Page last updated: 2024-11-13
acy-1215
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
ricolinostat: an HDAC6 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 53340666 |
| CHEMBL ID | 2364628 |
| CHEBI ID | 95073 |
| SCHEMBL ID | 574580 |
| MeSH ID | M0573810 |
Synonyms (59)
| Synonym |
|---|
| acy-1215 |
| 1316214-52-4 |
| rocilinostat (acy-1215) |
| wkt909c62b , |
| unii-wkt909c62b |
| 2-(diphenylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide |
| rocilinostat |
| 5-pyrimidinecarboxamide, 2-(diphenylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)- |
| ricolinostat [usan:inn] |
| acy-63 |
| ricolinostat |
| HY-16026 |
| CS-0965 |
| NCGC00345802-01 |
| ricolinostat [who-dd] |
| 2-(diphenylamino)-n-[7-(hydroxyamino)-7-oxoheptyl]pyrimidine-5-carboxamide |
| ricolinostat [usan] |
| ricolinostat [inn] |
| S8001 |
| gtpl7010 |
| n-[7-(hydroxyamino)-7-oxoheptyl]-2-(n-phenylanilino)pyrimidine-5-carboxamide |
| SCHEMBL574580 |
| CHEMBL2364628 |
| us8609678, 2-(diphenylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide [26] |
| bdbm50439674 |
| MLS006011181 |
| smr004702950 |
| AKOS024259260 |
| 2-(diphenylamino)-n-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide |
| D10661 |
| ricolinostat (usan/inn) |
| AC-30258 |
| DTXSID40157148 |
| J-690127 |
| EX-A139 |
| CHEBI:95073 |
| HMS3653F17 |
| AS-73344 |
| mfcd22666356 |
| NCGC00345802-05 |
| acy1215 |
| 7-{[2-(diphenylamino)pyrimidin-5-yl]formamido}-n-hydroxyheptanamide |
| SW219836-1 |
| DB12376 |
| ah4 , |
| ricolinostat (acy-1215) |
| BCP06028 |
| Q27088553 |
| 5-pyrimidinecarboxamide, 2-(diphenylamino)-n-[7-(hydroxyamino)-7-oxoheptyl]- |
| SB17054 |
| HMS3426C09 |
| HMS3886L21 |
| AMY38185 |
| CCG-269054 |
| SY096614 |
| nsc-767952 |
| nsc767952 |
| acy 1215 |
| BA164806 |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Most adverse events were grade 1-2, including diarrhea (57%), nausea (57%), and fatigue (43%)." | ( First-in-Class Selective HDAC6 Inhibitor (ACY-1215) Has a Highly Favorable Safety Profile in Patients with Relapsed and Refractory Lymphoma. Amengual, JE; Cremers, S; Jones, S; Lichtenstein, R; Lue, JK; Ma, H; Sawas, A; Shah, B, 2021) | 0.89 |
| "ACY-1215 is an oral selective HDAC6 inhibitor that was safe in patients with relapsed and refractory lymphoid malignancies and led to disease stabilization in half of the evaluable patients." | ( First-in-Class Selective HDAC6 Inhibitor (ACY-1215) Has a Highly Favorable Safety Profile in Patients with Relapsed and Refractory Lymphoma. Amengual, JE; Cremers, S; Jones, S; Lichtenstein, R; Lue, JK; Ma, H; Sawas, A; Shah, B, 2021) | 2.33 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " Pharmacokinetic data showed peak plasma levels of ACY-1215 at 4 hours after treatment coincident with an increase in acetylated α-tubulin, a marker of HDAC6 inhibition, by immunohistochemistry and Western blot analysis." | ( Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Anderson, KC; Bradner, J; Canavese, M; Cirstea, D; Eda, H; Hideshima, T; Jarpe, M; Jones, SS; Kung, AL; Mazitschek, R; Ogier, WC; Raje, N; Rodig, S; Santo, L; Scullen, T; Tamang, D; Tseng, JC; van Duzer, JH; Yang, M, 2012) | 0.85 |
| " This novel method has been applied to a pharmacokinetic study in mice." | ( Sensitive method for the determination of rocilinostat in small volume mouse plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. Bhamidipati, RK; Devaraj, VC; Dewang, P; Dixit, A; Gupta, M; Hallur, MS; Mullangi, R; Rajagopal, S; Zainuddin, M, 2016) | 0.43 |
Compound-Compound Interactions
| Excerpt | Reference | Relevance |
|---|---|---|
| " In the present study, we investigated the preclinical activity of ACY-1215, an HDAC6-selective inhibitor, alone and in combination with bortezomib in MM." | ( Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Anderson, KC; Bradner, J; Canavese, M; Cirstea, D; Eda, H; Hideshima, T; Jarpe, M; Jones, SS; Kung, AL; Mazitschek, R; Ogier, WC; Raje, N; Rodig, S; Santo, L; Scullen, T; Tamang, D; Tseng, JC; van Duzer, JH; Yang, M, 2012) | 0.83 |
Bioavailability
Dosage Studied
Flow cytometry was used to determine a suitable treatment dosage of ACY-1215 on lipopolysaccharide (LPS)-activated macrophages. 50% of patients treated on a twice-daily dosing schedule.
| Excerpt | Relevance | Reference |
|---|---|---|
| "Flow cytometry was used to determine a suitable treatment dosage of ACY-1215 on lipopolysaccharide (LPS)-activated macrophages for the present study." | ( Inhibition of HDAC6 attenuates LPS-induced inflammation in macrophages by regulating oxidative stress and suppressing the TLR4-MAPK/NF-κB pathways. Gong, ZJ; Jiao, FZ; Wang, LW; Wang, Y; Yang, F; Zhang, HY; Zhang, WB, 2019) | 0.75 |
| " ACY-1215 is well tolerated and led to disease stabilization in 50% of patients treated on a twice-daily dosing schedule." | ( First-in-Class Selective HDAC6 Inhibitor (ACY-1215) Has a Highly Favorable Safety Profile in Patients with Relapsed and Refractory Lymphoma. Amengual, JE; Cremers, S; Jones, S; Lichtenstein, R; Lue, JK; Ma, H; Sawas, A; Shah, B, 2021) | 1.8 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| pyrimidinecarboxylic acid | Any pyrimidine that bears one or more carboxylic acid substituents. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (21)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 9.3005 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 5.3081 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| Interferon beta | Homo sapiens (human) | Potency | 9.3005 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| interferon gamma precursor | Homo sapiens (human) | AC50 | 14.7950 | 0.1280 | 15.1730 | 38.6100 | AID1259418; AID1259420 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (347)
Molecular Functions (96)
Ceullar Components (70)
Bioassays (391)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1473216 | Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1882276 | Inhibition of HDAC5 (unknown origin) using fluorescent peptide 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. |
| AID1876341 | Inhibition of recombinant full length human HDAC3 expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
| AID1363811 | Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| 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 | |||
| AID1832809 | Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| AID1703041 | Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1814039 | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate and trypsin addition by microplate reader based assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1282241 | Inhibition of recombinant HDAC5 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1832830 | Induction of apoptosis in human K562 cells assessed as increase cleaved PARP expression measured after 24 to 72 hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| AID1355700 | Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 10 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. |
| AID1282239 | Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1282254 | Cytotoxicity against human Ramos cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1703049 | Inhibition of recombinant full length human HDAC2 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1679282 | Inhibition of HDAC4 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1473161 | Selectivity ratio of IC50 for recombinant human C-terminal His-tagged/N-terminal Strep2-tagged HDAC8 (1 to 377 residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1882272 | Inhibition of HDAC1 (unknown origin) using fluorescent peptide 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. |
| 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. |
| AID1845772 | Inhibition of HDAC5 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| 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. |
| 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 | |||
| AID1882279 | Inhibition of HDAC8 (unknown origin) using fluorescent peptide 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. |
| AID1814013 | Metal chelating activity assessed as compound-Cu2+ complex formation at 10 to 200 uM incubated for 2 mins followed by pyrocatechol violet addition and further incubated for 10 mins by microplate reader based assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1282242 | Inhibition of recombinant HDAC7 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID767940 | Inhibition of HDAC4 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1901780 | Competitive inhibition of N-terminal His-SUMO tagged zebra fish recombinant HDAC6 catalytic domain 2 transfected with pET28b(+) vector in Escherichia coli BL21 (DE3) RILP cells incubated for 10 mins followed by addition of FITC-M344 measured af ter 10 min | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1718999 | Stability in mouse liver microsomes assessed as parent compound remaining measured after 30 mins | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1703044 | Inhibition of recombinant full length human HDAC3 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1141797 | Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells. |
| AID1832810 | Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| AID1703055 | Selectivity ratio of IC50 for full length recombinant human HDAC3 to IC50 for full length recombinant human HDAC6 | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1407002 | Selectivity ratio of IC50 for human recombinant C-terminal His-tagged full length HDAC3/NcoR2 to IC50 for human recombinant 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. |
| AID1703046 | Inhibition of recombinant full length human HDAC8 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1363784 | Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1282303 | Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of alpha- tubulin acetylation after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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 | |||
| AID1679289 | Inhibition of human HDAC2 expressed in Sf9 insect cells using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1282257 | Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1814034 | Neuroprotection against mouse model of Alzheimer's disease at 1 mg/kg | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1384809 | Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylation of alpha-tubulin at 0.1 to 1 uM after 24 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 | 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
| AID1901765 | Selectivity ratio of IC50 for full length human recombinant HDAC8 to IC50 for full length human recombinant HDAC6 | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1845774 | Inhibition of HDAC7 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1141786 | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells. |
| AID1282248 | Inhibition of recombinant HDAC9 (unknown origin) using AMC labeled AC-peptide as substrate at 10 uM incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1753635 | Inhibition of human HDAC6 preincubated for 15 mins followed by substrate addition by fluorescence-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. |
| 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. |
| AID1739978 | Inhibition of HDAC9 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| 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. |
