Assay ID | Title | Year | Journal | Article |
AID90677 | Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi) | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
| Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation. |
AID1532634 | 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 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID1394889 | Inhibition of human HDAC1 using RHKK(Ac) as substrate | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID385445 | Effect on TNF-alpha-induced TFkappaB activation assessed as p65/p50 binding to TFkappaB in HUVEC preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID300678 | Antiproliferative activity against H661 cells after 48 hrs by XTT assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
| Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors. |
AID755476 | Inhibition of recombinant human HDAC7 using acetyl-Lys-(trifluoroacetyl)-AMC as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID1622916 | Inhibition of recombinant full-length human HDAC1 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1324229 | Inhibition of HDAC6 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
AID1384765 | Selectivity index, ratio of IC50 for human HDAC2 to IC50 for human HDAC6 | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID1595394 | Inhibition of HDAC in human HeLa nuclear extract assessed as enzyme residual activity at 500 nM using Boc-Lys(acetyl)-AMC as substrate and measured after 15 mins by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability. |
AID1401640 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1628751 | Antiproliferative activity against human SK-BR-3 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1294970 | Inhibition of human recombinant HDAC9 using trifluoroacetyl lysine as substrate | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1127328 | Inhibition of human HDAC7 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID488357 | Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1322061 | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID764213 | Inhibition of human recombinant HDAC4 using p53 residues 379-382 (RHKKAc) as substrate | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID1758522 | Inhibition of human recombinant HDAC8 using [RHKK(Ac)] fluorogenic substrate | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID1622925 | Inhibition of recombinant full-length human HDAC10 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1647308 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus infected insect cells using Boc-K(Ac)-AMC as substrate after 90 mins by fluorimetry analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1156707 | Cytotoxicity against human MOLT4 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID446381 | Inhibition of SIRT2 in human MCF7 cells assessed as tubulin hyperacetylation at 0.1 uM after 16 hrs by Western blot | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins). |
AID1853418 | Inhibition of human MMP-8 at 0.5 uM | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID1384758 | Inhibition of human HDAC10 using RHKKAc peptide as substrate | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID1628763 | Antiproliferative activity against human PC3 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID367241 | Selectivity ratio of IC50 for human recombinant histone deacetylase 8 to IC50 for human recombinant histone deacetylase 6 | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID525025 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 0.1 uM by RT-PCR | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1702070 | 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 | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID50586 | Inhibitory concentration against colon HCT116 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID156319 | Inhibitory activity against PC-3 cell line | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| QSAR studies of PC-3 cell line inhibition activity of TSA and SAHA-like hydroxamic acids. |
AID1401593 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID90346 | Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1); Potent inhibitor | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
| (2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors. |
AID1529528 | Antiproliferative activity against human K562 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID516284 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH412 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID90662 | Inhibition against partially purified human histone deacetylase 1 (HDAC-1) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID1401632 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1155332 | Inhibition of HDAC in Plasmodium falciparum 3D7 trophozoites assessed as histone H4 hyperacetylation level at 500 nM after 3 hrs by Western blotting analysis relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID385450 | Inhibition of IL-1-beta-induced tissue factor activity in C57BL/6J mouse macrophages preincubated for 4 hrs assessed after 5 hrs of IL1-beta challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1363777 | Inhibition of C-terminal FLAG-His-tagged full length recombinant human HDAC1 expressed in Sf21 insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID1387537 | Inhibition of mouse HDAC6 expressed in 293T cells at 100 uM using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay relative to control | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors. |
AID1363779 | Inhibition of recombinant human HDAC3/NCOR2 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID1384759 | Inhibition of human HDAC1 using RHKKAc peptide as substrate | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID1459971 | Inhibition of recombinant human HDAC7 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1863433 | Inhibition of HDAC1 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID503117 | Induction of p21 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA. |
AID1431818 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1862613 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID366644 | Inhibition of HDAC6 after 17 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. |
AID723728 | Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID90838 | Tested for inhibition of Histone deacetylase 6 induced acetylated tubulin in mammalian cells. | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID324484 | Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID324380 | Induction of light chain 3-GFP level in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID43027 | Cytotoxicity of compound against normal human ovarian C18013S cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID1656940 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability | | | |
AID90354 | Inhibitory concentration against human histone deacetylase (HDAC) | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID1173707 | Inhibition of HDAC6 (unknown origin) after 15 mins by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Aurones as histone deacetylase inhibitors: identification of key features. |
AID358673 | Induction of REST/NRSF-coupled repression of luciferase tagged rat RE1/NRSE BDNF promoter activity expressed in ST14A cells at 75 nM assessed as increase in luciferase activity | 2007 | The Journal of biological chemistry, Aug-24, Volume: 282, Issue:34
| Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators. |
AID1529535 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1833068 | Selectivity ratio of IC50 for full length recombinant C-terminal GST-fusion-tagged human HDAC2 to IC50 for full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID230221 | Inhibitory concentration against HDAC6/HDAC1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID90695 | Inhibition of maize Histone deacetylase 2 (HD-2) activity | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
| Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. |
AID1589335 | Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate at 50 uM by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors. |
AID769933 | Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1862615 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1862608 | Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1236441 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1127327 | Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1622966 | Inhibition of recombinant human HDAC1 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID408886 | Selectivity for HDAC6 over HDAC1 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID1765332 | Selectivity index, ratio of IC50 for human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID628435 | Inhibition of human recombinant HDAC4 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID1401636 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID723464 | Inhibition of human HDAC4 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID408887 | Selectivity for HDAC10 over HDAC1 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID503530 | Inhibition of HDAC in human GM15850 cells assessed as increase in total acetylated histone level at 0.1 uM after 12 hrs by Western blot analysis | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID408882 | Inhibition of HDAC3 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID1127326 | Inhibition of human HDAC5 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1529532 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1586078 | Inhibition of human HDAC2 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID90840 | Inhibitory activity against histone deacetylase 8 prepared from mouse melanoma B16/BL6 cells | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand. |
AID1394891 | Inhibition of human HDAC6 using RHKK(Ac) as substrate | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID417069 | Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives. |
AID1532656 | Antiangiogenic activity in zebrafish embryo assessed as effect on blood vessel development at 10 uM administered from 24 to 50 hrs post fertilization for 24 hrs and measured after 72 hrs by alkaline phosphatase assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID670032 | Inhibition of Class 1 histone deacetylase in human MCF7 cells assessed as up-regulation of p21 protein level at 0.5 uM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets. |
AID324432 | Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID524996 | Inhibition of HDAC8 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1363780 | 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 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID654541 | Inhibition of human HDAC1 after 30 mins by fluorescence assay | 2012 | Journal of natural products, Feb-24, Volume: 75, Issue:2
| Trichostatin analogues JBIR-109, JBIR-110, and JBIR-111 from the marine sponge-derived Streptomyces sp. RM72. |
AID1578490 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID1177040 | Cytotoxicity against human LO2 cells after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909. |
AID551713 | Inhibition of HDAC by fluorescent activity assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Design and synthesis of aryl ether and sulfone hydroxamic acids as potent histone deacetylase (HDAC) inhibitors. |
AID1557982 | 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 s | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models. |
AID417649 | Inhibition of human HDAC6 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID1758525 | Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC6 | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID1459973 | Inhibition of recombinant human HDAC9 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1260640 | Inhibition of human recombinant HDAC4 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID456799 | Cytotoxicity against african green monkey Vero cells after 1 to 2 days by neutral red assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID683274 | Inhibition of HDAC1 by fluorometric assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects. |
AID1781512 | Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9
| Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from |
AID1622918 | Inhibition of recombinant full-length human HDAC3/NCOR2 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1394892 | Inhibition of human HDAC8 using RHKAcKAc as substrate | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1156703 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID90338 | Tested for inhibitory concentration required to inhibit 50% of histone deacetylase (HDAC) from human T cell leukemia Jurkat cell | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
| Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group. |
AID519598 | Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1605942 | Inhibition of recombinant human C-terminal His-fusion tagged HDAC5 (657 to 1123 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1833064 | 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 | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID541646 | Inhibition of human HDAC3 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1651337 | Selectivity ratio of IC50 for recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells to IC50 of human HDAC6 | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID1401622 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID350020 | Antiproliferative activity against human NCI-H661 cells after 48 hrs by XTT assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression. |
AID1532636 | 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 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID316882 | Growth inhibition of human neonatal foreskin fibroblasts cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID456795 | Inhibition of HDAC in human HeLa cell nuclear extracts after 15 mins by fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID308643 | Inhibition of human HDAC1 | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
| Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID1423502 | Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins in presence of NAM by fluorescence-based SDS-denaturation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development. |
AID1421905 | Cytotoxicity against human NFF cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID487226 | Inhibition of recombinant HDAC3 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID487231 | Inhibition of HDAC10 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID90680 | Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies. |
AID1764791 | 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 | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model. |
AID1459954 | Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID417651 | Inhibition of human HDAC8 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID299644 | Increase in GRP78 protein level in HEK293 cells at 600 nM by immunoblot | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition. |
AID385470 | Effect on TNF-alpha-induced NF-kappaB activation assessed as p65/p50 binding to NF-kappaB in HUVEC at 0.3 uM preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1630623 | Inhibition of recombinant C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID1210092 | Increase in NAT1 enzyme activity in 100% confluent human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1628760 | Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1557981 | 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 mi | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models. |
AID90691 | Inhibition of maize Histone deacetylase 2 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies. |
AID764212 | Inhibition of human recombinant HDAC6 using p53 residues 379-382 (RHKKAc) as substrate | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID524999 | Inhibition of HDAC6 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID385465 | Induction of PMA-induced TFkappaB-dependent wild type tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay relative to control | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1901144 | 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 | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1622921 | Inhibition of recombinant full-length human HDAC5 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1276712 | Inhibition of recombinant human HDAC6 by fluorimetry | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors. |
AID1177041 | Cytotoxicity against human HEK293 cells after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909. |
AID80353 | Concentration required to inhibit the partially purified HDAC enzyme by 50% obtained from H1299 cell lysate | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
| Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1709383 | 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 | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1401602 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID723460 | Inhibition of human HDAC11 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID420318 | Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorimetric assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1182190 | Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors. |
AID1459955 | Inhibition of recombinant human HDAC6 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1529510 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID417646 | Inhibition of human HDAC3 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID143656 | Cytotoxicity of compound against normal human normal neonatal foreskin fibroblasts (NFF) | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID704015 | 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 | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
| Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose. |
AID447996 | Inhibition of human recombinant HDAC6 after 30 mins by fluorimetric assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides. |
AID507021 | Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Splicing factor SF3b as a target of the antitumor natural product pladienolide. |
AID1628750 | Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID331898 | 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 HDAC in human HeLa nuclear cell extract by fluorescence p | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. |
AID1401608 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID652766 | Induction of CFTR deltaF508 mutant protein expression in cystic fibrosis patient lung cells relative to control | 2011 | ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
| Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR. |
AID385446 | 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 | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1690107 | 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 | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID1173704 | Inhibition of HDAC in human HeLa cell extract after 15 mins by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Aurones as histone deacetylase inhibitors: identification of key features. |
AID611684 | Inhibition of human HDAC2 using rhodamine as substrate after 1 hrs by fluorescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors. |
AID465154 | Inhibition of HDAC6 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1384209 | Inhibition of HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease. |
AID1401557 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1901151 | Inhibition of recombinant human N-terminal GST-fused/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC class 2a substrate measured after 30 mins by fluorimetry | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID1401633 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1479817 | Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate after 60 mins by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID360096 | Inhibition of IL-1-beta-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of IL1-beta challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1764788 | Inhibition of HDAC6 in mouse Neuro2a cells assessed as fold increase in ratio of acetylated alpha-tubulin to alpha tubulin at 1 uM incubated for overnight by Western blot analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model. |
AID449703 | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
| In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. |
AID456796 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID1898913 | Inhibition of HDAC11 (unknown origin) using fluorogenic peptide 382 RHKK(Ac)AM as substrate and measured by fluorescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Antitumor activity of novel POLA1-HDAC11 dual inhibitors. |
AID1578491 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID628429 | Inhibition of human recombinant HDAC11 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID201971 | Cytotoxicity of compound against normal human melanoma SK-MEL-28 cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID1155333 | Inhibition of histone deacetylase in Plasmodium falciparum nuclear lysates at 1 uM by fluorescence assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID566552 | Inhibition of HDAC in human HeLa cells at 1 uM after 10 mins by fluorometric assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
| Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells. |
AID516295 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH444 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1294967 | 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 | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1591717 | Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID1690109 | Inhibition of recombinant human HDAC6 using RHK-K(Ac)-AMC as substrate by fluorescence based assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID538408 | Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Inhibitors selective for HDAC6 in enzymes and cells. |
AID1260638 | Inhibition of human recombinant HDAC2 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID628431 | Inhibition of human recombinant HDAC9 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID1431817 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1431813 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1127323 | Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID695596 | Inhibition of HDAC6 by fluorimetric assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
| Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases. |
AID90529 | Inhibitory concentration against histone deacetylase | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID496807 | Inhibition of human HDAC7 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1401598 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1605959 | Inhibition of recombinant full length human C-terminal His-tagged HDAC3 (1 to 428 residues) expressed in baculovirus infected insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluo | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID8297 | Inhibitory concentration required to reduce A549 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID1459970 | Inhibition of recombinant human HDAC5 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1532646 | Selectivity ratio of IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) to IC50 for recombinant C-terminal His-tagged human HDAC8 (1 to 377 residues) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID385434 | Inhibition of LPS-induced tissue factor activity in HUVEC at 0.3 uM preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1532640 | Selectivity ratio of IC50 for recombinant full length C-terminal FLAG/His-tagged human HDAC1 (1 to 482 residues) to IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID1656941 | Cytotoxicity against human A2058 cells assessed as reduction in cell viability | | | |
AID1758520 | Inhibition of human recombinant HDAC3 using [RHKK(Ac)] fluorogenic substrate | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID568155 | Inhibition of HDAC8 by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID1384762 | Inhibition of human HDAC8 using RHKAcKAc peptide as substrate | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID408885 | Inhibition of HDAC6 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID1479811 | Inhibition of full length recombinant human C-terminal GST-tagged HDAC2 expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID90520 | Inhibition of in vitro enzyme activity measured in partially purified rat liver Histone deacetylase preparation | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
| Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells. |
AID519597 | Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-resistant Plasmodium falciparum Dd2 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1127324 | Inhibition of human HDAC3 complexed with NCOR2 using fluorogenic tetrapeptide RHKKAc as susbtrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1127330 | Inhibition of human HDAC9 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1280314 | Inhibition of human KDAC1 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1503585 | 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 | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Serendipitous discovery of potent human head and neck squamous cell carcinoma anti-cancer molecules: A fortunate failure of a rational molecular design. |
AID420317 | Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID461092 | Inhibition of HDAC4 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length. |
AID755477 | Inhibition of recombinant human HDAC6 using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID102521 | Inhibitory concentration against lung H446 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID659293 | Inhibition of HDAC2 in human HeLa cell nuclear extracts in presence of dithiothreitol by HDAC fluorescent assay | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study. |
AID756006 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Cdh1 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID1863437 | Inhibition of HDAC5 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1622948 | Inhibition of human HDAC6 using fluorogenic HDAC substrate | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1765331 | Selectivity index, ratio of IC50 for human recombinant full length HDAC6 to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1622923 | Inhibition of recombinant full-length human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1863438 | Inhibition of HDAC6 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1605950 | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID417645 | Inhibition of human HDAC2 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID447579 | Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
| Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies. |
AID1647307 | 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 | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1765326 | 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 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1236443 | Inhibition of human HDAC2 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1656944 | Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability | | | |
AID1863434 | Inhibition of HDAC2 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID650229 | Inhibition of HDAC1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1276706 | Inhibition of recombinant human HDAC2 by fluorimetry | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors. |
AID755480 | Inhibition of recombinant human HDAC2 using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID503115 | Induction of p16 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA. |
AID1628746 | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1363778 | Inhibition of C-terminal GST-tagged recombinant human HDAC2 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID420326 | Inhibition of HDAC from human HeLa cells by fluorogenic enzyme assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1401630 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID496806 | Inhibition of human HDAC6 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID90661 | In vitro inhibition of partially purified recombinant human Histone deacetylase 1 | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
| Design and synthesis of a novel class of histone deacetylase inhibitors. |
AID316875 | Inhibition of HDAC from human HeLa cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1246510 | Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID449705 | NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
| In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. |
AID568153 | Inhibition of HDAC4 by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID525021 | Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 5 uM by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1294973 | 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 | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1622992 | Antiproliferative activity against human MCF7 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1246508 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1765324 | 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 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1260641 | Inhibition of human recombinant HDAC5 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID605941 | Cytostatic activity against human DMS53 cells assessed as inhibition of cell proliferation after 2 days by MTT assay | 2011 | Journal of natural products, May-27, Volume: 74, Issue:5
| Microbial transformation of trichostatin A to 2,3-dihydrotrichostatin A. |
AID385452 | Inhibition of baseline tissue factor activity in non-stimulated C57BL/6J mouse macrophages after 4 hrs by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1177038 | Cytotoxicity against human HepG2 cells after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909. |
AID516317 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate RB3 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID43458 | Inhibitory concentration against breast MCF-7 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1390226 | Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B-based colorimetric assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors. |
AID420325 | Inhibition of HDAC1 in human NIH3T3 cells by radiometric histone deacetylation assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1441700 | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
AID1401600 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID273168 | Inhibition of maize HD1B | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1384767 | Selectivity index, ratio of IC50 for human HDAC8 to IC50 for human HDAC6 | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID723726 | Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID1853420 | Inhibition of human TACE at 0.5 uM by fluorescence based assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID104356 | Cytotoxicity against human melanoma MM96L cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID1156708 | Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID1354369 | Antiproliferative activity against human HL60 cells after 24 hrs by MTT assay | | | |
AID723462 | Inhibition of human HDAC6 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID488277 | Inhibition of HDAC8 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1647302 | Inhibition of recombinant N-terminal GST-tagged/C-terminal His-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1586081 | Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID90199 | Experimental anti-HDAC (anti-histone deacetylase) activity of the compound | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
| 3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors. |
AID1862621 | Inhibition of HDAC8 (unknown origin) measured by fluorometry assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1605948 | 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 | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1431811 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID90681 | Inhibition of mouse HDAC1 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies. |
AID487228 | Inhibition of recombinant HDAC8 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID568150 | Inhibition of HDAC1 by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID1702063 | Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 (627 to 1084 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID382113 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by LDH reporter assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
| Structural insights into the Plasmodium falciparum histone deacetylase 1 (PfHDAC-1): A novel target for the development of antimalarial therapy. |
AID756008 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Sox2 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID105452 | Inhibitory concentration required to reduce MDAmb 231 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID756023 | Inhibition of HDAC2 (unknown origin) after 30 mins by fluorometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID143655 | Cytotoxicity of compound against human normal neonatal foreskin fibroblasts (NFF) cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID1758524 | Selectivity ratio of IC50 for human recombinant HDAC3 to IC50 for human recombinant HDAC6 | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID360090 | Effect on TNF-alpha-induced increase in HDAC3 binding to TFkappaB in HUVEC cells at preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by chromatin immunoprecipitation assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1702065 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID659292 | Inhibition of human HDAC1 in presence of dithiothreitol by HDAC fluorescent assay | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study. |
AID1324226 | Inhibition of HDAC1 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
AID360094 | 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 | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID723466 | Inhibition of human HDAC1 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID1293877 | Competitive inhibition of HDAC in human HeLa nuclear cells at 10 to 25 uM using Boc-acetyl-lysine-AMC as substrate after 30 mins by Lineweaver-Burk plot analysis | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID1595395 | Inhibition of HDAC in human HeLa nuclear extract assessed as enzyme residual activity at 50 nM using Boc-Lys(acetyl)-AMC as substrate and measured after 15 mins by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability. |
