Assay ID | Title | Year | Journal | Article |
AID1176365 | Inhibition of human recombinant SIRT2 at 25 uM | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton. |
AID1119564 | Inhibition of SIRT1 in human MCF7 cells assessed as increase in acetylation of H3-K9 up to 50 uM after 24 hrs by Western blot analysis | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID708886 | Induction of apoptosis in human U937 cells after 45 hrs by flow cytometry | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1371048 | Antiparasitic activity against Schistosoma mansoni assessed cell viability at 20 uM after 4 days | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID708884 | Antiproliferative activity against human MOLT4 cells at 25 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID460417 | Protection against mutant PABPN1-induced toxicity in transgenic Caenorhabditis elegans coexpressing nuclear GFP and PABPN1-A13 assessed as inhibition of nuclear collapse | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues. |
AID1371078 | Antiparasitic activity against Schistosoma mansoni assessed as pairing at 20 uM after 5 days relative to control | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1530562 | Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition at 10 uM after 48 hrs by SYBR green1 staining based flow cytometry relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID708878 | Antiproliferative activity against human MOLT4 cells at 100 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1322352 | Selectivity ratio of IC50 for recombinant human His6-tagged SIRT3 to IC50 for recombinant human His6-tagged SIRT2 | | | |
AID460426 | Effect on nuclear integrity in transgenic Caenorhabditis elegans coexpressing nuclear GFP and normal PABPN1-A10 | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues. |
AID1280430 | Inhibition of His-tagged recombinant human SIRT2 after 60 mins by fluorescence assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study. |
AID708882 | Antiproliferative activity against human RKO cells at 25 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1119572 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2-M phase at 50 uM after 24 hrs by flow cytometry (Rvb = 22.6 %) | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID708891 | Induction of apoptosis in human U937 cells at 5 uM after 45 hrs by flow cytometry | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID708881 | Antiproliferative activity against human MOLT4 cells at 50 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1280429 | Inhibition of His-tagged recombinant human SIRT1 after 60 mins by fluorescence assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study. |
AID708880 | Antiproliferative activity against human RKO cells at 50 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1322348 | Inhibition of recombinant human His6-tagged SIRT3 using H2N-HK-[Nepsilon-acetyl-lysine]-LM-COOH as substrate incubated for 10 mins in presence of beta-NAD+ by HPLC based assay | | | |
AID708873 | Cytotoxicity against human 30PT cells after 72 hrs by celltiter-glo luminescent assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID708877 | Antiproliferative activity against human MOLT4 cells at 100 uM by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID708876 | Cytotoxicity against human CRO cells after 72 hrs by celltiter-glo luminescent assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1119565 | Inhibition of SIRT2 in human MCF7 cells assessed as increase in hyperacetylation of alpha-tubulin up to 50 uM after 24 hrs by Western blot analysis | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID700824 | Inhibition of SIRT1 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| SIRT1 modulation as a novel approach to the treatment of diseases of aging. |
AID1119568 | Antiproliferative activity against human MCF7 cells at 30 uM after 24 to 72 hrs | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID1119569 | Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase at 50 uM after 24 hrs by flow cytometry (Rvb = 0.3 %) | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID1119558 | Inhibition of recombinant human N-tagged GST-SIRT1 fusion protein using fluorescent ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID460415 | Inhibition of human recombinant SIRT1 by Flour de Lys assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues. |
AID708874 | Cytotoxicity against human 30P cells after 72 hrs by celltiter-glo luminescent assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1371058 | Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi at 5 uM by Alamar Blue assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1119567 | Inhibition of SIRT1 in human MCF7 cells assessed as increase in acetylation of p53 at lys 382 at 50 uM after 24 hrs by Western blot analysis | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID708883 | Antiproliferative activity against human MDA-MB-231 cells at 25 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1322351 | Selectivity ratio of IC50 for recombinant human His6-tagged SIRT3 to IC50 for recombinant human GST or His6-tagged SIRT1 | | | |
AID1119570 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 50 uM after 24 hrs by flow cytometry (Rvb = 43.5 %) | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID708893 | Inhibition of human N-terminal GST-tagged SIRT1 expressed in Escherichia coli using Arg-His- Lys-Lys(Ac) as substrate after 1 hr by Fluor de Lys fluorescence based assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1322346 | Inhibition of recombinant human GST or His6-tagged SIRT1 using H2N-HK-[Nepsilon-acetyl-lysine]-LM-COOH as substrate incubated for 10 mins in presence of beta-NAD+ by HPLC based assay | | | |
AID1371059 | Inhibition of recombinant Trypanosoma cruzi Sir2rp3 | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID735756 | Inhibition of human His6-tagged SIRT2 expressed in Escherichia coli BL21(DE3) assessed as inhibition of ZMAL conversion to ZML after 4 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3. |
AID1119571 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 50 uM after 24 hrs by flow cytometry (Rvb = 30.8 %) | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID708888 | Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 25 uM after 40 hrs by flow cytometry | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID708875 | Cytotoxicity against human CRC 1.1 cells after 72 hrs by celltiter-glo luminescent assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID708890 | Induction of apoptosis in human U937 cells at 50 uM after 45 hrs by flow cytometry | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID1317158 | Inhibition of recombinant human His-tagged SIRT1 assessed as inhibition of deacetylase activity measured after 60 mins by Fluor de Lys assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | How much successful are the medicinal chemists in modulation of SIRT1: A critical review. |
AID708879 | Antiproliferative activity against human MDA-MB-231 cells at 50 uM after 24 to 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID723620 | Inhibition of human Sirt5 desuccinylation activity using SKEYFS-succinylLys-QK as substrate at 100 uM after 60 mins by glutamate dehydrpgenase-coupled assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibition of the human deacylase Sirtuin 5 by the indole GW5074. |
AID700823 | Inhibition of SIRT2 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| SIRT1 modulation as a novel approach to the treatment of diseases of aging. |
AID1119559 | Inhibition of recombinant human full length SIRT2 using fluorescent ZMAL as substrate after 4 hrs by homogeneous fluorescent deacetylase assay | 2012 | MedChemComm, Mar-01, Issue:3
| The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors. |
AID1322347 | Inhibition of recombinant human His6-tagged SIRT2 using H2N-HK-[Nepsilon-acetyl-lysine]-LM-COOH as substrate incubated for 12 mins in presence of beta-NAD+ by HPLC based assay | | | |
AID1322349 | Inhibition of recombinant human GST-tagged SIRT5 using CH3CONH-AR-[Nepsilon-succinyl-lysine]-ST-CONH2 as substrate incubated for 5 mins in presence of beta-NAD+ by HPLC based assay | | | |
AID735757 | Inhibition of human GST-tagged SIRT1 expressed in Escherichia coli BL21(DE3) assessed as inhibition of ZMAL conversion to ZML after 4 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3. |
AID460416 | Inhibition of human recombinant SIRT2 by Flour de Lys assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues. |
AID1371049 | Antiparasitic activity against Schistosoma mansoni assessed as cumulative egg reduction at 20 uM | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
AID1322350 | Inhibition of recombinant human His6-tagged SIRT6 using H2N-EALPK-[Nepsilon-myristoyl-lysine]-TGGPQ-CONH2 as substrate incubated for 12 mins in presence of beta-NAD+ by HPLC based assay | | | |
AID1530563 | Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
AID708892 | Inhibition of human SIRT2 expressed in Escherichia coli using Gln-Pro-Lys-Lys(Ac) as substrate after 1 hr by Fluor de Lys fluorescence based assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
| Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. |
AID723626 | Inhibition of human Sirt5 deacetylation activity using FKRGVL-acetylLys-EYGVKV as substrate at 100 uM after 60 mins by glutamate dehydrogenase-coupled assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Inhibition of the human deacylase Sirtuin 5 by the indole GW5074. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |