | IC50 | Eur J Med Chem (2020) 187: 111915-111915 [PMID:31838329] |
ChEMBL | Inhibition of human HDAC8 | B | 6.03 | pIC50 | 923 | nM | IC50 | Eur J Med Chem (2023) 248: 115054-115054 [PMID:36630883] |
ChEMBL | Inhibition of recombinant human HDAC8 using RHK-K(Ac)-AMC as substrate by fluorescence based assay | B | 6.09 | pIC50 | 820 | nM | IC50 | Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238] |
ChEMBL | Inhibition of HDAC8 (unknown origin) measured by fluorometry assay | B | 6.1 | pIC50 | 790 | nM | IC50 | Eur J Med Chem (2022) 240: 114573-114573 [PMID:35797900] |
ChEMBL | Inhibition of human recombinant histone deacetylase 8 | B | 6.11 | pIC50 | 770 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 688-692 [PMID:19111466] |
ChEMBL | Inhibition of recombinant C-terminal His-fusion tagged/N-terminal Strep2 tagged human HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-K(Ac)-AMC as substrate measured after 60 mins by fluorescence plate reader assay | B | 6.16 | pIC50 | 697 | nM | IC50 | Bioorg Med Chem (2021) 50: 116454-116454 [PMID:34634618] |
ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | B | 6.19 | pIC50 | 650 | nM | IC50 | Bioorg Med Chem (2020) 28: 115250-115250 [PMID:31924504] |
ChEMBL | Inhibition of C-terminal His-tagged recombinant human HDAC8 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay | B | 6.22 | pIC50 | 609 | nM | IC50 | J Med Chem (2018) 61: 10299-10309 [PMID:30365892] |
ChEMBL | Inhibition of human HDAC8 expressed in baculovirus expression system in Sf9 cells using RHKAcKAc (379 to 382 residues) fluorogenic peptide as substrate and measured after 2 hrs by fluorescence based analysis | B | 6.23 | pIC50 | 589 | nM | IC50 | J Med Chem (2023) 66: 10528-10557 [PMID:37463500] |
ChEMBL | Inhibition of human HDAC8 using RHKAcKAc peptide as substrate | B | 6.25 | pIC50 | 566 | nM | IC50 | J Med Chem (2018) 61: 7087-7102 [PMID:30028616] |
ChEMBL | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 6.31 | pIC50 | 490 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
ChEMBL | Inhibition of human HDAC8 using RHKAcKAc as substrate by fluorescence assay | B | 6.37 | pIC50 | 427 | nM | IC50 | Eur J Med Chem (2019) 162: 612-630 [PMID:30476825] |
ChEMBL | Inhibition of human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 6.38 | pIC50 | 420 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
ChEMBL | Inhibition of human recombinant HDAC8 using fluor de Lys as substrate preincubated for 5 mins followed by substrate addition measured after 25 mins by microplate reader analysis | B | 6.41 | pIC50 | 390 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6621-6627 [PMID:23010266] |
ChEMBL | Inhibition of recombinant C-terminal His-fusion tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in insect cells using fluorogenic peptide p53 residues 379-382 (RHK(Ac)K(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | B | 6.43 | pIC50 | 371 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
ChEMBL | Inhibition of recombinant human HDAC8 by fluorimetry | B | 6.44 | pIC50 | 360 | nM | IC50 | J Med Chem (2016) 59: 655-670 [PMID:26705137] |
ChEMBL | Inhibition of recombinant human HDAC8 using fluorogenic substrate by fluorescence assay | B | 6.5 | pIC50 | 314 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
ChEMBL | Inhibition of human recombinant HDAC8 using [RHKK(Ac)] fluorogenic substrate | B | 6.5 | pIC50 | 314 | nM | IC50 | Eur J Med Chem (2021) 217: 113338-113338 [PMID:33744690] |
ChEMBL | Inhibition of human full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell using fluorogenic HDAC class 2a substrate measured after 30 mins by fluorimetry | B | 6.51 | pIC50 | 310 | nM | IC50 | Bioorg Med Chem (2022) 56: 116599-116599 [PMID:35041998] |
ChEMBL | Inhibition of human recombinant C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.51 | pIC50 | 307.4 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
ChEMBL | Inhibition of HDAC8 | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
ChEMBL | Inhibition of HDAC8 (unknown origin) by colorimetric method | B | 6.54 | pIC50 | 290 | nM | IC50 | Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522] |
ChEMBL | Inhibition of human recombinant HDAC8 after 30 mins using fluorogenic substrate by fluorimetric assay | B | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (2018) 61: 6574-6591 [PMID:30004697] |
ChEMBL | Inhibition of recombinant full-length human HDAC8 using FAM-RHKK(Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of recombinant full-length human HDAC8 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | B | 6.63 | pIC50 | 232 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of human HDAC8 by fluorescence assay | B | 6.71 | pIC50 | 196 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
ChEMBL | Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
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 | 6.78 | pIC50 | 165 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of HDAC8 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem (2015) 23: 6785-6793 [PMID:26481659] |
ChEMBL | Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate | B | 6.89 | pIC50 | 129 | nM | IC50 | J Med Chem (2013) 56: 6775-6791 [PMID:23905680] |
ChEMBL | Inhibition of HDAC8 (unknown origin) by ELISA | B | 6.9 | pIC50 | 125 | nM | IC50 | Eur J Med Chem (2018) 148: 73-85 [PMID:29454918] |
ChEMBL | Inhibition of HDAC8 by in vitro deacetylation assay | B | 7 | pIC50 | 100 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
ChEMBL | Inhibition of human HDAC8 | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of human HDAC8 by fluorimetric assay | B | 7.05 | pIC50 | 89.53 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC8 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.05 | pIC50 | 89.5 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human histone deacetylase 8 prepared from 293T cells | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5343-5346 [PMID:15454224] |
ChEMBL | Inhibition of human recombinant HDAC8 after 30 mins by fluorimetric assay | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2009) 52: 7836-7846 [PMID:19705846] |
ChEMBL | Inhibition of HDAC8 after 17 hrs | B | 8.86 | pIC50 | 1.38 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
histone deacetylase 8/Histone deacetylase 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2347] [GtoPdb: 2619] [UniProtKB: Q8VH37] | ||||||||
ChEMBL | Inhibitory activity against histone deacetylase 8 prepared from mouse melanoma B16/BL6 cells | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2427-2431 [PMID:15109626] |
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
ChEMBL | Inhibition of human HDAC9 | B | 6.1 | pKi | 800 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC9 | B | 6.1 | pKi | 800 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
GtoPdb | - | - | 6.1 | pKi | 800 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of recombinant full-length human HDAC9 using FAM-RHKK (trifluor-Ac)-NH2 as substrate by electrophoretic mobility shift assay | B | 5.27 | pIC50 | 5370 | nM | IC50 | J Med Chem (2023) 66: 16075-16090 [PMID:37972387] |
ChEMBL | Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
ChEMBL | Inhibition of recombinant full-length human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | B | 5.31 | pIC50 | 4920 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
ChEMBL | Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
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 | 7.15 | pIC50 | 70.1 | nM | IC50 | US-9265734-B2. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors (2016) |
ChEMBL | Inhibition of human HDAC9 by fluorimetric assay | B | 7.42 | pIC50 | 38.12 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
ChEMBL | Inhibition of human HDAC9 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.42 | pIC50 | 38.1 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
ChEMBL | Inhibition of human HDAC9 | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2346-2349 [PMID:19285395] |
ChEMBL | Inhibition of human recombinant HDAC9 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 7.7 | pIC50 | 20.1 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL | Inhibition of HDAC9 by in vitro deacetylation assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
Histone deacetylase HD1B in Zea mays (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3541] [UniProtKB: Q9ZTP8] | ||||||||
ChEMBL | Inhibition of maize HD1B | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2006) 49: 6046-6056 [PMID:17004718] |
ChEMBL | Inhibition of maize histone deacetylase 1B | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Eur J Med Chem (2008) 43: 621-632 [PMID:17698257] |
Histone deacetylase HD2 in Zea mays (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4919] [UniProtKB: Q94F81] | ||||||||
ChEMBL | Binding affinity against Histone deacetylase 2 (HD2) in maize, expressed as binding constant (pKi) | B | 8.36 | pKi | 4.37 | nM | Ki | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
ChEMBL | Experimental anti-HDAC (anti-histone deacetylase) activity of the compound | B | 8.36 | pKi | 4.37 | nM | Ki | J Med Chem (2001) 44: 2069-2072 [PMID:11405644] |
ChEMBL | Inhibition of maize histone deacetylase 2 | B | 8.14 | pIC50 | 7.2 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
ChEMBL | Inhibitory concentration against histone deacetylase activity | B | 8.14 | pIC50 | 7.2 | nM | IC50 | J Med Chem (2001) 44: 2069-2072 [PMID:11405644] |
ChEMBL | Concentration required for inhibition of histone deacetylase HD2 in vitro. | B | 8.14 | pIC50 | 7.2 | nM | IC50 | J Med Chem (2004) 47: 1098-1109 [PMID:14971890] |
ChEMBL | Inhibitory activity against maize Histone deacetylase 2 at 1 mM | B | 8.14 | pIC50 | 7.2 | nM | IC50 | J Med Chem (2003) 46: 4826-4829 [PMID:14584932] |
ChEMBL | Inhibition of maize Histone deacetylase 2 | B | 8.15 | pIC50 | 7.08 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
ChEMBL | Inhibition of maize HD2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2006) 49: 6046-6056 [PMID:17004718] |
ChEMBL | In vitro for anti-HD2 (Histone deacetylase 2) activity in maize | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
ChEMBL | Inhibitory concentration against maize histone deacetylase 2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2005) 48: 3344-3353 [PMID:15857140] |
ChEMBL | Inhibition of maize Histone deacetylase 2 (HD-2) activity | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1999) 42: 4669-4679 [PMID:10579829] |
ChEMBL | Inhibitory concentration against maize Histone deacetylase 2 | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
ChEMBL | Inhibitory concentration against maize Histone deacetylase 2 | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
ChEMBL | Inhibition of in vitro enzyme activity measured in a highly purified maize Histone deacetylase 2 preparation | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2002) 45: 3296-3309 [PMID:12109913] |
Histone deacetylase-like amidohydrolase in Alcaligenes sp. (strain DSM 11172) (Bordetella sp. (strain FB188)) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6017] [UniProtKB: Q70I53] | ||||||||
ChEMBL | Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy | B | 6.15 | pKi | 700 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
ChEMBL | Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorimetric assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960] | ||||||||
ChEMBL | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 1817-1828 [PMID:28218840] |
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
ChEMBL | Inhibition of KDM4E (unknown origin) | B | 4.55 | pIC50 | 28400 | nM | IC50 | J Med Chem (2022) 65: 9564-9579 [PMID:35838529] |
sirtuin 6/NAD-dependent protein deacetylase sirtuin-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163182] [GtoPdb: 2712] [UniProtKB: Q8N6T7] | ||||||||
ChEMBL | Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins in presence of ADP-ribose by fluorescence-based SDS-denaturation assay | B | 4.48 | pKd | 33000 | nM | Kd | J Med Chem (2018) 61: 10922-10928 [PMID:30395713] |
ChEMBL | Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins in presence of ADP-ribose and acetylated H3K9 peptide by fluorescence-based SDS-denaturation assay | B | 4.54 | pKd | 29000 | nM | Kd | J Med Chem (2018) 61: 10922-10928 [PMID:30395713] |
ChEMBL | Inhibition of SIRT6 deacetylation (unknown origin) using p53K382Ac peptide as substrate | B | 5.34 | pKi | 4620 | nM | Ki | J Med Chem (2021) 64: 9732-9758 [PMID:34213345] |
ChEMBL | Inhibition of SIRT6 deacetylation (unknown origin) using H3K9Ac peptide as substrate | B | 5.69 | pKi | 2020 | nM | Ki | J Med Chem (2021) 64: 9732-9758 [PMID:34213345] |
ChEMBL | Inhibition of full length SIRT6 (unknown origin) using acetylated H3K9 peptide as substrate after 2 hrs in presence of NAD | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (2018) 61: 10922-10928 [PMID:30395713] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | F | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2009) 52: 2185-2187 [PMID:19317450] |
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by LDH reporter assay | F | 7.81 | pIC50 | 15.6 | nM | IC50 | Bioorg Med Chem (2008) 16: 5254-5265 [PMID:18362073] |
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by LDH reporter assay | F | 7.81 | pIC50 | 15.49 | nM | IC50 | Bioorg Med Chem (2008) 16: 5254-5265 [PMID:18362073] |
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | F | 7.96 | pIC50 | 11 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1454-1461 [PMID:18212103] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by LDH reporter assay | F | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2008) 16: 5254-5265 [PMID:18362073] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by LDH reporter assay | F | 8.01 | pIC50 | 9.77 | nM | IC50 | Bioorg Med Chem (2008) 16: 5254-5265 [PMID:18362073] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1454-1461 [PMID:18212103] |
ChEMBL | Antimalarial activity against Plasmodium falciparum infected in erythrocytes after 2 hrs | F | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum | F | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 6.7 | pEC50 | 200.2 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 6.77 | pEC50 | 170.8 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
Splicing factor 3B subunit 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250378] [UniProtKB: Q15393] | ||||||||
ChEMBL | Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay | B | 6.21 | pIC50 | 611.2 | nM | IC50 | Nat Chem Biol (2007) 3: 570-575 [PMID:17643112] |
ChEMBL | Inhibition of SAP130 mediated cell growth in human WiDr cells | B | 6.24 | pIC50 | 577.6 | nM | IC50 | Nat Chem Biol (2007) 3: 570-575 [PMID:17643112] |
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473] | ||||||||
ChEMBL | Agonist activity at Vitamin D receptor (unknown origin) by fluorescence polarization assay | B | 7.06 | pIC50 | 87 | nM | IC50 | Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264] |
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]