AID1630622 | Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID1586082 | Inhibition of human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID519600 | Antimalarial activity against Plasmodium falciparum infected in O+ human erythrocytes assessed as reduction in parasites at trophozoites stage at 200 nM after 48 hrs by Giemsa staining based microscopy | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID417647 | Inhibition of human HDAC4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID1853417 | Inhibition of human MMP-7 at 0.5 uM | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID71648 | Inhibitory concentration against friend cells proliferation | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID1862606 | Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1651336 | Selectivity ratio of IC50 for recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells to IC50 of human HDAC6 | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID1862612 | Antiproliferative activity against human SK-OV-3 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID350024 | Increase in E-cadherin mRNA expression in human NCI-H661 cells at 300 nM by qRT-PCR relative to control | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression. |
AID1210091 | Increase in NAT1 enzyme activity in 40% confluent human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1605939 | 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 | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID756005 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Dppa4 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID316876 | Inhibition of human SQ20B cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1387536 | Inhibition of human HDAC1 expressed in 293T cells at 100 uM using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay relative to control | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors. |
AID252223 | Average fold change in expression of CYP1A1 after treatment with compound of concentration 0.01 mM in human MCF-7 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells. |
AID628434 | Inhibition of human recombinant HDAC5 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID519587 | Toxicity in neonatal foreskin fibroblasts | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID541647 | Inhibition of human HDAC8 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID360091 | Inhibition of TNF-alpha-induced tissue factor activity in HUVEC at 1 uM preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1901071 | Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as serum EPO level at 10 mg/kg/day, ip | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1833065 | 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 | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID760387 | Inhibition of human recombinant HDAC4 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
| Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1656939 | Inhibition of mushroom tyrosinase using L-DOPA as substrate | | | |
AID366642 | Inhibition of HDAC3 after 17 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. |
AID1702062 | Inhibition of recombinant human C-terminal His-tagged HDAC3 (1 to 428 end residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins b | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID1210099 | Induction of Sp1 recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1246515 | Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1354370 | Antiproliferative activity against human MDA-MB-435 cells after 24 hrs by MTT assay | | | |
AID385448 | Inhibition of LPS-induced tissue factor activity in C57BL/6J mouse macrophages preincubated for 4 hrs assessed after 5 hrs of LPS challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1702061 | Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID242560 | Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 3b | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID1384760 | Inhibition of human HDAC2 using RHKKAc peptide as substrate | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID463864 | Inhibition of human HDAC in human HeLa cell nuclear extract at 50 nM after 15 mins by colorimetric assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors. |
AID1630587 | Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system using fluorogenic peptide RHKK(Ac) as substrate by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID1246507 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1459972 | Inhibition of recombinant human HDAC8 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID313186 | Inhibition of HDAC4 expressed in 293T cells | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides. |
AID385455 | Effect on TNF-alpha-induced NF-kappaB activation in HUVEC preincubated for 4 hrs assessed as increase in p50 level after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1605962 | Inhibition of HDAC10 (unknown origin) at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1702064 | Inhibition of HDAC5 (unknown origin) using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID756010 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Oct3/4 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID1605952 | Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1833063 | 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 | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID420321 | Inhibition of Bordetella / Alcaligenes strain FB188 HDAC6 by fluorescence polarization assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID1280315 | Inhibition of human KDAC3 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID252221 | Average fold change in expression of CYP1B1 after treatment with compound of concentration 0.1 mM in human MCF-7 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells. |
AID1578487 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID611685 | Inhibition of human HDAC6 using rhodamine as substrate after 1 hrs by fluorescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors. |
AID90699 | Inhibitory activity against histone deacetylase (HDAC4) prepared from mouse melanoma B16/BL6 cells | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand. |
AID496802 | Inhibition of human HDAC2 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1586080 | Inhibition of human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1363781 | 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 | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
AID764214 | Inhibition of human recombinant HDAC1 using p53 residues 379-382 (RHKKAc) as substrate | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID90679 | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells. | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID1387552 | Inhibition of HDAC in human HeLaS3 cells assessed as increase in histone H3K9 acetylation at 10 uM measured immediately by immunoblot analysis | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors. |
AID252219 | Average fold change in expression of CYP1B1 after treatment with compound of concentration 1 mM in human MCF-7 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells. |
AID1764792 | 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 | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model. |
AID760388 | Inhibition of human recombinant HDAC8 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
| Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1847753 | Antiproliferative activity against human T47D cells assessed as cell growth inhibition by burton method | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
AID1764793 | Selectivity index, ratio of IC50 for recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells to recombinant full length human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate pr | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model. |
AID755998 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Otx2 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID1479814 | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus-infected Sf21 insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID1709382 | Inhibition of recombinant human full-length C-terminal FLAG/His-tagged HDAC1 (1 to 482 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 af | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID1622922 | Inhibition of recombinant full-length human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID308644 | Inhibition of human HDAC4 | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
| Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID1882456 | Inhibition of HDAC1 (unknown origin) | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
| Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology. |
AID1702068 | Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID1578485 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID708215 | Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. |
AID659294 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study. |
AID1246512 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID525002 | Inhibition of HDAC3 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1479819 | Inhibition of recombinant human HDAC10 expressed in baculovirus-infected insect cells using fluorogenic peptide RHKKAc as substrate by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID299642 | Inhibition of HDAC in HEK293 cells assessed as increase in histone H4 acetylation at 600 nM after 48 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition. |
AID385471 | Effect on TNF-alpha-induced NF-kappaB activation assessed as p65/p50 binding to NF-kappaB in HUVEC at 1 uM preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID55804 | Cytotoxicity of compound against normal human prostate DU145 cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID233841 | Selectivity as ratio of inhibitory concentration for NFF cell line versus MM96L cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID385449 | Inhibition of TNF-alpha-induced tissue factor activity in C57BL/6J mouse macrophages preincubated for 4 hrs assessed after 5 hrs of TNFalpha challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID769928 | Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1847776 | Inhibition of HDAC4 in human HeLa cells incubated for 1 hr by mass spectrometry method | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
AID1591716 | 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 | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID8302 | Compound was tested for antiproliferative activity against human A549 cancer cell lines using MTT assay | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
AID683277 | Antiproliferative activity against human BE(2)-C cells after 72 hrs by Alamar blue assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects. |
AID503116 | Induction of p27 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA. |
AID1635106 | Upregulation of HDAC1 inhibition/ERK signalling activation-mediated extracellular SOD protein expression in human THP1 cells at 1 uM after 24 hrs by ELISA | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4
| Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells. |
AID538409 | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Inhibitors selective for HDAC6 in enzymes and cells. |
AID90693 | Binding affinity against Histone deacetylase 2 (HD2) in maize, expressed as binding constant (pKi) | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
| Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation. |
AID1622920 | Inhibition of recombinant full-length human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID90197 | Inhibitory concentration against histone deacetylase activity | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
| 3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors. |
AID1630621 | Inhibition of recombinant N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID769932 | Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID331899 | 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 | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. |
AID1651332 | 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 | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID516293 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH189 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1622973 | Inhibition of HDAC4 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID309970 | Induction of wild-type p21 promoter activation in mink Mv1Lu cells after 18 hrs by luciferase assay relative to basal level | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. |
AID1605955 | Inhibition of human PI3Kgamma assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1254049 | Inhibition of HDAC8 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation. |
AID385447 | 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 | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID417654 | Inhibition of human HDAC11 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID1322060 | 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 | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID324909 | Inhibition of human HDAC6 assessed as tubulin hyperacetylation in human HCT116 cells by Western blot | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs). |
AID516296 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH409 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID366643 | Inhibition of HDAC8 after 17 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. |
AID269912 | Inhibition of HDAC4 | 2006 | Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
| Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. |
AID1182186 | Inhibition of human HDAC1 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors. |
AID385467 | Induction of PMA-induced wild type NF-kappaB-dependent ICAM promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay relative to control | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID760385 | Inhibition of human recombinant HDAC5 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
| Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1628748 | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1127331 | Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1260647 | Inhibition of human recombinant HDAC11 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID104054 | Cytotoxicity of compound against normal human breast MCF-7 cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID541648 | Inhibition of human HDAC4 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1479812 | 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 | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID1401561 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1177036 | Up-regulation of transcriptional activity of human CLA-1 promoter region -1055 to -62bp transfected in HepG2 cells by luciferase reporter gene assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909. |
AID1431822 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID769927 | Induction of neurite outgrowth in rat PC12 cells at 10 uM after 5 days | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID309968 | Inhibition of human HDAC4 expressed in 293T cells | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. |
AID1605954 | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID316887 | Antiproliferative activity against human MKN45 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID385451 | Reduction of ICAM1 mRNA level in TNF-alpha-stimulated HUVEC at 1 uM preincubated for 4 hrs assessed after 1 to 2 hrs of TNFalpha challenge by RT-PCR | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID503304 | Antiproliferative activity against human PC3 cells at 5 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6
| Identifying off-target effects and hidden phenotypes of drugs in human cells. |
AID331900 | 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 | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. |
AID1622924 | Inhibition of recombinant full-length human HDAC6 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1758519 | Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect cells using [RHKK(Ac)] fluorogenic substrate | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID525008 | Inhibition of HDAC7 in Fdelta508 CFTR-expressing human CFBE41o- cell line assessed as increase in cAMP-stimulated iodide efflux in at 0.1 uM after 24 hrs relative to control | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID309967 | Inhibition of human HDAC1 expressed in 293T cells | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. |
AID1532649 | Selectivity ratio of IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) to IC50 for recombinant C-terminal His-tagged human HDAC11 (1 to 347 residues) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID1371055 | Inhibition of recombinant Trypanosoma brucei HDAC3 at 5 uM after 30 mins | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID90350 | Inhibitory activity against histone deacetylase (HDAC) enzyme obtained from H1299 human lung carcinoma cell lysates | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824). |
AID1605940 | 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 | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1479816 | Inhibition of recombinant human C-terminal GST-tagged HDAC4 expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID1901145 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorimetry | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID240034 | Effective concentration determined for p21 promoter assay | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones. |
AID1156700 | Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID1236442 | Inhibition of human HDAC1 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1647306 | Inhibition of human HDAC9 using fluorogenic Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence based analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID447994 | Inhibition of human recombinant HDAC3 after 30 mins by fluorimetric assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides. |
AID242587 | Inhibition concentration required to inhibit rat liver histone deacetylase (HDAC) in the presence of compound 5e as a substrate | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID209973 | Inhibition of acetylation of histone-4 in human T-24 cancer cells | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID240717 | Inhibition of human histone deacetylase 1 prepared from 293T cells | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones. |
AID1260642 | Inhibition of human recombinant HDAC6 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID566555 | Inhibition of HDAC in human PC3 cells at 1 uM after 10 mins by fluorometric assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
| Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells. |
AID478330 | Inhibition of HDAC in human HeLa cell nuclear extract assessed as inhibition of histone H4 deacetylation after 15 mins by fluorescence assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Synthesis and biological activity of cyclotetrapeptide analogues of the natural HDAC inhibitor FR235222. |
AID90671 | Inhibitory activity afgainst maize Histone deacetylase 1-A | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID299654 | Increase in GRP78 protein level in HEK293 cells at 600 nM by immunoblot | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition. |
AID1647311 | 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 | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1260643 | Inhibition of human recombinant HDAC7 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID1765329 | Selectivity index, ratio of IC50 for human recombinant full length HDAC1 to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1401626 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID568154 | Inhibition of HDAC6 by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID1529534 | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1586085 | Inhibition of human HDAC10 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID57526 | Cytotoxicity of compound against normal human melanoma DO4 cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID1401601 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1702067 | 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 | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID1586077 | Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID417644 | Inhibition of human HDAC1 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID382112 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by LDH reporter assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
| Structural insights into the Plasmodium falciparum histone deacetylase 1 (PfHDAC-1): A novel target for the development of antimalarial therapy. |
AID1622990 | Antiproliferative activity against human A549 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1529533 | Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1622968 | Inhibition of recombinant mouse HDAC6 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1432955 | Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors. |
AID488358 | Inhibition of HDAC1 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group. |
AID1431815 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID519584 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID385443 | Effect on TNF-alpha-induced IkappaB degradation in HUVEC at 1 uM preincubated for 4 hrs assessed after 60 mins of TNFalpha challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1127332 | Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1156704 | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID385466 | Induction of PMA-induced TFkappaB mutant-dependent tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay relative to control | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID58061 | Inhibitory concentration required to reduce DU145 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID539709 | Inhibition of human HDAC after 30 mins | 2010 | Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
| Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase. |
AID385468 | Inhibition of LPS-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID652765 | Induction of CFTR deltaF508 mutant mRNA expression in cystic fibrosis patient lung cells relative to control | 2011 | ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
| Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR. |
AID1518780 | Inhibition of human HDAC6 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID242559 | Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 3a | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID764211 | Selectivity ratio of IC50 for human recombinant HDAC1 to human recombinant HDAC6 | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID385462 | Inhibition of LPS-induced wild type TFkappaB-dependent tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of LPS challenge by luciferase reporter assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1401595 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1586084 | Inhibition of human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID611683 | Inhibition of human HDAC1 using rhodamine as substrate after 1 hrs by fluorescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors. |
AID541655 | Growth inhibition of human H460 cells after 48 hrs by SRB assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID367236 | Induction of histone H3 acetylation in human T24 cells | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID252225 | Average fold change in expression of CYP1B1 after treatment with compound of concentration 0.01 mM in human MCF-7 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells. |
AID1647310 | Inhibition of recombinant human C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in baculovirus infected insect cells using Boc-K(Ac)-AMC as substrate after 60 mins by fluorimetry analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID525034 | In vivo inhibition of HDAC | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1647300 | 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 | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1210095 | Increase in NAT1 mRNA expression in human HeLa cells at 0.5 uM after 24 hrs by qPCR method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1401605 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID73169 | Inhibitory concentration against normal fibroblast MRHF cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1155334 | Inhibition of Plasmodium falciparum recombinant histone deacetylase1 using HDAC substrate 3 as substrate at 1 uM by fluorescence assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID316886 | Antiproliferative activity against human SKBR3 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1479818 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus-infected insect cells after 60 mins by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID385454 | Reduction of tissue factor mRNA level in TNF-alpha-stimulated HUVEC at 1 uM preincubated for 4 hrs assessed after 1 to 2 hrs of TNFalpha challenge by RT-PCR | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1294953 | 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 | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1384761 | Inhibition of human HDAC3 using RHKKAc peptide as substrate | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID106868 | Compound was tested for antiproliferative activity against human MKN45 cancer cell lines | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
AID1401634 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1630624 | Inhibition of full length recombinant human HDAC11 expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID1881883 | Activation of PKM2 (unknown origin) Leu353, Glu397, Phe26, Gly315 residues | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| A Perspective on Medicinal Chemistry Approaches for Targeting Pyruvate Kinase M2. |
AID764209 | Partition coefficient, log D of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID695598 | Inhibition of HDAC assessed as induction of p21 promoter expression by cell-based assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
| Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases. |
AID541656 | Growth inhibition of human HCT116 cells after 48 hrs by SRB assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID269915 | Selectivity for HDAC6 over HDAC4 | 2006 | Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
| Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. |
AID769930 | Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1182188 | Inhibition of mouse HDAC6 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors. |
AID1246516 | Inhibition of HDAC7 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID350025 | Increase in semaphoring 3F mRNA expression in human NCI-H661 cells at 300 nM by qRT-PCR relative to control | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression. |
AID538413 | Selectivity index, ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC6 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
| Inhibitors selective for HDAC6 in enzymes and cells. |
AID503527 | Inhibition of HDAC in human GM15850 cells assessed as increase in histone H3 lysine 9 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1390224 | 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 | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors. |
AID1246509 | Inhibition of HDAC3 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1557983 | Selectivity index, ratio of IC50 for 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 prei | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
| Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models. |
AID769920 | Induction iof GAP-43 protein expression in rat PC12 cells after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID568152 | Inhibition of HDAC3 by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID1431814 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1586079 | Inhibition of human HDAC3 using RHKKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1431816 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID1781509 | Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9
| Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from |
AID1623248 | Inhibition of HDAC in HEK293 cells assessed as increase in histone H3 acetylation at Lys27 residues at 10 uM incubated for 24 hrs by Western blot analysis relative to control | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | The P-glycoprotein inhibitor diltiazem-like 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxadiazolo[3,4-c][1,4]thiazin-3-one inhibits esterase activity and H3 histone acetylation. |
AID1431820 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID103356 | Inhibitory concentration required to reduce MCF-7 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID756021 | Inhibition of HDAC8 (unknown origin) after 30 mins by fluorometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID1518779 | Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID1863439 | Inhibition of HDAC7 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1401627 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1173705 | Inhibition of HDAC1 (unknown origin) after 15 mins by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Aurones as histone deacetylase inhibitors: identification of key features. |
AID723465 | Inhibition of human HDAC2 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID1605953 | Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1155322 | Selectivity index, ratio of IC50 for erythrocytes (unknown origin) to IC50 for Plasmodium falciparum | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID764210 | Selectivity ratio of IC50 for human recombinant HDAC4 to human recombinant HDAC6 | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID208533 | Concentration of compound required for acetylation of histone-4 in human T24 cancer cells | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
| Design and synthesis of a novel class of histone deacetylase inhibitors. |
AID1781511 | Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9
| Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from |
AID708216 | Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. |
AID1882462 | Inhibition of HDAC6 (unknown origin) | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
| Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology. |
AID1155321 | Cytotoxicity against erythrocytes (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1371070 | Antiparasitic activity against tachyzoite stage of Toxoplasma gondii | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1401592 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1556848 | Inhibition of HDAC8 (unknown origin) using R-H-K(Ac)-K(Ac)-AFC as substrate at 10 uM by fluorescence based assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Selenocoumarins as new multitarget antiproliferative agents: Synthesis, biological evaluation and in silico calculations. |
AID302799 | Inhibition of mouse recombinant HDAC6 expressed in 293 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. |
AID456800 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID1628756 | Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1401635 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID695594 | Inhibition of HDAC4 by fluorimetric assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
| Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases. |
AID1401607 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1765328 | 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 assa | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID620532 | Reactivation of MeCp2 mutant expression in human GM11272 cells at 1 to 100 nM by PCR method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Clonal Rett Syndrome cell lines to test compounds for activation of wild-type MeCP2 expression. |
AID541645 | Inhibition of human HDAC2 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1354394 | Inhibition of HDAC8 (unknown origin) by ELISA | | | |
AID488276 | Inhibition of HDAC6 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1529531 | Antiproliferative activity against human U87 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1384766 | Selectivity index, ratio of IC50 for human HDAC3 to IC50 for human HDAC6 | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID1628754 | Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1529529 | Antiproliferative activity against human K562R cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID621738 | Antiproliferative activity against human HCT116 cells by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| 2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors. |
AID488274 | Inhibition of HDAC2 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1390227 | Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B-based colorimetric assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors. |
AID91803 | Cytotoxicity of compound against normal human ovarian JAM cell line | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
| Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. |
AID1236450 | Inhibition of human HDAC6 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1901147 | 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 | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID524995 | Inhibition of HDAC10 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1885254 | Inhibition of KDM4E (unknown origin) | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
AID1833069 | Selectivity ratio of IC50 for recombinant C-terminal His-fusion tagged/N-terminal Strep2 tagged human HDAC8 (1 to 377 residues) expressed in insect cells to IC50 full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected S | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID242600 | Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 12a | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID1390225 | Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B-based colorimetric assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors. |
AID1371053 | Antitrypanosomal activity against Trypanosoma brucei brucei measured after 22 hrs by fluorescence-based Alamar blue viability assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1401606 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1459974 | Inhibition of recombinant human HDAC10 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1236444 | Inhibition of human HDAC3 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1765325 | 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 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID408883 | Inhibition of HDAC8 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID568156 | Inhibition of HDAC assessed as increase of histone H3 acetylation | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID316888 | Inhibition of HDAC from human SNU16 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID408881 | Inhibition of HDAC2 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID1155340 | Inhibition of HDAC in Plasmodium falciparum 3D7 trophozoites assessed as histone H3 hyperacetylation level at 500 nM after 3 hrs by Western blotting analysis relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1901070 | Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma SCr concentration at 10 mg/kg/day, ip | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1862611 | Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1781508 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9
| Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from |
AID269911 | Inhibition of HDAC1 | 2006 | Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
| Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. |
AID1322066 | Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID1578488 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID1628762 | Antiproliferative activity against human MDA-MB-231 cells by WST8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1322067 | Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID1210100 | Induction of Sp1 (GC>TA) mutant recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1156705 | Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID764208 | Intrinsic aqueous solubility of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2). |
AID331617 | Inhibition of human HDAC6 expressed in 293T cells | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells. |
AID344918 | Inhibition of 2-oxoglutarate-dependent human JMJD2E preincubated for 30 mins by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
AID1622993 | Antiproliferative activity against human SKBR3 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID525022 | Inhibition of HDAC in human CFBE41o- cell line assessed as increase in total CFTR protein level including CFTR glycoform at 0.1 uM by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1690113 | Selectivity index, ratio of IC50 for recombinant human HDAC8 to IC50 for recombinant human HDAC6 | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID1622971 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID414980 | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. |
AID1384206 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease. |
AID1690111 | Selectivity index, ratio of IC50 for recombinant human C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells to IC50 for recombinant human HDAC6 | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID1623249 | Inhibition of HDAC in human HepG2 cells assessed as increase in histone H3 acetylation at Lys27 residues at 10 uM incubated for 24 hrs by Western blot analysis relative to control | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | The P-glycoprotein inhibitor diltiazem-like 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxadiazolo[3,4-c][1,4]thiazin-3-one inhibits esterase activity and H3 histone acetylation. |
AID81709 | Inhibitory concentration against human colon cancer HCT116 cell proliferation | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID1895827 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020). |
AID1591715 | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
AID1651333 | 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 | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID208400 | Inhibitory concentration required to reduce T24 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID90211 | Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
| Heterocyclic ketones as inhibitors of histone deacetylase. |
AID90673 | Inhibitory activity against histone deacetylases (HDAC1) prepared from mouse melanoma B16/BL6 cells | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand. |
AID1853419 | Inhibition of human MMP-14 at 0.5 uM | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID411793 | Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg of protein | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC-MS/MS validation. |
AID1853414 | Inhibition of human MMP-1 at 0.5 uM | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID1260637 | Inhibition of human recombinant HDAC1 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID1605951 | Inhibition of human PI3Kgamma assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1605945 | 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 | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1173706 | Inhibition of HDAC2 (unknown origin) after 15 mins by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Aurones as histone deacetylase inhibitors: identification of key features. |
AID1401623 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1605946 | Inhibition of HDAC9 (unknown origin) using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID302801 | Selectivity for human HDAC6 over human HDAC4 | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. |
AID566558 | Inhibition of HDAC in human LNCAP cells at 1 uM after 10 mins by fluorometric assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
| Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells. |
AID487227 | Inhibition of recombinant HDAC6 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID385439 | Effect on TNF-alpha-induced NF-kappaB activation in HUVEC preincubated for 4 hrs assessed as increase in p65 level after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1210103 | Induction of acetylated histone H4 recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by ChIP assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID769929 | Selectivity index, ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC6 | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID102520 | Inhibitory concentration against lung A549 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1863440 | Inhibition of HDAC8 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1423498 | Inhibition of full length SIRT6 (unknown origin) using acetylated H3K9 peptide as substrate after 2 hrs in presence of NAD | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development. |
AID316885 | Antiproliferative activity against human A549 cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID516283 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH754 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID449704 | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
| In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. |
AID1156701 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID420329 | Inhibition of HDAC from RT extract | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases. |
AID541650 | Inhibition of human HDAC7 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1847754 | Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition by SRB assay | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
AID628432 | Inhibition of human recombinant HDAC7 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID568151 | Inhibition of HDAC2 by fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID417653 | Inhibition of human HDAC10 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID331615 | Inhibition of human HDAC1 expressed in 293T cells | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells. |
AID628437 | Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID1578486 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID240719 | Inhibition of human histone deacetylase 6 prepared from 293T cells | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones. |
AID241474 | Inhibitory concentration against maize histone deacetylase 2 | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. |
AID1901067 | Antiproliferative activity against human HK-2 cells assessed as decrease in cell viability at 0.78 uM measured after 24 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1394893 | Selectivity index, ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID541649 | Inhibition of human HDAC5 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1862616 | Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1628747 | Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1394890 | Inhibition of human HDAC3 using RHKK(Ac) as substrate | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1155320 | Antimalarial activity against Plasmodium falciparum infected in erythrocytes after 2 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
AID1651335 | 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 | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID1622967 | Inhibition of recombinant human HDAC4 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1765330 | Selectivity index, ratio of IC50 for human recombinant full length HDAC3 to IC50 for human recombinant full length HDAC2 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID324536 | Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID384317 | Inhibition of maize histone deacetylase 1A | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies. |
AID516298 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate H0058-1-818 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID525030 | Inhibition of HDAC7 in human CFBE41o- cell line assessed as correction of mutant Fdelta508 CFTR trafficking to cell surface as glycoform at 0.1 uM by Immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1236445 | Inhibition of human HDAC8 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1280317 | Inhibition of human KDAC8 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1651334 | Inhibition of human HDAC6 using fluorogenic-(RHKKAc) as substrate by fluorescence assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID81711 | Concentration required to inhibit the HCT116 cell growth by 50%. | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
| Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1432956 | Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors. |
AID316881 | Inhibition of human MM96L cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1441632 | Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
AID503525 | Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 16 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID254794 | Inhibitory concentration against histone deacetylase 6 | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| Design and synthesis of phthalimide-type histone deacetylase inhibitors. |
AID44724 | Inhibitory concentration against bladder T24 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID1479820 | Inhibition of recombinant human N-terminal His-tagged HDAC11 (1 to 347 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID417650 | Inhibition of human HDAC7 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID1280316 | Inhibition of human KDAC6 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
AID1758521 | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using [RHKK(Ac)] fluorogenic substrate | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID723463 | Inhibition of human HDAC5 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID769931 | Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1371054 | Inhibition of recombinant Trypanosoma brucei HDAC1 at 5 uM after 30 mins | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1702066 | Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID1628749 | Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1605944 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID90515 | Effective concentration in histone deacetylases (HDAC) using p21 promoter assay | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand. |
AID252220 | Average fold change in expression of CYP1A1 after treatment with compound of concentration 0.1 mM in human MCF-7 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells. |
AID1503589 | Inhibition of HDAC in human HN13 cells assessed as reduction in histone H3 Lys9 acetylation incubated for 24 hrs by immunofluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Serendipitous discovery of potent human head and neck squamous cell carcinoma anti-cancer molecules: A fortunate failure of a rational molecular design. |
AID80246 | Inhibitory activity against HCT116 human colon cell growth | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824). |
AID384316 | Inhibition of maize histone deacetylase 1B | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies. |
AID1586083 | Inhibition of human HDAC8 using RHKAcKAc as substrate by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
AID1690110 | Inhibition of recombinant human HDAC8 using RHK-K(Ac)-AMC as substrate by fluorescence based assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID385469 | Inhibition of TNF-alpha-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID302798 | Inhibition of human recombinant HDAC4 expressed in 293 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. |
AID506770 | Displacement of [3H]probe from SAP130 in human WiDr cell immunoprecipitate sample assessed as radioactive intensity at 500 nM after 1 hr by scintillation counting relative to control | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Splicing factor SF3b as a target of the antitumor natural product pladienolide. |
AID1605947 | 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 | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1635107 | Upregulation of HDAC1 inhibition/ERK signalling activation-mediated extracellular SOD mRNA expression in human THP1 cells at 1 uM after 24 hrs by RT-PCR method | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4
| Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells. |
AID90666 | Inhibitory activity on partially purified recombinant human Histone deacetylase 1 (HDAC-1) | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID461093 | Inhibition of HDAC6 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length. |
AID503526 | Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 8 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1459969 | Inhibition of recombinant human HDAC4 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID70208 | Inhibitory concentration against normal epithelial HMEC cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID385461 | Effect on LPS-induced wild type NF-kappaB-dependent ICAM1 promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of LPS challenge by luciferase reporter assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID240720 | Inhibition of human histone deacetylase 8 prepared from 293T cells | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones. |
AID506784 | Inhibition of SAP130 mediated cell growth in human WiDr cells | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Splicing factor SF3b as a target of the antitumor natural product pladienolide. |
AID1862620 | Inhibition of HDAC6 (unknown origin) measured by fluorometry assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID516299 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate H00581-1941 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID503694 | Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 12 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID447995 | Inhibition of human recombinant HDAC8 after 30 mins by fluorimetric assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides. |
AID254792 | Inhibitory concentration against histone deacetylase 2 | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| Design and synthesis of phthalimide-type histone deacetylase inhibitors. |
AID1236446 | Inhibition of human HDAC4 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID299649 | Increase in protein disulfide isomerase level in HEK293 cells at 600 nM by immunoblot | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition. |
AID1622919 | Inhibition of recombinant full-length human HDAC8 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID465149 | Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1605957 | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 h | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1273502 | Inhibition of HDAC in human HeLa cell nuclear extract using BML-KI104 Fluor de Lys as substrate by fluorescence-based assay | 2015 | Journal of natural products, Dec-24, Volume: 78, Issue:12
| Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors. |
AID541653 | Inhibition of human HDAC10 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1401628 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1294971 | Inhibition of human recombinant HDAC10 using RHK-K(Ac)-AMC as substrate | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID316891 | Inhibition of HDAC | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1210094 | Increase in NATa promoter activity in human HeLa cells at 0.5 uM after 24 hrs by qPCR method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID503682 | Inhibition of HDAC in human GM15850 cells assessed as increase in histone H3 lysine 14 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID541652 | Inhibition of human HDAC6 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1401639 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID90835 | Inhibitory activity against histone deacetylase 6 prepared from mouse melanoma B16/BL6 cells | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand. |
AID488273 | Inhibition of HDAC1 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID461095 | Inhibition of HDAC4 assessed as induction of p21 promotor activity by cell based assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length. |
AID611686 | Inhibition of N terminal hexahistidine-tagged human HDAC8 expressed in Sf9 cells after 1 hr by fluorescence assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors. |
AID1847752 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by SRB assay | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
AID367237 | Inhibition of human recombinant histone deacetylase 2 | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID1401610 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID695592 | Inhibition of HDAC1 by fluorimetric assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
| Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases. |
AID360095 | 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 | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID90208 | Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives. |
AID755997 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Lhx1 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID1853415 | Inhibition of human MMP-2 at 0.5 uM | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID90675 | In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
| Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation. |
AID1628752 | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1532642 | Selectivity ratio of IC50 for human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) to IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID78390 | Inhibitory concentration required to reduce H446 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID331618 | Induction of p21 expression in human HeLa cells after 24 hrs | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells. |
AID1401594 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1622994 | Antiproliferative activity against human MKN45 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID516288 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B5788 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID90690 | In vitro for anti-HD2 (Histone deacetylase 2) activity in maize | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
| Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation. |
AID269913 | Inhibition of HDAC6 | 2006 | Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
| Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. |
AID1182187 | Inhibition of human HDAC4 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors. |
AID302797 | Inhibition of human recombinant HDAC1 expressed in NIH3T3 cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. |
AID1628745 | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID161227 | Inhibitory concentration against prostate DU145 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID525020 | Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 1 uM by immunoblot analysis | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID769924 | Induction of neurite outgrowth in human SH-SY5Y cells at 10 uM after 5 days | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID488275 | Inhibition of HDAC3 | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| On the inhibition of histone deacetylase 8. |
AID1656945 | Mixed-type of inhibition of mushroom tyrosinase using varying level of L-DOPA as substrate by Dixon plot analysis | | | |
AID274171 | Antiproliferative activity against HCT116 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Synthesis of rigid trichostatin A analogs as HDAC inhibitors. |
AID1401629 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID496808 | Activity of human HDAC8 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID465150 | Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID769914 | Inhibition of HDAC6 in rat PC12 cells assessed as acetylation of histone H3 at 10 uM after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID628433 | Inhibition of human recombinant HDAC6 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID1210101 | Induction of Sp1 recruitment to NATb promoter in human HeLa cells nuclear extracts at 0.5 uM after 24 hrs by EMSA method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1622970 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1862614 | Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1690112 | Selectivity index, ratio of IC50 for recombinant human HDAC3 to IC50 for recombinant human HDAC6 | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID760390 | Inhibition of human recombinant HDAC1 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
| Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID90521 | Inhibitory activity against histone deacetylase (HDAC) | 2003 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
| Amide analogues of TSA: synthesis, binding mode analysis and HDAC inhibition. |
AID1529526 | Inhibition of human recombinant HDAC11 after 30 mins using fluorogenic substrate by fluorimetric assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID670029 | Inhibition of HDAC1 in human MCF7 cells assessed as up-regulation of acetylated histone H3 protein level at 0.5 uM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets. |
AID90701 | Inhibition of Histone deacetylase 4 in mammalian cells | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID1915533 | Agonist activity at Vitamin D receptor (unknown origin) by fluorescence polarization assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID417648 | Inhibition of human HDAC5 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID385463 | Inhibition of TNFalpha induced wild type TFkappaB-dependent tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of TNFalpha challenge by luciferase reporter assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1628757 | Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID465153 | Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1424816 | Inhibition of human recombinant HDAC6 using RHKKAcAMC as substrate by fluorescence assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors. |
AID769916 | Inhibition of HDAC6 in rat PC12 cells assessed as induction of alpha-tubulin acetylation at 10 uM after 48 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1628753 | Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1324227 | Inhibition of HDAC2 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
AID1294969 | 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 | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1421931 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID525001 | Inhibition of HDAC2 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1833066 | 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 | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID1605938 | 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 flu | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1690108 | Inhibition of recombinant human HDAC3 using RHK-K(Ac)-AMC as substrate by fluorescence based assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. |
AID385460 | Effect on TNF-alpha-induced wild type NF-kappaB-dependent ICAM1 promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of TNFalpha challenge by luciferase reporter assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1394895 | Selectivity index, ratio of IC50 for human HDAC8 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1431819 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID600531 | Inhibition of HDAC in human HL60 cells assessed as increase in histone H3 acetylation at 20 ug/ml after 24 hrs by Western blot analysis | 2009 | Journal of natural products, Jul, Volume: 72, Issue:7
| Cytotoxic triterpenoids from the stems of Microtropis japonica. |
AID1529524 | Inhibition of human recombinant HDAC6 after 30 mins using fluorogenic substrate by fluorimetric assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID309969 | Inhibition of mouse HDAC6 expressed in 293T cells | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. |
AID1863441 | Inhibition of HDAC9 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1401638 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1254047 | Inhibition of HDAC1 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation. |
AID723730 | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID1532631 | 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 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID447993 | Inhibition of human recombinant HDAC1 after 30 mins by fluorimetric assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides. |
AID1479813 | Inhibition of recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in baculovirus-infected insect cells using RHK(Ac)K(Ac)AMC as substrate after 60 mins by fluorimeter | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID1322068 | Selectivity index, ratio of IC50 for HDAC1 in human SHSY5Y cells to IC50 for HDAC6 in human SHSY5Y cells | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID1441630 | Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA preincubated for 10 mins followed by substrate addition measured after 10 mins | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
AID273990 | Inhibition of HDAC1 | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
| Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor. |
AID1384764 | Selectivity index, ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID302800 | Selectivity for human HDAC6 over human HDAC1 | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. |
AID1432957 | Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay | 2017 | ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
| Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors. |
AID1862610 | Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1863442 | Inhibition of HDAC10 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID449706 | NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested. | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
| In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. |
AID1446915 | Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy. |
AID324910 | Inhibition of human HDAC1 assessed as histone hyperacetylation in human HCT116 cells by Western blot | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs). |
AID252218 | Average fold change in expression of CYP1A1 after treatment with compound of concentration 1 mM in human MCF-7 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells. |
AID254791 | Inhibitory concentration against histone deacetylase 1 | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| Design and synthesis of phthalimide-type histone deacetylase inhibitors. |
AID1635111 | Inhibition of HDAC1 in human THP1 cells assessed as increase in histone H3 acetylation level at 1 uM after 12 hrs by Western blot analysis relative to control | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4
| Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells. |
AID496805 | Inhibition of human HDAC5 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1266100 | Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates. |
AID1401611 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1354391 | Inhibition of human HDAC1 by ELISA | | | |
AID1656942 | Cytotoxicity against human A549 cells assessed as reduction in cell viability | | | |
AID90528 | Inhibition of histone deacetylase (HDAC) activity in HeLa cell nuclear extract | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides. |
AID769935 | Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1758523 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma. |
AID360097 | Inhibition of HOSCN-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of HOSCN challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID90359 | Concentration required for inhibition of histone deacetylase HD2 in vitro. | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| 3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity. |
AID269914 | Selectivity for HDAC6 over HDAC1 | 2006 | Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
| Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. |
AID496803 | Inhibition of human HDAC3 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID456798 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID756007 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Rex1 expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID1605941 | Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID385464 | Induction of PMA-induced wild type TFkappaB-dependent tissue factor promoter expression in HUVEC at 100 nM preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID90351 | Concentration required to inhibit human Histone deacetylase (HDAC) enzyme by 50% | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
| Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1529525 | Inhibition of human recombinant HDAC8 after 30 mins using fluorogenic substrate by fluorimetric assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID408880 | Inhibition of HDAC1 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID408884 | Inhibition of HDAC10 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
AID1276711 | Inhibition of recombinant human HDAC1 by fluorimetry | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors. |
AID1630619 | Inhibition of recombinant C-terminal His-tagged/N-terminal GST-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID456797 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID628430 | Inhibition of human recombinant HDAC10 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID1853422 | Inhibition of human HDAC8 at 0.5 uM by fluorometric method | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID503693 | Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 5 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID90522 | Inhibitory concentration against rat liver Histone deacetylase | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID516291 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B3939 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1324228 | Inhibition of HDAC3 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
AID90687 | Inhibitory concentration against maize Histone deacetylase 2 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID273167 | Inhibition of maize HD1A | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID242687 | Inhibitory concentration against human histone deacetylase (HDAC) from HeLa cells with substrate 5a | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID313187 | Inhibition of HDAC6 expressed in 293T cells | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides. |
AID756022 | Inhibition of HDAC1 (unknown origin) after 30 mins by fluorometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID385442 | Increase in acetylated histone H3 level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blot | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1236448 | Inhibition of human HDAC7 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID760389 | Inhibition of human recombinant HDAC2 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
| Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID1294965 | Inhibition of human recombinant N-terminal GST-tagged C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID302099 | Antiproliferative activity against H661 cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
| Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues. |
AID1833067 | Selectivity ratio of IC50 for full length recombinant C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf21 insect cells to IC50 for full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 in | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2. |
AID1210102 | Induction of Sp1 recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by ChIP assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID525003 | Inhibition of HDAC1 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID80076 | Inhibitory activity against H1299 human lung carcinoma cell growth | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824). |
AID308645 | Inhibition of human HDAC6 | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
| Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. |
AID90688 | Inhibitory activity against maize Histone deacetylase 2 at 1 mM | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID358670 | Induction of REST/NRSF-coupled repression of luciferase tagged rat RE1/NRSE BDNF promoter activity expressed in ST14A cells assessed as increase in luciferase activity | 2007 | The Journal of biological chemistry, Aug-24, Volume: 282, Issue:34
| Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators. |
AID243634 | In vitro inhibition against human Histone deacetylase | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors. |
AID1254048 | Inhibition of HDAC6 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
| New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation. |
AID1127325 | Inhibition of human HDAC4 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1322065 | Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID1182189 | Ratio of IC50 for mouse HDAC6 to IC50 for human HDAC1 | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors. |
AID650228 | Inhibition of HDAC2 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
| Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain. |
AID1431821 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID90696 | Inhibition of maize histone deacetylase 2 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies. |
AID417652 | Inhibition of human HDAC9 | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
| N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. |
AID1322062 | Selectivity index, ratio of IC50 for human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant HDAC6 expressed in baculovirus infected insect cells | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID1401599 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1156699 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID541651 | Inhibition of human HDAC9 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID516285 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH535 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID500916 | Inhibition of heat-induced AML1-ETO protein expression in heterozygous transgenic zebrafish embryo at 0.5 uM by Western blot analysis | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation. |
AID1530556 | Inhibition of recombinant human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by homogeneous fluorescence release assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID1630620 | Inhibition of recombinant C-terminal His-tagged human HDAC5 catalytic domain (656 to 1122 residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity. |
AID447991 | Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorimetric assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides. |
AID309971 | Selectivity for human HDAC4 over human HDAC1 | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. |
AID1423499 | Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins by fluorescence-based SDS-denaturation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development. |
AID1293871 | Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 200 nM after 24 hrs by fluorescence microscopy | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID525000 | Inhibition of HDAC4 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID708214 | Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. |
AID605940 | Antifungal activity against Saccharomyces cerevisiae ATCC 9763 by microdilution method | 2011 | Journal of natural products, May-27, Volume: 74, Issue:5
| Microbial transformation of trichostatin A to 2,3-dihydrotrichostatin A. |
AID367240 | Selectivity ratio of IC50 for human recombinant histone deacetylase 2 to IC50 for human recombinant histone deacetylase 6 | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID414981 | Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. |
AID524994 | Inhibition of HDAC9 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID242561 | Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 5a | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID1401631 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1529564 | Antiproliferative activity against human HT-29 cells in presence of isoCA-4 after 72 hrs by MTS assay relative to control | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1294968 | 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 | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID360092 | 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 | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1622969 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID775831 | Inhibition of HDAC2 (unknown origin)-mediated deacetylation at 10 uM preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Investigating the selectivity of metalloenzyme inhibitors. |
AID274170 | Antiproliferative activity against H1299 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Synthesis of rigid trichostatin A analogs as HDAC inhibitors. |
AID201624 | Compound was tested for antiproliferative activity against human SK-BR-3 cancer cell lines | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
AID1622972 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID519602 | Antimalarial activity against Plasmodium falciparum infected in O+ human erythrocytes assessed as reduction in parasites at schizonts stage at 200 nM after 48 hrs by Giemsa staining based microscopy | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1659230 | Inhibition of human HDAC1 | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
| Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6. |
AID723479 | Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID385456 | Effect on TNF-alpha-induced SP1 protein level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1294963 | 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 | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID755481 | Inhibition of recombinant human HDAC1 using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID1651338 | Selectivity ratio of IC50 for recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells to IC50 of human HDAC6 | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
AID1635110 | Inhibition of HDAC1 in human THP1 cells assessed as increase in histone H4 acetylation level at 1 uM after 12 hrs by Western blot analysis relative to control | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4
| Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells. |
AID463865 | Inhibition of human HDAC in human HeLa cell nuclear extract after 15 mins by colorimetric assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors. |
AID80247 | Inhibitory concentration required to reduce HCT 116 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID1622917 | Inhibition of recombinant full-length human HDAC2 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID273173 | Inhibition of mouse HDAC1 | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1605943 | 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 | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID628436 | Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
AID1530557 | Inhibition of recombinant human HDAC6 using RHK-K(Ac) as substrate by homogeneous fluorescence release assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID1246517 | Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID226263 | Fold selectivity for classI HDAC | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID1652187 | Inhibition of human recombinant HDAC1 using fluorogenic substrate incubated for 30 mins by fluorescence based assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
AID1863435 | Inhibition of HDAC3 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1595396 | Inhibition of HDAC in human HeLa nuclear extract assessed as enzyme residual activity at 5 nM using Boc-Lys(acetyl)-AMC as substrate and measured after 15 mins by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability. |
AID1459968 | Inhibition of recombinant human HDAC3 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID516297 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH771 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID239792 | Selectivity for class I HDACs as ratio of IC50 for maize histone deacetylase 1-A and 1-B | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. |
AID43462 | Inhibitory concentration against breast MDA-MB-231 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID496809 | Inhibition of human HDAC9 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID456801 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
AID516289 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B5763 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1246514 | Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID524822 | Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 0.1 uM | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID760386 | Inhibition of human recombinant HDAC6 by Michaelis-Menten equation analysis | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
| Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors. |
AID366641 | Inhibition of HDAC2 after 17 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. |
AID1518781 | Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
AID367235 | Induction of alpha tubulin acetylation in human T24 cells | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID525035 | Inhibition of CFTR transcription assessed as decrease of CFTR protein level at 50 uM by immunoblot method | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID1454738 | Decrease in alcohol intake in rat assessed as ethanol intake at 2 mg/kg, ip administered daily during last 3 days of 10 day period of two-bottel choice paradigm (Rvb = 7 g/kg) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD). |
AID1765327 | 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 | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles. |
AID1473143 | 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 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
| (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
AID385458 | Inhibition of TNF-alpha-induced p65 binding to TFkappaB in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by chromatin immunoprecipitation assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID71776 | Tested in vivo for the inhibition of proliferation of friend leukemic cells | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
| Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells. |
AID350022 | Inhibition of HDAC in human NCI-H661 cells assessed as induction of alpha-tubulin acetylation at 300 nM after 6 hrs by Western blot analysis | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression. |
AID1431812 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
AID242586 | Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 5b | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Subtype selective substrates for histone deacetylases. |
AID83150 | Inhibitory concentration required to reduce normal human epithelial cell line (HMEC), growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID755478 | Inhibition of recombinant human HDAC4 using acetyl-Lys-(trifluoroacetyl)-AMC as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID1702069 | Inhibition of N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID1605960 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1125 residues) expressed in baculovirus infected insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence as | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1605961 | Inhibition of recombinant C-terminal His-fusion tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHK(Ac)K(Ac)AMC) as substrate measured after 1 to | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1293876 | Inhibition of HDAC in human HeLa nuclear extract assessed as accumulation of acetylated histone H3 after 24 hrs by western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID1901069 | Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma BUN concentration at 10 mg/kg/day, ip | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1532639 | 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 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID1589336 | Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors. |
AID1260646 | Inhibition of human recombinant HDAC10 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID1401596 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID524997 | Inhibition of HDAC7 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID313185 | Inhibition of HDAC1 expressed in 293T cells | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides. |
AID1628755 | Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1276713 | Inhibition of recombinant human HDAC8 by fluorimetry | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors. |
AID519709 | Antimalarial activity against Plasmodium falciparum infected in O+ human erythrocytes assessed as reduction in parasites at ring stage at 200 nM after 48 hrs by Giemsa staining based microscopy | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1354393 | Inhibition of HDAC3 (unknown origin) by ELISA | | | |
AID1401558 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID608776 | Inhibition of HDAC in human HeLa cells using Ac-Arg-Gly-Lys(Ac)-AMC as fluorescent substrate after 20 mins by fluorescence assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
| Structure-based optimization of click-based histone deacetylase inhibitors. |
AID50591 | Inhibitory concentration against colon SW48 cell line | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
AID274375 | Inhibition of SIRT2 in A549 cells assessed as ability to induce hyperacetylation of tubulin by Western blot analysis at 0.1 uM | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
| Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition. |
AID1578489 | 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 | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
AID1605949 | Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID516294 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate NIH34 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1628761 | Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1656943 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability | | | |
AID1702060 | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
| Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
AID461091 | Inhibition of HDAC1 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length. |
AID1901052 | Inhibition of HDAC in human HK-2 cells assessed as increase in histone H3 expression acetylation at 5 uM measured by western blot analysis | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID274169 | Antiproliferative activity against H661 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Synthesis of rigid trichostatin A analogs as HDAC inhibitors. |
AID1394894 | Selectivity index, ratio of IC50 for human HDAC3 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. |
AID1401603 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID90668 | Inhibitory concentration against recombinant human Histone deacetylase 1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID1210096 | Effect on NAT1 mRNA stability in human HeLa cells assessed as slope of mRNA decay curve at 0.5 uM after 24 hrs in presence of transcription inhibitor actinomycin D by qPCR method (Rvb = -0.78 +/- 0.02/hr) | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1401641 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID756009 | Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Nanog expression after 24 hrs by qPCR analysis | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity. |
AID90682 | Inhibition of in vitro enzyme activity measured in a highly purified maize Histone deacetylase 2 preparation | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
| Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells. |
AID487225 | Inhibition of recombinant HDAC2 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID1622926 | Inhibition of recombinant full-length human HDAC11 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
AID1628758 | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID1210098 | Induction of NATb Sp1 site in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID516282 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH200 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1529527 | Antiproliferative activity against human A549 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID316880 | Inhibition of mouse liver HDAC1 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID465151 | Inhibition of HDAC3 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID1529530 | Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID385453 | Decrease in thioglycolate-induced tissue factor activity in C57BL/6J mouse macrophage at 1 mg/kg, ip preincubated for 4 hrs assessed after 5 hrs of thioglycolate challenge by one stage clotting assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID367239 | Inhibition of human recombinant histone deacetylase 8 | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID516290 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH198 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1421930 | Antiplasmodial activity against Plasmodium falciparum | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
AID350021 | Inhibition of HDAC in human NCI-H661 cells assessed as induction of histone H4 acetylation at 300 nM after 6 hrs by Western blot analysis | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression. |
AID1210097 | Induction of NATb 3657 bp fragment upstream of exon 4 in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID1423500 | 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 | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development. |
AID1647301 | 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 b | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1246511 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID769934 | Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease. |
AID1384763 | Inhibition of human HDAC6 using RHKKAc peptide as substrate | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID385457 | Effect on TNF-alpha-induced Egr1 protein level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blotting | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID286454 | Inhibition of Histone deacetylase in HeLa cell nuclear extracts by fluorescence-based assay | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
| Design and synthesis of a potent histone deacetylase inhibitor. |
AID366645 | Inhibition of HDAC10 after 17 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. |
AID1260644 | Inhibition of human recombinant HDAC8 at 20 uM using Ac-RHK(Ac)K(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID382342 | Inhibition of human HDAC in HeLa cells by flour de lys assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
| Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group. |
AID503668 | Cytotoxicity against human GM15850 cells at 5 uM after 96 hrs by trypan blue exclusion assay | 2006 | Nature chemical biology, Oct, Volume: 2, Issue:10
| Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia. |
AID1236449 | Inhibition of human HDAC9 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID506769 | Displacement of [3H]probe from SAP130 in human WiDr cells assessed as radioactive intensity at 500 nM after 1 hr by scintillation counting relative to control | 2007 | Nature chemical biology, Sep, Volume: 3, Issue:9
| Splicing factor SF3b as a target of the antitumor natural product pladienolide. |
AID331616 | Inhibition of human HDAC4 expressed in 293T cells | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells. |
AID240718 | Inhibition of human histone deacetylase 4 prepared from 293T cells | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones. |
AID385441 | Increase in acetylated histone H4 level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blot | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID90672 | Inhibitory activity against maize Histone deacetylase 1-B | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
| Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A. |
AID1528345 | Inhibition of human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHKKAc as substrate | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
| Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6. |
AID541654 | Inhibition of human HDAC11 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID541644 | Inhibition of human HDAC1 by fluorimetric assay | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. |
AID1628759 | Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
| Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
AID519604 | Inhibition of HDAC in Plasmodium falciparum Dd2 infected in O+ human erythrocytes assessed as alteration of histone acetylation at 500 nM after 3.5 hrs by Westen blot | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID241538 | Inhibitory concentration against maize histone deacetylase 1-B (class I HDAC) | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. |
AID1294964 | Inhibition of human recombinant N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID1529562 | Antiproliferative activity against human HT-29 cells assessed as cell viability after 72 hrs by MTS assay relative to control | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
| Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4. |
AID1210090 | Increase in NAT1 enzyme activity in human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID273166 | Inhibition of maize HD2 | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors. |
AID1781510 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9
| Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from |
AID1387553 | Inhibition of HDAC in human HeLaS3 cells assessed as increase in histone H3K9 acetylation at 10 uM treated for 16 hrs followed by compound washout and measured up to 24 hrs by immunoblot analysis | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
| Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors. |
AID487224 | Inhibition of recombinant HDAC1 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID723461 | Inhibition of human HDAC8 by fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. |
AID1441631 | 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 | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
AID1401625 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID516287 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B4506 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1525777 | Inhibition of HADC1 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
| Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. |
AID1459953 | Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID1322059 | Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa nuclear extracts using MAL as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
AID1401604 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1647309 | 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 | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. |
AID1294966 | Inhibition of human recombinant C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID385440 | Effect on TNF-alpha-induced NF-kappaB activation in HUVEC preincubated for 4 hrs assessed as increase in c-Rel level after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1294961 | Inhibition of HDAC1 in human HeLa cells assessed as hyperacetylation of histone H3 at 2 uM incubated for 24 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
AID385459 | Inhibition of TNF-alpha-induced p65 binding to ICAM1 NF-kappaB in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by chromatin immunoprecipitation assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID544397 | Inhibition of Plasmodium falciparum 3D7 histone deacetylase infected in human erythrocytes assessed as alteration of histone H3 acetylation at 100 nM after 3.5 hrs by SDS-PAGE | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
| Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
AID1246513 | Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID496801 | Inhibition of human HDAC1 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID465152 | Inhibition of HDAC8 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. |
AID519583 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Potent antimalarial activity of histone deacetylase inhibitor analogues. |
AID1764798 | Inhibition of class1 HDAC in mouse Neuro2a cells assessed as fold increase in ratio of acetylated histone H3 to histone H4 at 1 uM incubated for overnight by Western blot analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model. |
AID1156702 | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID385444 | Effect on TNF-alpha-induced TFkappaB activation assessed as p65/c-Rel binding to TFkappaB in HUVEC preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID1401637 | Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1532629 | 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 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
AID201882 | Inhibitory concentration required to reduce SW48 tumor cell growth by 50% in MTT assay | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
AID1605958 | Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay relative t | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1441699 | Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
AID568157 | Inhibition of HDAC assessed as increase of histone H4 acetylation | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors. |
AID1390223 | 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 | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors. |
AID1862622 | Inhibition of HDAC11 (unknown origin) measured by fluorometry assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID80362 | In vitro antiproliferative activity against human colon cancer HCT 116 cells determined by MMT assay | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
| Design and synthesis of a novel class of histone deacetylase inhibitors. |
AID1659237 | Inhibition of human HDAC6 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
| Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6. |
AID1853416 | Inhibition of human MMP-3 at 0.5 uM | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID1384768 | Selectivity index, ratio of IC50 for human HDAC10 to IC50 for human HDAC6 | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
AID1177037 | Cytotoxicity against human U2OS cells after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909. |
AID1236447 | Inhibition of human HDAC5 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1459975 | Inhibition of recombinant human HDAC11 using fluorogenic substrate by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. |
AID90349 | Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
| Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors. |
AID1177039 | Cytotoxicity against human HeLa cells after 96 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909. |
AID90344 | Induction of p21 using Histone deacetylase inhibitors | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
| Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. |
AID1210093 | Increase in NATb promoter activity in human HeLa cells at 0.5 uM after 24 hrs by qPCR method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
| Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells. |
AID316883 | Selectivity index, ratio of IC50 for human MM96L cells to IC50 for human NFF cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Histone deacetylase inhibitors: from bench to clinic. |
AID1781513 | Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate incubated for 20 mins by fluorometric assay | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9
| Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from |
AID1401624 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID621737 | Inhibition of HDAC1 by fluorescent activity assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| 2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors. |
AID1127329 | Inhibition of human HDAC8 using fluorogenic tetrapeptide RHKKAc as substrate | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors. |
AID1853421 | Inhibition of human HDAC3 at 0.5 uM by fluorometric method | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| |
AID1525776 | Inhibition of HADC6 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
| Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. |
AID1605956 | Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
AID1479815 | 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 | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
AID1901146 | 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 | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors. |
AID360093 | 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 | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes. |
AID755475 | Inhibition of recombinant human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID500920 | Inhibition of Hsp70 expression in heterozygous transgenic zebrafish embryo at 0.5 uM by Western blot analysis | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation. |
AID366640 | Inhibition of HDAC1 after 17 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. |
AID516292 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH184 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1863436 | Inhibition of HDAC4 (unknown origin) by colorimetric method | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier. |
AID1423501 | 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 | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development. |
AID1156706 | Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
AID1423503 | Inhibition of human SIRT6 preincubated for 5 mins in presence of substrate followed enzyme addition measured after 5 to 10 mins in presence of NAD by fluorescence spectrophotometry | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
| Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development. |
AID1709384 | Selectivity index, ratio of IC50 for inhibition of recombinant human full-length C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 insect cells to IC50 for inhibition of recombinant human full-length N-terminal GST | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors. |
AID90519 | Inhibitory concentration against partially purified mouse histone deacetylase (HDAC) | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| Histone deacetylase inhibitors. |
AID421211 | Antitumor activity against mouse ML1 cells | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Recent advances in the development of polyamine analogues as antitumor agents. |
AID1401597 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID755479 | Inhibition of HDAC3/NCOR2 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Structural basis for the design and synthesis of selective HDAC inhibitors. |
AID1266099 | Inhibition of HDAC6 in human HeLa cells assessed as tubulin acetylation incubated for overnight by immunofluorescence microscopic analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates. |
AID1260645 | Inhibition of human recombinant HDAC9 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID384318 | Selectivity for IC50 of maize histone deacetylase 1B over IC50 of maize histone deacetylase 1A | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies. |
AID367238 | Inhibition of human recombinant histone deacetylase 6 | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors. |
AID496780 | Inhibition of shATP citrate lyase-induced cell differentiation in mouse C2C12 assessed as myosin heavy chain expression at 100 nM | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Carbon metabolism-mediated myogenic differentiation. |
AID1401609 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID241537 | Inhibitory concentration against maize histone deacetylase 1-A (class IIa HDAC) | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. |
AID516286 | Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate NIH257 at 64 ug/ml | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Heteroresistance of Cryptococcus gattii to fluconazole. |
AID1862609 | Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors. |
AID1845905 | Reversal of HIV-1 latency infected in human J-Lat Tat-GFP Clone A7 cells assessed as increase in GFP expressing cells at 100 nM incubated for 72 hrs by flow cytometry analysis relative to control | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
AID670035 | Inhibition of HDAC6 in human MCF7 cells assessed as change in tubulin acetylation level at 0.5 uM after 24 hrs by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets. |
AID1401560 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors. |
AID1202473 | Antiproliferative activity against human A549 cells assessed as shrunken and sharp shape at 0.4 uM after 24 hrs by phase contrast microscopy | 2015 | European journal of medicinal chemistry, , Volume: 96 | Efficient synthesis and biological activity of Psammaplin A and its analogues as antitumor agents. |
AID1354392 | Inhibition of human HDAC2 by ELISA | | | |
AID1530555 | Inhibition of recombinant human HDAC1 using RHK-K(Ac) as substrate by homogeneous fluorescence release assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID1260639 | Inhibition of human recombinant HDAC3 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay | | | |
AID447992 | Inhibition of HDAC in human HeLa cell cytosolic extract after 30 mins by fluorimetric assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides. |
AID524998 | Inhibition of HDAC5 by in vitro deacetylation assay | 2010 | Nature chemical biology, Jan, Volume: 6, Issue:1
| Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis. |
AID496804 | Inhibition of human HDAC4 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1802398 | Enzymatic HDAC Activity Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\ | 2013 | The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
| Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. |
AID1802451 | HDAC Cell-Free Assays from Article 10.1074/jbc.M113.472563: \\The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity.\\ | 2013 | The Journal of biological chemistry, Nov-22, Volume: 288, Issue:47
| The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity. |
AID1802399 | Proteros Reporter Displacement Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\ | 2013 | The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
| Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2008 | The Journal of biological chemistry, Apr-25, Volume: 283, Issue:17
| Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3
| High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
| Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID1346090 | Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346032 | Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346066 | Human histone deacetylase 5 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346134 | Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346104 | Human histone deacetylase 4 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346131 | Human histone deacetylase 7 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346068 | Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346077 | Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID1346082 | Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs)) | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3
| Chemical phylogenetics of histone deacetylases. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Inside HDAC with HDAC inhibitors. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 1999 | Nature, Sep-09, Volume: 401, Issue:6749
| Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 1999 | Nature, Sep-09, Volume: 401, Issue:6749
| Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |