| Assay ID | Title | Year | Journal | Article |
|---|
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC 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. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1384226 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 500 nM after 4 hrs by Western blot analysis relative to control | 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. |
| AID1406988 | Inhibition of HDAC6 in human U87 cells assessed as levels of alpha-tubulin acetylation at 1 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1783124 | Induction of apoptosis in human HL-60 cells assessed as necrotic cells at 3 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 0.017%) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1280318 | Inhibition of recombinant human KDAC3/NcoR2 using acetylated p53 (379 to 382 residues) as substrate by fluorescence assay | 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. |
| AID1406980 | Selectivity ratio of IC50 for human recombinant C-terminal His/FLAG-tagged full length HDAC1 to IC50 for N-terminal GST-tagged full length HDAC6 | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1572374 | Inhibition of recombinant human HDAC1 using RHKKAc fluorogenic peptide substrate | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1173506 | Inhibition of N-terminal GST-tagged human HDAC10 (1 to 481 residues) using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1864666 | Inhibition of recombinant HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1452867 | Inhibition of HDAC5 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1337280 | Antiproliferative activity against human Jurkat cells | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID748109 | Inhibition of HDAC6 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1572341 | Inhibition of recombinant C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1493600 | Inhibition of HDAC11 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| 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. |
| AID1587861 | Inhibition of dye-labeled tracer binding to HDAC6 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1493591 | Inhibition of human recombinant full-length HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1572342 | Inhibition of recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID655909 | Inhibition of human recombinant HDAC1 using RHKKAc peptide as substrate incubated for 5 to mins prior to substrate addition measured after 2 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1707495 | Synergistic antifungal activity against Candida albicans 9884 assessed as fluconazole MIC incubated for 48 hrs in presence of fluconazole by microdilution assay (Rvb = fluconazole alone MIC = >64 ug/ml) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1428512 | Cell cycle arrest in human HCT116 cells assessed as accumulation at sub-G1 phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1655374 | Free drug concentration in mouse brain at 25 mg/kg measured at 8 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1322063 | Effective passive permeability of the compound at 100 uM at pH 7.4 after 18 hrs by UHPLC-UV based PAMPA-BBB assay | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
| 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. |
| AID1202601 | Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation at 14 uM after 24 hrs by Western blotting analysis | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
| 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. |
| AID1337255 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1557975 | Induction of cell death in human T24 cells at 0.1 to 25 uM | 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. |
| AID1785337 | Inhibition of recombiant human HDAC6 using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1600730 | Inhibition of C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
| Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1707497 | Synergistic antifungal activity against Candida albicans 4108 assessed as fluconazole MIC incubated for 48 hrs in presence of fluconazole by microdilution assay (Rvb = fluconazole alone MIC = >64 ug/ml) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID772636 | Inhibition of human recombinant HDAC4 using acetyl-Lys(trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1418687 | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 to 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs coincubated with ebselen by MTT assay | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1384232 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level after 2 hrs by Western blot analysis | 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. |
| AID1587866 | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1617403 | Stability in human plasma assessed as parent compound remaining at 100 uM after 4 hrs by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| AID1879890 | Inhibition of recombinant human HDAC1 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
| AID1723744 | Selectivity index, ratio of IC50 for inhibition of human recombinant HDAC1 to IC50 for inhibition of human recombinant HDAC6 | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups. |
| AID1864735 | Inhibition of HDAC3 (unknown origin) | | | |
| AID1728672 | Inhibition of recombinant human HDAC8 using Fluor-de-Lys as substrate measured after 1 hr by fluorescence assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation. |
| AID772633 | Inhibition of human recombinant HDAC7 using acetyl-Lys(trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1401478 | Selectivity ratio of IC50 for HDAC2 in human HeLa-S3 cell lysates to IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1355724 | Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1294948 | Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 substrate assessed as remaining activity at 1 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1849157 | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
| Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
| AID1785345 | Inhibition of full length human CDK4 (1 to 303 residues)/N-terminal GST-fusion tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay | | | |
| AID1728673 | Selectivity ratio of IC50 for inhibition of recombinant human HDAC8 to IC50 for inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation. |
| AID1783109 | Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1476148 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1355699 | Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 5 uM after 48 hrs propidium iodide staining based flow cytometry | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID767950 | Inhibition of human recombinant HDAC5 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| 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). |
| 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. |
| AID1476183 | Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells at 10 uM using RHKKAc as substrate in presence of ATP | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1587860 | Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1864672 | Inhibition of recombinant HDAC9 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1384234 | Inhibition of PDE5 in human SH-SY5Y cells assessed as induction of phosphorylated CREB level at 500 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID1384218 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 4 hrs by AlphaLISA assay relative to control | 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. |
| AID1396958 | Antiproliferative activity against human MDA-MB-231 cells | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
| AID1418684 | Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based inverted fluorescence microscopic analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID767945 | Inhibition of human recombinant HDAC10 protein using RHKKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1864663 | Selectivity index, ratio of IC50 for recombinant HDAC1(unknown origin) to IC50 for full length recombinant human HDAC6 | | | |
| AID1452870 | Inhibition of HDAC8 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| 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. |
| AID767949 | Inhibition of human recombinant HDAC6 protein using RHKKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1655349 | AUC in CD-1 mouse at 3 mg/kg, iv | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1452872 | Inhibition of HDAC10 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1785334 | Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells measured after 30 mins by fluorescence microplate reader ass | | | |
| AID1459957 | Selectivity ratio of IC50 for recombinant human HDAC2 to IC50 for recombinant human HDAC6 | 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. |
| AID1679254 | Selectivity ratio of IC50 for human HDAC3/human NCOR2 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1406979 | Inhibition of human recombinant HDAC8 using fluor de Lys(R) as substrate after 90 mins by fluorescence-based assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1848583 | Inhibition of full length C-terminal his6-tagged human recombinant HDAC2 (1 to 488 residues) | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
| AID732154 | Inhibition of HDAC2 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1294947 | Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 as substrate incubated for 15 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. |
| AID1337299 | Inhibition of HDAC1/HDAC2/HDAC3 signalling in human MOLM14 cells assessed as increase in acetylated histone-3(Lys9/Lys14) level at 15 uM up to 48 hrs by immunoblot method | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1785332 | Inhibition of HDAC1 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1525778 | Inhibition of HADC2 (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. |
| AID767953 | Inhibition of human recombinant HDAC2 protein using RHKKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1452868 | Inhibition of HDAC6 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1655368 | Drug concentration in CD-1 mouse brain at 3 mg/kg, iv measured at 60 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1424823 | Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC6 | 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. |
| AID1587862 | Selectivity ratio of compound effect for inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells to compound effect for inhibition of dye-labeled tracer binding to HDAC6 (unknown origin) transfected in human HeL | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1819859 | Inhibition of full length human HDAC6 using FAM-labeled acetylated peptide as substrate by electrophoretic mobility shift assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
| Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype. |
| AID1600731 | Inhibition of C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins mea | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
| Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1452869 | Inhibition of HDAC7 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1655369 | Drug concentration in CD-1 mouse plasma at 3 mg/kg, iv measured at 8 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1339573 | Selectivity ratio of IC50 for HDAC2 in human HeLaS3 cells to IC50 for HDAC6 in human HeLaS3 cells | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1493598 | Inhibition of HDAC9 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1740089 | Inhibition of human full length recombinant HDAC8 using p53 (379 to 382 residues) (RHK(Ac)K(Ac)AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1845808 | Inhibition of HDAC11 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1845801 | Inhibition of HDAC3 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| 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. |
| AID1396961 | Antiproliferative activity against human MCF7 cells | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
| AID1572391 | Selectivity ratio of IC50 for recombinant human HDAC1 using RHKKAc fluorogenic peptide substrate to IC50 for recombinant human HDAC6 using RHKKAc fluorogenic peptide substrate | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1355690 | Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1452871 | Inhibition of HDAC9 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID772631 | Inhibition of human recombinant HDAC11 using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1679250 | Selectivity ratio of IC50 for human HDAC5 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1337298 | Inhibition of HDAC1/HDAC2/HDAC3 signalling in human KMS-12-BM cells assessed as increase in acetylated histone-3(Lys9/Lys14) level at 15 uM up to 48 hrs by immunoblot method | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1655363 | Inhibition of HDAC6 in mouse N2A cells | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1655355 | Oral bioavailability in CD-1 mouse at 30 mg/kg | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1322064 | Effective passive permeability of the compound assessed as membrane retention at 100 uM at pH 7.4 after 18 hrs by UHPLC-UV based PAMPA-BBB assay | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Synthesis of a selective HDAC6 inhibitor active in neuroblasts. |
| 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. |
| 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. |
| AID1785355 | Synergistic antiproliferative activity against human A549 cells assessed as combination index in presence of 2.5 to 46 uM palbociclib by Chou-Talalay method | | | |
| AID1249598 | Inhibition of recombinant human HDAC6 using RHKKAc as substrate by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators. |
| AID1401479 | Selectivity ratio of IC50 for HDAC3 in human HeLa-S3 cell lysates to IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1783136 | Inhibition of HDAC5 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID655912 | Immunosuppressive activity against C57BL/6 mouse CFSE-labelled effector T cells assessed as inhibition of T regulatory cells-mediated proliferation at Treg:Teff ratio of 1:1 at 1 uM after 3 to 4 days by flow cytometry (Rvb = 42.2%) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1764253 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
| AID1534436 | Inhibition of human full-length recombinant HDAC6 expressed in baculovirus infected Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer. |
| AID1864687 | Inhibition of HDAC6 in human MV4-11 cells assessed as decrease in accumulation of tubulin acetylation preincubated for 6 hrs followed by compound washout measured after 30 mins by western blot analysis | | | |
| 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. |
| AID1432959 | Inhibition of HDAC1 in HEK293 cells assessed as increase in histone H3 acetylation at 10 uM after 24 hrs by Western blot method | 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. |
| AID1864699 | AUC(0 to infinity) in CD-1 mouse at 3 mg/kg, iv measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1707463 | Potentiation of fluconazole-induced antimicrobial activity against Candida albicans assessed as fraction inhibitory concentration index incubated for 48 hrs by checkerboard microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID772635 | Inhibition of human recombinant HDAC6 using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| 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. |
| AID1384225 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 500 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID1783113 | Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1418691 | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with tubastatin A by DCFH-DA dye-based fluoresce | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1882271 | Selectivity ratio of IC50 for recombinant human HDAC8 to IC50 for recombinant human HDAC6 | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| AID1655366 | Efflux ratio of permeability in MDCK-MDR1 cells | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1493593 | Inhibition of human recombinant full-length C-terminal GST-tagged HDAC3 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1418679 | Neuroprotective activity against H2O2-induced toxicity in rat PC12 cells assessed as cell viability at 10 uM pretreated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1428503 | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using RHKK(Ac) as substrate after 90 mins by fluorimetric method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| 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. |
| AID1065961 | Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
| AID1449322 | Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1783122 | Induction of apoptosis in human HL-60 cells assessed as early apoptotic cells at 3 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 5.12%) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1280319 | Inhibition of recombinant human KDAC6 using acetylated p53 (379 to 382 residues) as substrate by fluorescence assay | 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. |
| AID1384210 | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | 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. |
| AID1723742 | Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups. |
| AID732144 | Inhibition of HDAC5 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1165110 | Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| AID1418670 | GPx-like activity of the compound assessed as velocity for H2O2 reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1452866 | Inhibition of HDAC4 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1655367 | Drug concentration in CD-1 mouse brain at 3 mg/kg, iv measured at 8 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1864671 | Inhibition of recombinant HDAC8 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1355728 | Antitumor activity against human HEL cells xenografted in BALB/C nude mouse assessed as tumor growth inhibition at 10 mg/kg, ip bid treated for 21 consecutive days relative to control | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1165104 | Antileishmanial activity against promastigote stage of Leishmania donovani after 72 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| AID1418695 | Cytotoxicity against rat PC12 cells at 20 uM in presence of ebselen after 24 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1384227 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 100 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID772637 | Inhibition of HDAC3/NcoR2 (unknown origin) using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1337254 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1707489 | Synergistic antifungal activity against Candida albicans 9172 incubated for 48 hrs in presence of fluconazole by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1845800 | Inhibition of HDAC2 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1339577 | Selectivity ratio of IC50 for HDAC3 in human HeLaS3 cells to IC50 for full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1558020 | Effect on cell viability in mouse SM1 cells up to 10 uM by ApoTox-Glo triplex assay | 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. |
| AID1655354 | AUC in CD-1 mouse at 30 mg/kg, po | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1723896 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to HDAC6 (unknown origin) | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models. |
| AID1384212 | Inhibition of full length human recombinant C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (95 to 489 residues) expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | 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. |
| AID1337196 | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1864708 | Inhibition of HDAC6/dynein interaction in mouse J774.A1 cells measured after 8 hrs by co-immunoprecipitation based Western blotting analysis | | | |
| AID1384219 | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells assessed residence time preincubated fopr 2 hrs followed by dilution and subsequent fluorogenic HDAC substrate 3 addition measured at | 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. |
| 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. |
| AID1655347 | Initial plasma concentration in CD-1 mouse at 3 mg/kg, iv measured at 0 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1587859 | Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1418689 | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by DCFH-DA dye-based fluorescence analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1355744 | In vivo antifungal activity against FLC resistant Candida albicans 0304103 infected in ICR mouse assessed as mouse survival at 5 mg/kg, ip qd up to 20 days in co-treated with 1 mg/kg, ip qd fluconazol (Rvb = 4.5 day) | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1617398 | Selectivity ratio of IC50 for C-terminal His/Flag tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells to IC50 for human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| AID1572375 | Inhibition of recombinant human HDAC6 using RHKKAc fluorogenic peptide substrate | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1493599 | Inhibition of HDAC10 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1406993 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as levels of alpha-tubulin acetylation at 5 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1452863 | Inhibition of HDAC1 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| 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. |