| AID1882277 | Inhibition of HDAC6 (unknown origin) using fluorescent peptide 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. |
| AID1882274 | Inhibition of HDAC3 (unknown origin) using fluorescent peptide 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. |
| 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. |
| AID1511157 | Inhibition of HDAC in human HL60 cells assessed as increase in acetylation of H3 at 0.08 to 1.6 uM incubated for 24 hrs by western blot analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
| 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. |
| AID1363796 | Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1849173 | Inhibition of HDAC6 in human HL-60 cells assessed as increase in Ac-H3 level at 0.9 uM incubated for 24 hrs by immunoblot 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. |
| AID1282233 | Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC6 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1882260 | Inhibition of HDAC6 (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | A review on the treatment of multiple myeloma with small molecular agents in the past five years. |
| 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 | |||
| AID1473146 | Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1558032 | Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr | 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. |
| AID1739981 | Inhibition of recombinant human HDAC11 using fluorogenic HDAC substrate class 2a incubated for 30 mins by fluorimetry | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1703047 | Inhibition of recombinant full length human HDAC11 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1895832 | Inhibition of HDAC6 (unknown origin) using FTS as substrate pre-incubated with compound for 10 mins followed by substrate addition measured after 30 mins by microtiter plate reader 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). |
| AID1363817 | Cytotoxicity against human BCP-ALL cells derived from patient 4 after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1141787 | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells. |
| AID767941 | Inhibition of HDAC3 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1845771 | Inhibition of HDAC4 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1739979 | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1363806 | Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1814029 | Anti-alzheimer activity against amyloid beta (25 to 35) induced working memory deficit mouse assessed as step-through latency time to enter dark compartment at 0.3 to 3 mg/kg, ip administered for 7 days and measured on day 9 days by passive avoidance test | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1703050 | Inhibition of recombinant full length human HDAC4 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1363809 | Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1363795 | Inhibition of HDAC6 in human SEM cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1363797 | Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| 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. |
| AID1473156 | Selectivity ratio of IC50 for full length recombinant human C-terminal GST-tagged HDAC2 to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1849166 | Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay | 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. |
| AID1473149 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| 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. |
| AID1679288 | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1280285 | Selectivity ratio of IC50 for class1 HDAC (unknown origin) to IC50 for HDAC6 (unknown origin) | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors. |
| 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 | |||
| AID1679279 | Inhibition of HDAC9 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| 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. |
| AID1282229 | Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| 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. |
| AID1282256 | Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID767937 | Inhibition of HDAC8 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID767935 | Inhibition of HDAC9 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1703045 | Inhibition of recombinant full length human HDAC6 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1535345 | Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma. |
| AID1864697 | AUC(0 to infinity) in CD-1 mouse at 5 mg/kg, iv measured after 0.083 to 24 hrs by LC-MS/MS analysis | |||
| AID1814024 | Toxicity in mouse model of Alzheimer's disease assessed as drug tolerability at 0.3 to 3 mg/kg, ip measured after 7 days | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1832806 | Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| 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. |
| 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. |
| AID1901764 | Inhibition of full length human recombinant HDAC11 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1813992 | 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 assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1901805 | Cytotoxicity against human HD-MB03 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1363787 | Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1578486 | Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1 | Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
| AID1901766 | Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1282255 | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID767939 | Inhibition of HDAC5 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1441700 | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1739976 | Inhibition of HDAC5 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| 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. |
| AID1739972 | Inhibition of HDAC1 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1363816 | Cytotoxicity against human BCP-ALL cells derived from patient 3 after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1679290 | Inhibition of HDAC1 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1473215 | Antiproliferative activity against human U266 cells after 48 hrs by SRB assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| 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. |
| AID1890307 | Inhibition of recombinant human HDAC1 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
| 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. |
| AID1363815 | Cytotoxicity against human BCP-ALL cells derived from patient 2 after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1558034 | Selectivity index, ratio of IC50 for recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells to IC50 for recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected | 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. |
| AID1876340 | Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
| AID1534493 | AUC (0 to 24 hrs) in C57BL/6 mouse kidney at 40 mg/kg, po administered via gavage by LC-MS/MS 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. |
| AID1511156 | Inhibition of HDAC6 in human HL60 cells assessed as increase in acetylation of alpha tubulin at 0.08 to 1.6 uM incubated for 24 hrs by western blot analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8 | Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors. |
| 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 | |||
| AID1200994 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
| AID1679275 | Inhibition of human sirtuin 2 using fluoro-lysine sirtuin 2 deacetylase as substrate incubated for 60 mins by fluorimetry | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| 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. |
| AID1390013 | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID1282259 | Cytotoxicity against human H460 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1363807 | Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1679284 | Selectivity ratio of IC50 for human HDAC2 expressed in Sf9 insect cells to IC50 for HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1901763 | Inhibition of full length human recombinant HDAC8 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1876343 | Inhibition of recombinant full length human HDAC8 expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
| AID1718998 | Stability in human liver microsomes assessed as parent compound remaining measured after 30 mins | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1534443 | Cytotoxicity against human A549 cells after 72 hrs by MTT 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. |
| 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. |
| AID1282260 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1390010 | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID1473164 | Selectivity ratio of IC50 for recombinant human N-terminal Strep2-tagged HDAC11 (1 to 347 residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| 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. |
| AID1363814 | Cytotoxicity against human BCP-ALL cells derived from patient 1 after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1535346 | Growth inhibition of human U266 cells after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma. |
| AID1428507 | Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| 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. |
| AID1534494 | AUC (0 to 24 hrs) in C57BL/6 mouse plasma at 40 mg/kg, po administered via gavage by LC-MS/MS 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. |
| AID1849167 | Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay | 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. |
| 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. |
| AID1739973 | Inhibition of human HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1864693 | Half life in CD-1 mouse at 5 mg/kg, iv measured after 0.083 to 24 hrs by LC-MS/MS analysis | |||
| 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 | |||
| AID1864730 | Inhibition of HDAC2 (unknown origin) using FTS as substrate preincubated for 6 mins followed by substrate addition measured after 60 secs | |||
| AID1814033 | Cognitive enhancing effect in mouse model of Alzheimer's disease at 1 mg/kg | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1764270 | Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay | 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. |
| AID1814032 | Anti-alzheimer activity against amyloid beta (25 to 35) induced working memory deficit mouse assessed as step-through latency time to enter dark compartment at 1 mg/kg, ip administered for 7 days and measured on day 9 days in presence of melatonin and fer | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1473157 | Selectivity ratio of IC50 for full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1200996 | Selectivity index, ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
| AID1876342 | Inhibition of recombinant full length human HDAC6 expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
| AID1753636 | Inhibition of human HDAC1 preincubated for 15 mins followed by substrate addition by fluorescence-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. |
| AID1882275 | Inhibition of HDAC4 (unknown origin) using fluorescent peptide 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. |
| 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. |
| AID1537571 | Inhibition of HDAC6 (unknown origin) | 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. |
| AID1679283 | Selectivity ratio of IC50 for C-terminal His-tagged human HDAC3/N-terminal GST tagged human NCOR2 to IC50 for HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1282240 | Inhibition of recombinant HDAC4 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1679281 | Inhibition of HDAC5 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| 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. |
| AID1679285 | Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| 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. |
| AID1679274 | Inhibition of HDAC8 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| 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. |
| AID1473153 | Inhibition of recombinant human N-terminal Strep2-tagged HDAC11 (1 to 347 residues) expressed in baculovirus infected insect cells using Boc-Lys(TFA)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1864731 | Inhibition of HDAC3 (unknown origin) using FTS as substrate preincubated for 6 mins followed by substrate addition measured after 60 secs | |||
| AID1849172 | Inhibition of HDAC6 in human HL-60 cells assessed as increase in alpha tubulin acetylation at 0.9 uM incubated for 24 hrs by immunoblot 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. |
| AID767934 | Inhibition of HDAC10 (unknown origin) | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1535340 | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma. |
| AID1282231 | Inhibition of human recombinant HDAC8 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1282253 | Cytotoxicity against human K562 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1282245 | Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1814038 | Inhibition of HDAC3 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate and trypsin addition by microplate reader based assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1473150 | Inhibition of recombinant human C-terminal His-tagged/N-terminal Strep2-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1915605 | Cytotoxicity against human KCL-22 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
| AID1441630 | Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA preincubated for 10 mins followed by substrate addition measured after 10 mins | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1813996 | Antioxidant activity of compound assessed as trolox equivalent of AAPH radical scavenging activity at 2 to 4 uM preincubated for 15 mins followed by AAPH addition and measured every 2 mins for 90 mins by ORAC-fluorescein assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| 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. |
| 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. |
| 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 | |||
| AID1882281 | Inhibition of HDAC11 (unknown origin) using fluorescent peptide 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. |
| AID1901767 | Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1537570 | Inhibition of HDAC1 (unknown origin) | 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. |
| 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. |
| AID1739974 | Inhibition of human C-terminal His-tagged HDAC3 (1 to 428 residues)/human N-terminal GST-tagged NcoR2 (395 to 489 residues) expressed in sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and me | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1864725 | Binding affinity to recombinant HDAC2 (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 | |||
| 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. |
| AID1578487 | Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1 | Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. |
| 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. |
| 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. |
| AID1473159 | Selectivity ratio of IC50 for recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1845769 | Inhibition of HDAC2 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1141788 | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells. |
| AID1282232 | Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC6 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1849168 | Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay | 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. |
| AID1739977 | Inhibition of HDAC7 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1679287 | Cytotoxicity against human MM1.S cells incubated for 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1718995 | Inhibition of human HDAC6 (unknown origin) using RHKKAc as substrate by fluorescence method | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1282251 | Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1282250 | Cytotoxicity against human U266 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1473154 | Inhibition of recombinant human N-terminal His-tagged SIRT1 (1 to 747 end residues) expressed in Escherichia coli using Ac-RHK-K(Ac)-AMC as substrate after 30 mins in presence of NAD+ by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1814027 | Anti-alzheimer activity against amyloid beta (25 to 35) induced working memory deficit mouse assessed as increase in spontaneous alternation performance by measuring total number of arm entries at 0.3 mg/kg, ip administered for 7 days and measured on day | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1473147 | Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using Boc-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1890308 | Inhibition of recombinant human HDAC6 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. |
| AID1473145 | Inhibition of full length recombinant human C-terminal GST-tagged HDAC2 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| 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. |
| AID1537572 | Selectivity index, ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC6 (unknown origin) | 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. |
| AID1534491 | AUC (0 to 24 hrs) in C57BL/6 mouse lung at 40 mg/kg, po administered via gavage by LC-MS/MS 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. |
| 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. |
| 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. |
| AID1473148 | Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in insect cells using Boc-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1363786 | Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1917532 | Antiproliferative activity against human KM12 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. |
| AID1363818 | Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1390012 | Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate additi | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID1473160 | Selectivity ratio of IC50 for recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1282252 | Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1813993 | 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 assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1282261 | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1473217 | Antiproliferative activity against human HS5 cells after 48 hrs by SRB assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1845770 | Inhibition of HDAC3 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1473165 | Selectivity ratio of IC50 for recombinant human N-terminal His-tagged SIRT1 (1 to 747 end residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1845773 | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1428508 | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID1282247 | Inhibition of recombinant HDAC7 (unknown origin) using AMC labeled AC-peptide as substrate at 10 uM incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1679286 | Cytotoxicity against human OPM-2 cells incubated for 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1832811 | Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| AID1832808 | Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| AID1473214 | Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| 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. |
| AID1864663 | Selectivity index, ratio of IC50 for recombinant HDAC1(unknown origin) to IC50 for full length recombinant human HDAC6 | |||
| AID1282301 | Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 1000 nM after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1882273 | Inhibition of HDAC2 (unknown origin) using fluorescent peptide 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. |
| AID1915604 | Cytotoxicity against human SEM cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
| AID1390011 | Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID1718994 | Inhibition of LSD1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1282238 | Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1753637 | Selectivity index, ratio of IC50 for inhibition of human HDAC1 to IC50 for inhibition of human HDAC6 | 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. |
| AID767942 | Inhibition of HDAC2 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1814016 | Neurotoxicity in mouse HT-22 cells assessed as cell survival at 10 uM incubated for 48 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID767938 | Inhibition of HDAC6 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| 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. |
| AID1282230 | Inhibition of human recombinant HDAC6 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1864689 | Cmax in CD-1 mouse at 5 mg/kg, iv measured after 0.083 to 24 hrs by LC-MS/MS analysis | |||
| AID1864729 | Inhibition of HDAC1 (unknown origin) using FTS as substrate preincubated for 6 mins followed by substrate addition measured after 60 secs | |||
| AID1739975 | Inhibition of HDAC4 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1363808 | Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1814015 | Metal chelating activity assessed as Fe2+ -ferrozoine complex formation at 10 to 200 uM preincubated for 2 mins followed by ferrozine addition and further incubated for 10 mins by microplate reader based assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1473143 | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1282246 | Inhibition of recombinant HDAC5 (unknown origin) using AMC labeled AC-peptide as substrate at 10 uM incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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 | |||
| AID1718996 | Inhibition of human HDAC1 at 1uM using RHKKAc as substrate by fluorescence method relative to control | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1363819 | Antiproliferative activity against human SEM cells at IC50 to 2 times IC50 after 24 to 72 hrs by trypan exclusion method | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1282258 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1679277 | Inhibition of human sirtuin 1 using fluorogenic HDAC substrate incubated for 20 mins by fluorimetry | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1282262 | Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1363810 | Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| 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. |
| AID1845776 | Inhibition of HDAC9 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1718997 | Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1703043 | Cytotoxicity against human MRC9 cells measured after 72 hrs by spectrophotometer method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1441632 | Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1363812 | Cytotoxicity against human RPMI18226 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1917533 | Antiproliferative activity against human HCT-116 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. |
| AID1384810 | Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as increase in acetylation of histone H3 at 0.1 to 1 uM after 24 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16 | 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes. |
| AID1282243 | Inhibition of recombinant HDAC9 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1363813 | Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1282297 | Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of alpha- tubulin acetylation after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1845768 | Inhibition of HDAC1 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1282249 | Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate at 10 uM incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1363785 | Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1917535 | Antiproliferative activity against human SU-DHL-6 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. |
| AID1473151 | Inhibition of HDAC9 (unknown origin) | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| 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. |
| AID1813994 | Selectivity ratio of IC50 for recombinant HDAC3 (unknown origin) to IC50 for recombinant HDAC6 (unknown origin) | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1703056 | Inhibition of N-terminal 6 His-SUMO tagged Zebrafish HDAC6 CD2 domain expressed in Escherichia coli BL21(DE3) RILP pretreated for 10 mins before FITC-M344 addition and measured after 10 mins by fluorescence polarization competition assay | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. |
| AID1901762 | Inhibition of full length human recombinant HDAC6 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1282244 | Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1535339 | Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma. |
| 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. |
| AID1876339 | Cytotoxicity against human MRC9 cells assessed as cell viability incubated for 72 hrs by Cell titer- blue assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
| AID1832807 | Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| AID1814014 | Metal chelating activity compound-Zn2+ complex formation at 10 to 200 uM preincubated for 2 mins followed by di-thizone addition by microplate reader based assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1901786 | Binding affinity to full length HDAC6-NanoLuc fusion protein (unknown origin) expressed in HeLa cells assessed as residence time by NanoBRET assay | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1390009 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID767936 | Inhibition of HDAC7 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1473158 | Selectivity ratio of IC50 for recombinant human C-terminal His-tagged/N-terminal GST-tagged HDAC4 (627 to 1084 residues) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1390014 | Inhibition of full length recombinant human C-terminal His-tagged HDAC8 expressed in baculovirus infected sf9 cells using Boc-Lys-(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID1901768 | Cytotoxicity against human MRC9 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1390015 | Selectivity ratio of IC50 for full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. |
| AID1719020 | Antitumour activity against human MM1.S cells xenografted in SCID mouse assessed as tumour growth inhibition at 50 mg/kg, ip for 12 days relative to control | 2021 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 34 | Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. |
| AID1363798 | Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1917534 | Antiproliferative activity against human T47D 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. |
| AID1845775 | Inhibition of HDAC8 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition by microtiter plate reader 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. |
| AID1679278 | Inhibition of human HDAC11 using fluorogenic HDAC substrate incubated for 30 mins by fluorimetry | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1441699 | Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1441631 | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| 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. |
| 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. |
| 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. |
| AID1407001 | Selectivity ratio of IC50 for human recombinant C-terminal His/FLAG-tagged full length HDAC2 to IC50 for human recombinant 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. |
| 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. |
| AID1813995 | Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins under dark condition by microplate reader based assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| AID1882280 | Inhibition of HDAC9 (unknown origin) using fluorescent peptide 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. |
| 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 | |||
| AID1534492 | AUC (0 to 24 hrs) in C57BL/6 mouse liver at 40 mg/kg, po administered via gavage by LC-MS/MS 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. |
| AID1363799 | Inhibition of chymotrypsin-like activity of 20S proteasome in imatinib-resistant human SUP-B15 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1141798 | Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells. |
| AID1876344 | Inhibition of recombinant full length HDAC11 (unknown origin) expressed in insect Sf9 cells by EMSA analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia. |
| AID1901761 | Inhibition of full length human recombinant HDAC3 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Discovery of HDAC6-Selective Inhibitor NN-390 with |
| AID1428506 | Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. |
| AID767943 | Inhibition of HDAC1 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | 2013 | Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16 | Development and therapeutic implications of selective histone deacetylase 6 inhibitors. |
| AID1363794 | Inhibition of HDAC6 in human HL60 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1473162 | Selectivity ratio of IC50 for HDAC9 (unknown origin) to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1363842 | Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at 1.6 uM after 18 hrs by FACS analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| 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 | |||
| AID1363838 | Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at IC50 after 18 hrs by fluorescence microscopic method | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1814037 | Anti-alzheimer activity against amyloid beta (25 to 35) induced working memory deficit in mouse assessed as increase in spontaneous alternation performance at 1 mg/kg, ip administered for 7 days and measured on day 8 by Y-maze test | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects |
| 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 | |||
| AID1363782 | Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| AID1558033 | Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a | 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. |
| AID1739983 | Inhibition of HDAC8 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight. |
| AID1864726 | Binding affinity to recombinant HDAC3 (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 | |||
| AID1200995 | Selectivity index, ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC6 (unknown origin) | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors. |
| AID1473155 | Selectivity ratio of IC50 for full length recombinant human C-terminal FLAG/His-tagged HDAC1 to IC50 for full length recombinant human N-terminal GST-tagged HDAC6 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1864732 | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 6 mins followed by substrate addition measured after 60 secs | |||
| AID1363783 | Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. |
| 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. |
| AID1473144 | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf21 cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | (N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo. |
| AID1764269 | Inhibition of Class 1/2b HDAC in human HL-60 cells by HDAC-Glo assay | 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. |
| AID1832819 | Induction of apoptosis in human K562 cells assessed as apoptosis at 6 uM after 24 to 72 hrs using annexin V/PI followed by flow cytometry | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. |
| 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. |
| AID1882278 | Inhibition of HDAC7 (unknown origin) using fluorescent peptide 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. |
| AID1679280 | Inhibition of HDAC7 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent advances in the discovery of potent and selective HDAC6 inhibitors. |
| AID1282237 | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1282295 | Toxicity in NOD/SCID mouse xenografted with human Ramos cells assessed as death at 40 mg/kg, po q2d for 6 days | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| 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. |
| AID1346134 | Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs)) | 2012 | Blood, Mar-15, Volume: 119, Issue:11 | Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. |
| AID1346068 | Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs)) | 2012 | Blood, Mar-15, Volume: 119, Issue:11 | Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. |
| AID1346082 | Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs)) | 2012 | Blood, Mar-15, Volume: 119, Issue:11 | Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. |
| AID1346032 | Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs)) | 2012 | Blood, Mar-15, Volume: 119, Issue:11 | Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. |
| AID1346077 | Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs)) | 2012 | Blood, Mar-15, Volume: 119, Issue:11 | Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (116)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 63 (54.31) | 24.3611 |
| 2020's | 53 (45.69) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 28.30
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (28.30) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (0.85%) | 5.53% |
| Reviews | 9 (7.69%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 107 (91.45%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||