| AID1882269 | Inhibition of recombinant human HDAC8 using RHKAcKAc peptide as substrate | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| 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. |
| AID1065960 | Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
| AID1679258 | Inhibition of human HDAC6 using p53 fluorogenic peptide (379 to 382 residues) RHKKAc as substrate by fluorescence-based assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1917543 | Selectivity index, ratio IC50 for inhibition of HDAC8 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| 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. |
| AID1173497 | Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1864696 | Half life in CD-1 mouse at 30 mg/kg, po measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1572345 | Selectivity ratio of IC50 for recombinant human HDAC8 to IC50 for N-terminal GST-tagged human HDAC6 | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1384211 | Inhibition of full length human recombinant C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | 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. |
| AID1591719 | Inhibition of Class 1 histone deacetylase in human HeLa cells assessed as increase in histone acetylation at 0.1 to 10 uM after 24 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
| AID1065957 | Cytotoxicity against human Jurkat gamma1 cells assessed as growth inhibition at 20 uM after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
| 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. |
| 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. |
| AID1783107 | Inhibition of HDAC6 (unknown origin) using Ac-LeuGlyLy-s(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence microtiter plate reader assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID732145 | Inhibition of HDAC3 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1864665 | Inhibition of recombinant HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1882267 | Inhibition of recombinant human HDAC3/NcoR2 using RHKKAc peptide as substrate | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| AID1864669 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1449317 | Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1679256 | Selectivity ratio of IC50 for human HDAC2 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1449338 | Potentiation of cisplatin-induced cytotoxicity against human CAL27 cells assessed as decrease in cell viability at 10 uM preincubated for 48 hrs followed by cisplatin treatment measured after 72 hrs by MTT assay relative to cisplatin alone | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1726030 | Inhibition of human recombinant HDAC8 expressed in Escherichia coli using Fluor de Lys substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation. |
| AID1723895 | Inhibition of HDAC6 (unknown origin) | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models. |
| AID1785333 | Inhibition of HDAC2 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1384207 | Inhibition of HDAC2 (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. |
| AID1537555 | Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7
| Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
| 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. |
| AID1740087 | Inhibition of human full length recombinant HDAC2 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1655352 | Initial plasma concentration in CD-1 mouse at 30 mg/kg, po measured at 0 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1882265 | Inhibition of recombinant human HDAC1 using RHKKAc peptide as substrate | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| AID1785336 | Inhibition of HDAC5 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1165111 | Inhibition of HDAC6 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| AID1355746 | In vivo antifungal activity against FLC resistant Candida albicans 0304103 infected in ICR mouse assessed as mouse survival at 5 mg/kg, ip qd up to 20 days (Rvb = 4.5 day) | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1707487 | Antifungal activity against Candida albicans 4108 incubated for 48 hrs by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| 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. |
| AID655908 | Immunosuppressive activity against C57BL/6 mouse CFSE-labelled effector T cells assessed as inhibition of T regulatory cell-mediated proliferation at Treg:Teff ratio of 1:4 at 1 uM after 3 to 4 days by flow cytometry (Rvb = 74.2%) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1783111 | Antiproliferative activity against human KG-1 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1558049 | Induction of cell death in human 5637 cells at 0.1 to 25 uM | 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. |
| AID1401476 | Selectivity ratio of IC50 for HDAC3 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1572344 | Inhibition of recombinant human HDAC8 expressed in baculovirus expression system using fluorogenic Arg-His-Lys(Ac)-Lys(Ac) as substrate incubated for 90 mins by fluorescence assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1384215 | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 4 hrs fluorescence assay | 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. |
| 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. |
| AID1655350 | Volume of distribution at steady state in CD-1 mouse at 3 mg/kg, iv | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1355734 | Antitumor activity in human HEL cells xenografted in SCID mouse assessed as mouse survival time at 10 mg/kg, ip qd | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1401356 | Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 2 x 10'-5 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1337300 | Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1864734 | Inhibition of HDAC2 (unknown origin) | | | |
| AID1783112 | Antiproliferative activity against human HEL cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1783110 | Inhibition of HDAC8 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID772656 | Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC6 | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1424817 | Inhibition of human recombinant HDAC1 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. |
| AID1753628 | Neuroprotective activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as reduction in neurobehavioral defects at 25 mg/kg, ip after 24 hrs by TTC staining based assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
| AID1401344 | Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 1.6 x 10'-4 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| 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. |
| AID1655344 | Metabolic stability in mouse liver microsomes assessed as half life | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| 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. |
| AID655914 | Immunosuppressive activity against C57BL/6 mouse CFSE-labelled effector T cells assessed as inhibition of T regulatory cells-mediated proliferation at Treg:Teff ratio of 1:2 at 1 uM after 3 to 4 days by flow cytometry (Rvb = 64.8%) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1452873 | Inhibition of HDAC11 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| 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. |
| AID1406992 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as levels of alpha-tubulin acetylation at 1 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1785342 | Inhibition of recombinant human SIRT2 measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1294956 | Inhibition of recombinant human HDAC1 using Fluor de Lys-SIRT1 as substrate assessed as remaining activity at 1000 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1324255 | Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level measured after 24 hrs relative to control | 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. |
| AID1864702 | Oral bioavailability in CD-1 mouse at 30 mg/kg measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1280289 | Inhibition of recombinant human KDAC1 using acetylated p53 (379 to 382 residues) as substrate by fluorescence assay | 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. |
| AID1633995 | Therapeutic index, ratio of CC50 for human HuH7 cells to EC50 for antiviral activity against HCV infected in human HuH7-luc/neo cells assessed as inhibition of DNA replication i | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV). |
| AID1525780 | Inhibition of HADC8 (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. |
| AID1864681 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 0 min followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| 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. |
| AID1173495 | Inhibition of recombinant N-GST-tagged HDAC6 (unknown origin) assessed as reduction in deacetylation of Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1679251 | Selectivity ratio of IC50 for human HDAC7 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1384230 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID1864727 | Binding affinity to recombinant HDAC6 (unknown origin) assessed as inhibition constant using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1165112 | Inhibition of HDAC8 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| AID1355723 | Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1401502 | Cytotoxicity against human U937 cells assessed as cell viability at 80 uM after 44 hrs in presence of PCI-34051 by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1679255 | Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1785346 | Inhibition of full length human CDK6 (1 to 326 end residues)/N-terminal GST-fusion tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay | | | |
| AID1396959 | Antiproliferative activity against human HCT116 cells | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
| AID1707492 | Synergistic antifungal activity against Candida albicans 4108 incubated for 48 hrs in presence of fluconazole by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1065958 | Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
| AID1845804 | Inhibition of HDAC7 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1355689 | Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1452865 | Inhibition of HDAC3 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1337197 | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells at 10 uM preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluoresce | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1655364 | Selectivity index, ratio of IC50 for HDAC1 in mouse N2A cells to IC50 for HDAC6 in mouse N2A cells | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1337278 | Antiproliferative activity against human HL60 cells | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1249616 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators. |
| AID1418666 | Inhibition of recombinant human HDAC6 using fluorogenic HDAC substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1845459 | Inhibition of HDAC1 (unknown origin) | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery? |
| AID708192 | Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. |
| AID1679259 | Inhibition of human HDAC1 using p53 fluorogenic peptide (379 to 382 residues) RHKKAc as substrate by fluorescence-based assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID655916 | Immunosuppressive activity against C57BL/6 mouse CFSE-labelled effector T cells assessed as inhibition of T regulatory cells-mediated proliferation at Treg:Teff ratio of 1:16 at 1 uM after 3 to 4 days by flow cytometry (Rvb = 86.9%) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1384217 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 0.5 to 2 hrs by Western blot analysis | 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. |
| AID1879893 | Inhibition of recombinant human HDAC6 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
| AID1424825 | Selectivity ratio of IC50 for human recombinant HDAC4 to IC50 for human recombinant HDAC6 | 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. |
| AID1406981 | Inhibition of human recombinant N-terminal GST-tagged full length HDAC6 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1424820 | Inhibition of human recombinant HDAC8 using RHKAcKAcAMC 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. |
| AID1401341 | Inhibition of HDAC in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1753836 | Selectivity index, ratio of IC50 for inhibition of recombinant human HDAC1 to IC50 for inhibition of recombinant human HDAC6 | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
| AID1740092 | Inhibition of human full length recombinant HDAC7 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1294949 | Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 substrate assessed as remaining activity at 10 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1428502 | Inhibition of full length human recombinant C-terminal GST-tagged HDAC2 expressed in insect cells using RHKK(Ac) as substrate after 60 mins by fluorimetric method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1845460 | Inhibition of HDAC6 (unknown origin) | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery? |
| 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. |
| AID1406984 | Inhibition of HDAC6 in human NB4 cells assessed as levels of alpha-tubulin acetylation at 1 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1424822 | Selectivity ratio of IC50 for human recombinant HDAC2 to IC50 for human recombinant HDAC6 | 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. |
| AID1848585 | Inhibition of full length C-terminal his6/FLAG-tagged human recombinant HDAC3 (1 to 2383 residues) expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
| AID1726028 | Inhibition of full length N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using ZMAL as substrate incubated for 90 mins by fluorescence assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation. |
| AID1864670 | Inhibition of recombinant HDAC7 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1476146 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID772638 | Inhibition of human recombinant HDAC2 using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1449324 | Inhibition of HDAC in human A2780CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1895829 | Inhibition of human HDAC6 | 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). |
| AID1882268 | Inhibition of recombinant human HDAC6 using RHKKAc peptide as substrate | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| AID1294957 | Inhibition of recombinant human HDAC1 using Fluor de Lys-SIRT1 as substrate assessed as remaining activity at 10000 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1337201 | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate by fluorescence assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1173499 | Inhibition of full length GST-tagged human HDAC1 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1428501 | Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf21 cells using RHKK(Ac) as substrate after 60 mins by fluorimetric method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1165106 | Selectivity ratio of IC50 for axenic amastigote stage of Leishmania donovani to IC50 for amastigote stage of Leishmania donovani infected in human THP1 cells | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| 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. |
| 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. |
| AID1707500 | Synergistic antifungal activity against Candida albicans 9884 assessed as potentiation of fluconazole antifungal activity by measuring FICI incubated for 48 hrs in presence of fluconazole by checkerboard microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1355691 | Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1617399 | Selectivity ratio of IC50 for human HDAC2 expressed in baculovirus infected sf9 insect cells to IC50 for human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| 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. |
| AID1679248 | Selectivity ratio of IC50 for human HDAC9 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1651330 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
| AID1740094 | Inhibition of human full length recombinant HDAC10 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1294958 | Inhibition of recombinant human HDAC1 using Fluor de Lys-SIRT1 as substrate assessed as remaining activity at 100000 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID655921 | Immunosuppressive activity against C57BL/6 mouse CFSE-labelled effector T cells assessed as Treg suppression of Teffector proliferation AUC at 1 uM after 3 to 4 days by flow cytometry relative to control | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1418676 | Neuroprotective activity against H2O2-induced toxicity in rat PC12 cells assessed as cell viability at 5 to 10 uM pretreated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with ebselen by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1655373 | Protein binding in mouse brain homogenate | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID655911 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| 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. |
| AID1339575 | Selectivity ratio of IC50 for HDAC1 in human HeLaS3 cells to IC50 for full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1534440 | Inhibition of human full-length recombinant HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as substrate Km using Boc-Lys (Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluores | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer. |
| AID1401375 | Inhibition of HDAC6 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1384213 | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | 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. |
| AID1587867 | Inhibition of HDAC6 in human BE(2)-C cells assessed as increase in tubulin acetylation measured after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1764797 | Inhibition of HDAC6 in mouse Neuro2a cells assessed as fold increase in ratio of acetylated alpha-tubulin to alpha tubulin at 0.01 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. |
| AID1449341 | Inhibition of HDAC6 in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 10 uM preincubated for 48 hrs followed by cisplatin treatment measured after 72 hrs by MTT assay relat | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1707485 | Antifungal activity against Candida albicans 9884 incubated for 48 hrs by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1459956 | Selectivity ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC6 | 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. |
| AID1783142 | Inhibition of HDAC11 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| 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. |
| AID1339570 | Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1587868 | Inhibition of HDAC10 in human BE(2)-C cells assessed as expansion of lysosomal compartment at 0.1 to 10 uM incubated for 24 hrs by LysoTracker Red DND-99 probe-based fluorescence assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1882450 | Inhibition of human recombinant HDAC6 using RHKKAc as substrate | 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. |
| AID1401352 | Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 4 x 10'-5 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1864736 | Inhibition of HDAC6 (unknown origin) | | | |
| AID1845807 | Inhibition of HDAC10 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1452864 | Inhibition of HDAC2 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors. |
| AID1848582 | Inhibition of full length his6/FLAG-tagged human recombinant HDAC1(1 to 482 residues) expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
| AID1882451 | Inhibition of human recombinant HDAC1 using RHKKAc as substrate | 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. |
| AID1428505 | Selectivity ratio of IC50 for full length human recombinant C-terminal GST-tagged HDAC2 to IC50 for full length human recombinant N-terminal GST-tagged HDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1280320 | Inhibition of recombinant human KDAC8 using diacetylated p53 (379 to 382 residues) as substrate by fluorescence assay | 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. |
| AID1537554 | Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based a | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7
| Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
| AID1173500 | Inhibition of full length C-terminal 6x-His tagged human HDAC2 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1707491 | Synergistic antifungal activity against Candida albicans 10061 incubated for 48 hrs in presence of fluconazole by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1917536 | Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID655906 | Immunosuppressive activity against C57BL/6 mouse CFSE-labelled effector T cells assessed as inhibition of T regulatory cells-mediated proliferation at Treg:Teff ratio of 1:8 at 1 uM after 3 to 4 days by flow cytometry (Rvb = 78.2%) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1294950 | Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 substrate assessed as remaining activity at 100 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1401376 | Inhibition of human recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1655341 | Ratio of drug level in brain to plasma in C57BL/6 mouse at 3 mg/kg, iv measured after 8 mins by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID655910 | Inhibition of human recombinant HDAC6 using RHKKAc peptide as substrate incubated for 5 to mins prior to substrate addition measured after 2 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. |
| AID1572343 | Selectivity ratio of IC50 for recombinant C-terminal His/FLAG-tagged human HDAC1 to IC50 for N-terminal GST-tagged human HDAC6 | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| 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. |
| AID1384216 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 4 hrs by Western blot analysis relative to control | 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. |
| AID1339578 | Inhibition of HDAC6 in human U937 cells assessed as increase in alpha-tubulin acetylation at Lys-40 residue at 2 uM after 18 hrs by Western blot method | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1493594 | Inhibition of HDAC4 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1753834 | Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
| AID732151 | Inhibition of HDAC8 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1707499 | Synergistic antifungal activity against Candida albicans 9172 assessed as potentiation of fluconazole antifungal activity by measuring FICI incubated for 48 hrs in presence of fluconazole by checkerboard microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1849158 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
| Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
| AID1864733 | Inhibition of HDAC1 (unknown origin) | | | |
| AID1655375 | In vivo inhibition of HDAC6 in C57BL/6 mouse cortex assessed as increase in alpha tubulin acetylation at 20 mg/kg, ip administered bid with interval of 4 hrs and measured after 1.5 hrs of last dosage by Western blot analysis | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1753633 | Ratio of drug concentration in brain to plasma of mouse at 5 to 50 mg/kg, ip after 2 hrs by HPLC/MS-MS analysis | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
| AID1401475 | Selectivity ratio of IC50 for HDAC2 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1707502 | Synergistic antifungal activity against Candida albicans 4108 assessed as potentiation of fluconazole antifungal activity by measuring FICI incubated for 48 hrs in presence of fluconazole by checkerboard microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1173507 | Inhibition of full length N-terminal GST-tagged human HDAC11 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1572392 | Selectivity ratio of IC50 for recombinant human HDAC8 using RHKKAc fluorogenic peptide substrate to IC50 for recombinant human HDAC6 using RHKKAc fluorogenic peptide substrate | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1655346 | Half life in CD-1 mouse at 3 mg/kg, iv | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1418669 | Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation measured as trolox equivalent at 10 to 100 uM preincubated for 10 mins followed by AAPH addition and measured every minute for 120 mins by ORAC-FL assay | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| 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. |
| AID1679249 | Selectivity ratio of IC50 for human HDAC10 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1845806 | Inhibition of HDAC6 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1864667 | Inhibition of recombinant HDAC4 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1845854 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1424824 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 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. |
| AID1707496 | Synergistic antifungal activity against Candida albicans 10061 assessed as fluconazole MIC incubated for 48 hrs in presence of fluconazole by microdilution assay (Rvb = fluconazole alone MIC = >64 ug/ml) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1617402 | Stability in rat plasma assessed as parent compound remaining at 100 uM after 4 hrs by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| AID1707488 | Antifungal activity against Candida krusei 10153 incubated for 48 hrs by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1337279 | Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1428497 | Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1428504 | Selectivity ratio of IC50 for full length human recombinant C-terminal FLAG-His-tagged HDAC1 to IC50 for full length human recombinant N-terminal GST-tagged HDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1406982 | Inhibition of human recombinant C-terminal His/FLAG-tagged full length HDAC1 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1753835 | Inhibition of recombinant human HDAC1 using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity. |
| AID1707498 | Synergistic antifungal activity against Candida krusei 10153 assessed as fluconazole MIC incubated for 48 hrs in presence of fluconazole by microdilution assay (Rvb = fluconazole alone MIC = 64 ug/ml) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID767947 | Inhibition of human recombinant HDAC8 protein using RHKAcKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| 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. |
| AID1882270 | Ratio of AUC in mouse brain to plasma | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| AID1783115 | Antiproliferative activity against human NCI-H929 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1493592 | Inhibition of human recombinant full-length C-terminal GST-tagged HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1449319 | Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1339569 | Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1532658 | Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
| AID1401484 | Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1764256 | Induction of histone H-3 expression in human CAL-27 cells for 24 hrs by Western blot analysis | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. |
| AID1384208 | Inhibition of HDAC3 (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. |
| AID1600728 | Inhibition of C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation fo | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
| Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1401492 | Cytotoxicity against human U937 cells assessed as cell viability at 5 x 10'-4 M after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1294951 | Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 substrate assessed as remaining activity at 1000 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1723894 | Inhibition of HDAC1 (unknown origin) | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models. |
| AID1679247 | Selectivity ratio of IC50 for human HDAC11 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1355705 | Antifungal activity against FLC resistant Candida albicans 0304103 after 48 hrs by checkerboard microdilution method | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1707501 | Synergistic antifungal activity against Candida albicans 10061 assessed as potentiation of fluconazole antifungal activity by measuring FICI incubated for 48 hrs in presence of fluconazole by checkerboard microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID767954 | Inhibition of human recombinant HDAC1 protein using RHKKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1785338 | Inhibition of HDAC7 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | | | |
| AID767944 | Inhibition of human recombinant HDAC11 protein using RHKKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1726029 | Selectivity ratio of IC50 for full length C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system to IC50 full length N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation. |
| AID1783123 | Induction of apoptosis in human HL-60 cells assessed as late apoptotic cells at 3 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 1.45%) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1493590 | Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID732146 | Inhibition of HDAC1 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1424819 | Inhibition of human recombinant HDAC4 using fluorogenic trifluoroacetyl lysine 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. |
| AID1679257 | Inhibition of human HDAC2 using p53 fluorogenic peptide (379 to 382 residues) RHKKAc as substrate by fluorescence-based assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1406985 | Inhibition of HDAC6 in human NB4 cells assessed as levels of alpha-tubulin acetylation at 5 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1558048 | Induction of cell death in human PC3 cells at 0.1 to 25 uM | 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. |
| AID1449226 | Inhibition of HDAC6 in human Cal27CisR cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 10 uM preincubated for 48 hrs followed by cisplatin addition measured after 72 hrs by MTT assay relati | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups. |
| AID1202591 | Cytotoxicity against human KB cells after 72 hrs by MTS assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
| AID1764817 | Inhibition of HDAC6 in human RPMI-8226 cells assessed as increase in tubulin acetylation incubated for 6 hrs 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. |
| 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. |
| AID1449316 | Antiproliferative activity against human A2780 cells measured after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1917530 | Inhibition of HDAC1 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1428498 | Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1785339 | Inhibition of HDAC8 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1783135 | Inhibition of HDAC4 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| 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. |
| AID1418683 | Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based fluorescence analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1879896 | Inhibition of recombinant human HDAC8 using H2N-Arg- His-Lys(Ac)-Lys(Ac)-AMC as substrate incubated for 90 mins and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
| 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. |
| AID1864695 | Half life in CD-1 mouse at 3 mg/kg, iv measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1785343 | Inhibition of recombinant human SIRT5 measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1493596 | Inhibition of HDAC7 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| 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. |
| AID1384220 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 4 hrs cotreated with sildenafil by AlphaLISA assay relative to control | 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. |
| AID1401474 | Selectivity ratio of IC50 for HDAC1 in human HeLa-S3 cell lysates to IC50 for HDAC6 in human HeLa-S3 cell lysates | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1655370 | Drug concentration in CD-1 mouse plasma at 3 mg/kg, iv measured at 60 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1655356 | In vivo inhibition of HDAC6 in C57BL/6 mouse heart assessed as increase in alpha tubulin acetylation at 10 mg/kg, ip measured at 1 hr by Western blot analysis | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1707484 | Antifungal activity against Candida albicans 9172 incubated for 48 hrs by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| 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. |
| AID1783126 | Cytotoxicity against human GEC1 cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| 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. |
| AID1587865 | 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 baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1173505 | Inhibition of full length C-terminal 6x-His tagged human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1651331 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
| Synthesis and biological evaluation of 2-quinolineacrylamides. |
| AID1917529 | Inhibition of HDAC6 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1655359 | Protein binding in mouse plasma assessed as unbound fraction measured at initial point | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1165109 | Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| AID1864691 | Cmax in CD-1 mouse at 3 mg/kg, iv measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1633994 | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV). |
| AID1337253 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1534485 | Inhibition of HDAC6 in mouse LL/2 cells assessed as reduction in PD-L1 expression at 10 uM after 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer. |
| 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. |
| AID1864682 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1845809 | Inhibition of HDAC8 (unknown origin) using RHKAcKAc fluorogenic-diacyl peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1401477 | Selectivity ratio of IC50 for HDAC1 in human HeLa-S3 cell lysates to IC50 for recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1848584 | Inhibition of full length C-terminal FLAG-tagged human recombinant HDAC6 expressed inSf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
| AID1617397 | Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| AID1384233 | Inhibition of PDE5 in human SH-SY5Y cells assessed as induction of phosphorylated CREB level at 500 nM after 30 mins by Western blot analysis relative to control | 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. |
| AID1740093 | Inhibition of human full length recombinant HDAC9 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1882453 | Inhibition of human recombinant HDAC3/NcoR2 using RHKKAc as substrate | 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. |
| AID1401491 | Cytotoxicity against human U937 cells assessed as cell viability at 1 x 10'-3 M after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1917544 | Selectivity index, ratio IC50 for inhibition of HDAC11 (unknown origin) to IC50 for inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1476152 | Antiproliferative activity against human Jurkat cells | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| 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. |
| AID1740096 | Inhibition of human full length recombinant HDAC6 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1587864 | Inhibition of recombinant full-length C-terminal His-tagged human HDAC2 expressed in baculovirus infected Sf9 insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1783134 | Inhibition of HDAC3 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1655358 | Protein binding in mouse plasma | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1384231 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 1000 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID1294952 | Inhibition of recombinant human HDAC6 using Fluor de Lys-SIRT1 substrate assessed as remaining activity at 10000 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1355708 | Antifungal activity against FLC resistant Candida albicans 100 after 48 hrs by checkerboard microdilution method | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1917531 | Selectivity index, ratio IC50 for inhibition of HDAC6 (unknown origin) to IC50 for inhibition of HDAC1 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1864700 | AUC(0 to infinity) in CD-1 mouse at 30 mg/kg, po measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1753634 | Neuroprotective activity in Sprague-Dawley rat middle cerebral artery occlusion model assessed as reduction in cerebral infarction at 25 mg/kg, ip after 24 hrs by TTC staining based assay (Rvb = 21.22%) | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
| AID1479822 | Selectivity ratio of Ki for recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) to Ki for full length recombinant human N-terminal GST-tagged HDAC6 | 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. |
| AID1655357 | In vivo inhibition of HDAC6 in C57BL/6 mouse heart assessed as increase in alpha tubulin acetylation at 10 mg/kg, ip measured after 1 to 24 hrs by Western blot analysis | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1493595 | Inhibition of HDAC5 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| 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). |
| AID1864674 | Binding affinity to recombinant HDAC1 (unknown origin) assessed as inhibition constant using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1882452 | Inhibition of human recombinant HDAC2 using RHKKAc as substrate | 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. |
| AID1617400 | Selectivity ratio of IC50 for 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 to human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| AID1449318 | Antiproliferative activity against human A2780cisR cells measured after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1845805 | Inhibition of HDAC9 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1337301 | Inhibition of HDAC6 in human MOLM14 cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1406987 | Inhibition of class 1 HDAC in human U87 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 5 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1845802 | Inhibition of HDAC4 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1740086 | Inhibition of human full length recombinant HDAC1 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1339572 | Selectivity ratio of IC50 for HDAC1 in human HeLaS3 cells to IC50 for HDAC6 in human HeLaS3 cells | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1424818 | Inhibition of human recombinant HDAC2 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. |
| AID1895831 | Ratio of AUC in brain to plasma in mouse measured for 5 to 60 mins by HPLC/MS/MS analysis | 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). |
| AID1707486 | Antifungal activity against Candida albicans 10061 incubated for 48 hrs by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1849159 | Selectivity index, ratio of IC50 for inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells to IC50 for inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
| Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia. |
| AID1401493 | Cytotoxicity against human U937 cells assessed as cell viability at 2.5 x 10'-4 M after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1633992 | Inhibition of HDAC6 in human HuH7 cells assessed as increase in alpha-tubulin K40 acetylation at varying concentrations incubated for 24 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV). |
| AID1424821 | Inhibition of human recombinant HDAC10 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. |
| AID1587863 | Inhibition of recombinant full-length C-terminal FLAG-fused/His-tagged human HDAC1 expressed in baculovirus infected Sf9 insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
| Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. |
| AID1754884 | Inhibition of HDAC6 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. |
| AID1406989 | Inhibition of HDAC6 in human U87 cells assessed as levels of alpha-tubulin acetylation at 5 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1707493 | Synergistic antifungal activity against Candida krusei 10153 incubated for 48 hrs in presence of fluconazole by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1173504 | Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID772630 | Inhibition of human recombinant HDAC10 using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1406983 | Inhibition of class 1 HDAC in human NB4 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 5 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1882454 | Inhibition of human recombinant HDAC8 using RHKAcKAc as substrate | 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. |
| AID1476149 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1525779 | Inhibition of HADC3 (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. |
| AID1339567 | Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1558022 | Induction of apoptosis in mouse SM1 cells at 0.1 to 25 uM by caspase3/7 reagent based luminescence assay | 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. |
| AID1864664 | Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1785341 | Inhibition of recombinant human HDAC11 measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1384235 | Effective permeability of the compound at 50 uM after 18 hrs by UV spectroscopy based PAMPA | 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. |
| 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. |
| 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. |
| AID1428513 | Induction of apoptosis in human HCT116 cells assessed as increase in cleaved PARP levels at 1.25 to 2.5 uM after 48 hrs Western blot method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1707490 | Synergistic antifungal activity against Candida albicans 9884 incubated for 48 hrs in presence of fluconazole by microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1753648 | Inhibition of N-terminal GST-tagged full-length human HDAC6 expressed in Sf9 infected baculovirus system using FTS as substrate preincubated for 10 mins followed by substrate addition and measured for 30 mins | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction. |
| AID1418671 | GPx-like activity of the compound assessed as velocity for tert-butyl hydroperoxide reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1783133 | Inhibition of HDAC2 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1401489 | Cytotoxicity against human U937 cells assessed as cell viability at 4 x 10'-3 M after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1707494 | Synergistic antifungal activity against Candida albicans 9172 assessed as fluconazole MIC incubated for 48 hrs in presence of fluconazole by microdilution assay (Rvb = fluconazole alone MIC = >64 ug/ml) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1785335 | Inhibition of HDAC4 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1707507 | Inhibition of human HDAC1 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1406991 | Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as levels of histone H3 acetylation at lysine 9/14 at 5 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1740095 | Inhibition of human full length recombinant HDAC11 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID767952 | Inhibition of HDAC3/NcoR2 (unknown origin) using RHKKAc from p53 as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID772634 | Inhibition of human recombinant HDAC5 using acetyl-Lys(trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1726027 | Inhibition of full length C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using ZMAL as substrate incubated for 90 mins by fluorescence assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation. |
| AID1294962 | Inhibition of HDAC6 in human HeLa cells assessed as increase in hyperacetylation of alpha-tubulin 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. |
| AID1337256 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines. |
| AID1882266 | Inhibition of recombinant human HDAC2 using RHKKAc peptide as substrate | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy. |
| AID1355731 | Protection against spleen enlargement in SCID mouse xenografted with human HEL cells at 10 mg/kg, ip qd | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1476147 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1740090 | Inhibition of human full length recombinant HDAC4 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1401490 | Cytotoxicity against human U937 cells assessed as cell viability at 3 x 10'-3 M after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1740091 | Inhibition of human full length recombinant HDAC5 using p53 (379 to 382 residues) Ac-LGK(TFA)-AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1783121 | Induction of apoptosis in human HL-60 cells assessed as viable cells at 3 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 93.4%) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1406990 | Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as levels of histone H3 acetylation at lysine 9/14 at 1 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1591718 | Inhibition of HDAC6 in human HeLa cells assessed as increase in alpha-tubulin acetylation at 0.1 to 10 uM after 24 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
| Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors. |
| AID1537556 | Selectivity index, ratio of IC50 for recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells to IC50 for recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cel | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7
| Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. |
| AID1572373 | Inhibition of recombinant human HDAC8 using RHKKAc fluorogenic peptide substrate | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
| AID1558014 | Inhibition of HDAC6 in mouse SM1 cells assessed as increase in acetylated alpha-tubulin level at 5 to 10 uM after 24 hrs by Western blot analysis | 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. |
| AID767948 | Inhibition of human recombinant HDAC7 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1864684 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1401342 | Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 3.2 x 10'-4 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| 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. |
| AID1783125 | Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1655353 | Plasma concentration in CD-1 mouse at 30 mg/kg, po measured at 1 hr | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1655362 | Inhibition of HDAC1 in mouse N2A cells | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1339568 | Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1173502 | Inhibition of N-terminal GST-tagged human HDAC4 (627 to 1085 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1917542 | Inhibition of HDAC11 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1785344 | Inhibition of full length human CDK2 (1 to 298 end residues)/N-terminal GST-tagged CyclinA2 (1 to 432 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate and ATP addition by mobility shift assay | | | |
| AID1679246 | Selectivity ratio of IC50 for human HDAC8 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1355722 | Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID1783138 | Inhibition of HDAC7 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1424826 | Inhibition of HDAC6 in human MV4-11 cells assessed as accumulation of acetylated alpha-tubulin at 200 nM after 24 hrs by Western blot analysis | 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. |
| AID1600729 | Inhibition of N-terminal GST-tagged recombinant human HDAC6 (1 to 1215 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins me | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
| Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| 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. |
| AID1655345 | Clearance in CD-1 mouse at 3 mg/kg, iv | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| 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). |
| AID1655343 | Metabolic stability in mouse plasma assessed as half life | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID772632 | Inhibition of human recombinant HDAC8 using RHKAcKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1418677 | Cytotoxicity against rat PC12 cells at 20 uM after 24 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1339571 | Inhibition of full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1449224 | Inhibition of HDAC6 in human Cal27 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring fold reduction in cisplatin IC50 at 10 uM preincubated for 48 hrs followed by cisplatin addition measured after 72 hrs by MTT assay relative t | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups. |
| AID1418681 | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1532657 | Inhibition of human HDAC6 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Highly fluorescent and HDAC6 selective scriptaid analogues. |
| AID1418668 | Inhibition of recombinant human HDAC3 at 1 uM using fluorogenic HDAC substrate after 30 mins by fluorescence analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| 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). |
| AID1383998 | Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. |
| AID1428499 | Antiproliferative activity against human A549 cells after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1401373 | Inhibition of HDAC2 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1384228 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 1000 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID1864692 | Cmax in CD-1 mouse at 30 mg/kg, po measured after 0.083 to 24 hrs by LC-MS/MS analysis | | | |
| AID1864668 | Inhibition of recombinant HDAC5 (unknown origin) using Boc-Lys (trifluoroacetyl) AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1476120 | Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells at 10 uM using RHKKAc as substrate in presence of ATP relative to control | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1294954 | Inhibition of recombinant human HDAC1 using Fluor de Lys-SIRT1 as substrate incubated for 15 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. |
| AID1173503 | Inhibition of C-terminal 6x-His tagged human HDAC5 (657 to 1123 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1864673 | Inhibition of HDAC11(unknown origin) preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1864686 | Inhibition of recombinant human HDAC6 at 10 to 1000 nM using acetyl-Lys (Ac)-AMC as substrate measured after 1 hr by sharp dilution method | | | |
| 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. |
| AID732143 | Inhibition of HDAC7 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID767946 | Inhibition of human recombinant HDAC9 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1201001 | Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC6 | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
| Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
| 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. |
| AID1355711 | Antifungal activity against FLC resistant Candida albicans 0710922 after 48 hrs by checkerboard microdilution method | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
| Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections. |
| AID732152 | Inhibition of HDAC6 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1633993 | Antiviral activity against HCV infected in human HuH7-luc/neo cells assessed as inhibition of DNA replication incubated for 3 days by luciferase reporter gene assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
| Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV). |
| AID732142 | Inhibition of HDAC9 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1707503 | Synergistic antifungal activity against Candida krusei 10153 assessed as potentiation of fluconazole antifungal activity by measuring FICI incubated for 48 hrs in presence of fluconazole by checkerboard microdilution assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1655361 | Inhibition of HDAC6 in mouse N2A cells assessed as increase in alpha tubulin acetylation | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1783139 | Inhibition of HDAC8 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1396955 | Inhibition of human HDAC6 using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
| AID1723743 | Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
| Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups. |
| AID1401500 | Cytotoxicity against human U937 cells assessed as cell viability at 80 uM after 44 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1294955 | Inhibition of recombinant human HDAC1 using Fluor de Lys-SIRT1 as substrate assessed as remaining activity at 100 nM incubated for 15 mins by fluorescence assay relative to control | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity. |
| AID1783132 | Inhibition of HDAC1 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1396960 | Antiproliferative activity against human PC3 cells | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
| AID767951 | Inhibition of human recombinant HDAC4 protein using Acetyl-Lys (trifluoroacetyl)-AMC as substrate | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1476121 | Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHKKAc as substrate in presence of ATP | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1173501 | Inhibition of full length C-terminal 6x-His tagged human HDAC3 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform. |
| AID1617413 | Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
| Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation. |
| AID1864685 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 120 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1848586 | Inhibition of full length C-terminal his-tagged human recombinant HDAC8 expressed in Sf9 insect cells | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. |
| AID1406986 | Inhibition of class 1 HDAC in human U87 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 1 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1396954 | Inhibition of human HDAC1 at 10 uM using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate relative to control | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6). |
| AID1401347 | Inhibition of HDAC in human HeLa-S3 cell lysates assessed as residual activity at 8 x 10'-5 M preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 35 mins by fluorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1189852 | Antiviral activity against HCV genotype 1b infected in human Huh7 cells at 10 uM after 3 days by luciferase reporter gene assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
| Hydroxamic acids block replication of hepatitis C virus. |
| AID1165105 | Antileishmanial activity against axenic amastigote stage of Leishmania donovani after 72 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
| The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors. |
| AID1557976 | Induction of cell death in mouse SM1 cells at 0.1 to 25 uM | 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. |
| AID1754886 | Inhibition of HDAC6 (unknown origin) at 0.5 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. |
| AID1845857 | Selectivity index, ratio of IC50 for HDAC8 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1655348 | Plasma concentration in CD-1 mouse at 3 mg/kg, iv measured at 1 hr | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1418672 | GPx-like activity of the compound assessed as velocity for cumene hydroperoxide reduction at 80 uM in presence of GSH and NADPH by spectrophotometric analysis | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID732153 | Inhibition of HDAC4 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. |
| AID1428514 | Induction of apoptosis in human HCT116 cells assessed as increase in cleaved caspase 3 levels at 1.25 to 2.5 uM after 48 hrs Western blot method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1534513 | Inhibition of human full-length recombinant HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as substrate Vmax using Boc-Lys (Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluor | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer. |
| AID1655351 | Half life in CD-1 mouse at 30 mg/kg, po | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1449323 | Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1879887 | Inhibition of zebra fish HDAC10 using Ac-spermidine-AMC as substrate incubated for 25 mins and measured by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells. |
| 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. |
| AID1065962 | Cytotoxicity against androgen-independent human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors. |
| AID1783114 | Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1558021 | Cytotoxicity against mouse SM1 cells at 0.1 to 25 uM by ApoTox-Glo triplex assay | 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. |
| AID1449325 | Inhibition of HDAC in human Cal27CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines. |
| AID1189853 | Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability at 10 uM after 3 days by CellTiter 96 assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
| Hydroxamic acids block replication of hepatitis C virus. |
| 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. |
| AID1864683 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | | | |
| AID1479835 | Inhibition of HDAC6 in human MV4-11 cells assessed as induction of alpha-tubulin hyperacetylation at 5 uM after 2 to 24 hrs by Western blot method | 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. |
| 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. |
| AID1476151 | Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1655342 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK-MDR1 cells incubated for 2 hrs by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1459978 | Selectivity ratio of IC50 for recombinant human HDAC8 to IC50 for recombinant human HDAC6 | 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. |
| AID1679252 | Selectivity ratio of IC50 for human HDAC4 to IC50 for human HDAC6 | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| 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. |
| AID1384224 | Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay | 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. |
| AID1655371 | Ratio of drug level in brain to plasma in CD-1 mouse at 3 mg/kg, iv measured after 8 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1740088 | Inhibition of human full length recombinant HDAC3/ NcoR2 using p53 (379 to 382 residues) (RHKK(Ac)AMC) as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence method | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1655365 | Ratio of EC50 for inhibition of HDAC6 in mouse N2A cells assessed as alpha tubulin acetylation to IC50 for HDAC6 in mouse N2A cells | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1783140 | Inhibition of HDAC9 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1917528 | Inhibition of PI3Kdelta (unknown origin) measured by ADP-Glo assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| 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. |
| AID1845799 | Inhibition of HDAC1 (unknown origin) using RHKKAc fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1401374 | Inhibition of HDAC3 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1783141 | Inhibition of HDAC10 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1384214 | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 1 hr fluorescence assay | 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. |
| AID1917933 | Inhibition of HDAC6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease. |
| AID1503856 | Antitumor activity against mouse B16-F10-luc cells xenografted in C57BL/6 mouse assessed as reduction in tumor volume at 20 mg/kg, ip administered daily for 22 days | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models. |
| AID1655360 | Protein binding in mouse plasma assessed as unbound fraction measured at 1 hr | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1655372 | Ratio of drug level in brain to plasma in CD-1 mouse at 3 mg/kg, iv measured after 60 mins | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1845803 | Inhibition of HDAC5 (unknown origin) using Acetyl-Lys(trifluoroacetyl)-AMC fluorogenic peptide as substrate by fluorescence assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity. |
| AID1917541 | Inhibition of HDAC8 (unknown origin) measured by fluorescence based assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template. |
| AID1384229 | Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 100 nM after 2 hrs by Western blot analysis relative to control | 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. |
| AID1406978 | Inhibition of class 1 HDAC in human NB4 cells assessed as levels of histone H3 acetylation at lysine 9/14 at 1 uM after 30 hrs by Western blot analysis relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies. |
| AID1707508 | Inhibition of human HDAC6 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis. |
| AID1493597 | Inhibition of HDAC8 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of a fluorescent probe with HDAC6 selective inhibition. |
| AID1339576 | Selectivity ratio of IC50 for HDAC2 in human HeLaS3 cells to IC50 for full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1202599 | Inhibition of HDAC1 (unknown origin) | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. |
| AID1418680 | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID772654 | Inhibition of human recombinant HDAC1 using RHKKAc as substrate | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. |
| AID1785340 | Inhibition of recombinant human HDAC9 measured after 30 mins by fluorescence microplate reader assay | | | |
| AID1324256 | Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation measured after 24 hrs relative to control | 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. |
| AID1783108 | Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1418690 | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with ebselen by DCFH-DA dye-based fluore | 2018 | Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
| Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease. |
| AID1476150 | Antiproliferative activity against human HL60 cells | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat. |
| AID1339574 | Selectivity ratio of IC50 for HDAC3 in human HeLaS3 cells to IC50 for HDAC6 in human HeLaS3 cells | 2017 | ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
| Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity. |
| AID1783137 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors. |
| AID1655376 | Metabolic stability in mouse Hepatocyte assessed as half life | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor. |
| AID1401372 | Inhibition of HDAC1 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity. |
| AID1802356 | Inhibitor Competition Assay from Article 10.1021/acschembio.6b00776: \\LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation.\\ | 2017 | ACS chemical biology, 01-20, Volume: 12, Issue:1
| LSD1 Substrate Binding and Gene Expression Are Affected by HDAC1-Mediated Deacetylation. |
| 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. |
| 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. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| 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. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |