| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1558070 | Half life in Wistar Han rat at 2 mg/kg, iv | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558080 | Drug uptake in rat brain at 3 mg/kg, po measured after 24 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1378940 | Selectivity index, ratio of Ki for human lysosomal beta-hexosaminidase to Ki for human O-GlcNAcase | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Tau protein aggregation in Alzheimer's disease: An attractive target for the development of novel therapeutic agents. |
| AID1527147 | Inhibition of human O-GlcNAcase | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Sugar Kick Prevents Memory Impairment. |
| AID1558051 | AUC (0 to 24 hrs) in rat brain at 10 mg/kg, po measured upto 24 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498256 | Reduction in tau protein phosphorylation at Thr231 in Sprague-Dawley rat brain CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498248 | Reduction in tau protein phosphorylation at Ser422 position in NGF-differentiated rat PC12 cells at 100 uM after 4 hrs by Western blot analysis relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558072 | Volume of distribution at steady state in Wistar Han rat at 2 mg/kg, iv or 10 mg/kg, po | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558108 | Inhibition of Nav1.5 (unknown origin) | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1860603 | Neuroprotective activity against amyloid beta (1 to 42)-induced cognitive impairement in ICR mouse assessed as decrease in spontaneous alteration at 50 mg/kg, ip for 3 days by Y-maze test | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1624713 | Inhibition of OGA in mouse NIH/3T3 cells assessed as increase in O-GlcNAcylation at 20 uM after 24 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
| Ac |
| AID498253 | Reduction in tau protein phosphorylation at Ser396 in Sprague-Dawley rat brain CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1378939 | Competitive inhibition of human O-GlcNAcase using 4-Np-GlcNAc as substrate after 5 mins by Dixon plot analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Tau protein aggregation in Alzheimer's disease: An attractive target for the development of novel therapeutic agents. |
| AID1558054 | Tmax in rat brain at 10 mg/kg, po measured upto 24 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1860584 | Inhibition of human recombinant OGA pretreated for 20 mins followed by 4-Methylumbelliferyl N-acetyl-(3-D-glucosaminide substrate addition by fluorometer | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1558107 | Displacement of MK-0499 from human ERG | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498263 | Reduction in tau protein phosphorylation at Ser396 in Sprague-Dawley rat brain epitope of CA1 region at 200 mg/kg, po by DAPI staining relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558111 | Inhibition of CYP2D6 (unknown origin) | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558062 | Inhibition of recombinant human OGA | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498259 | Decrease in pSer396 immunoreactivity in Sprague-Dawley rat brain epitops of CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558112 | Inhibition of CYP2C9 (unknown origin) | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558058 | Inhibition of OGA (unknown origin) by cell based assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498249 | Reduction in tau protein phosphorylation at Ser262 position in NGF-differentiated rat PC12 cells at 100 uM after 4 hrs by Western blot analysis relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498257 | Increase in O-GlcNAc immunoreactivity in Sprague-Dawley rat brain nucleus at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558066 | AUCN in Wistar Han rat at 10 mg/kg, po | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558075 | Oral bioavailability in Wistar Han rat at 10 mg/kg | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498237 | Inhibition of human lysosomal beta-hexosaminidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558142 | Fraction unbound in human plasma | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558077 | Elevation of O-protein in rat brain at 3 mg/kg, po measured after 8 hrs relative to control | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558110 | Inhibition of CYP3A4 (unknown origin) | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558068 | Clearance in Wistar Han rat at 2 mg/kg, iv | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498245 | Induction of O-GlcNAc level in NGF-differentiated rat PC12 cells at >25 uM by Western blot analysis | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558065 | Fraction unbound in Wistar Han rat plasma at 2.5 uM by equilibrium dialysis | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1860597 | AUClast in ICR mouse brain at 50 mg/kg, ip after 24 hrs by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1860585 | Inhibition of human recombinant beta-hexosaminidase at 10 uM pretreated with compound followed by 4-nitrophenyl Nacetyl-beta-D-glucosaminide substrate addition by fluorometer | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1558081 | Ratio of drug uptake in rat brain to plasma at 3 mg/kg, po measured after 8 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498242 | Binding affinity to Bacteroides thetaiotaomicron N-acetyl-glucosaminidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498239 | Increase in O-GlcNAc level in Sprague-Dawley rat brain pyramidal cell layer of CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558052 | Increase in O-protein AUC in rat brain at 10 mg/kg, po measured upto 24 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1371342 | Inhibition of recombinant human O-GlcNAcase using pNP-GlcNAc as substrate measured for 5 mins by UV-VIS spectrophotometer | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
| AID1558063 | Inhibition of OGA in rat PC12 cells assessed as OGlcNAcylated protein level incubated for 24 hrs by ELISA | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558064 | Inhibition of human beta hexosaminidase assessed as inhibitory constant using 4-methylumbelliferyl N-acetyl-beta-D-glucosaminide dihydrate as substrate measured every 60 sec for 45 mins by fluorescence spectrophotometry | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1860583 | Inhibition of human recombinant OGA at 10 uM pretreated for 20 mins followed by 4-Methylumbelliferyl N-acetyl-(3-D-glucosaminide substrate addition by fluorometer | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1558061 | Fraction unbound in human plasma at 2.5 uM by equilibrium dialysis | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498234 | Inhibition of Vibrio cholerae glycoside hydrolase NagZ | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498233 | Inhibition of Saccharomyces cerevisiae alpha-glucosidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558059 | Apparent permeability in pig LLC-PK1 cells transfected with MDR1 | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498264 | Reduction in tau protein phosphorylation at Thr231 in Sprague-Dawley rat brain epitope of CA1 region at 200 mg/kg, po by DAPI staining relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498250 | Induction of O-GlcNAc level in rat at 50 mg/kg, iv by Western blot analysis | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1371344 | Inhibition of O-GlcNAcase in rat PC12 cells assessed as induction of OGlcNAcylation after 24 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
| AID1860600 | Invivo inhibition of OGA in amyloid-beta-induced ICR mouse assessed as decrease in 4-MUF level at 50 mg/kg, ip for 3 days by fluorescence analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1558079 | Drug uptake in rat brain at 3 mg/kg, po measured after 8 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498252 | Reduction in tau protein phosphorylation at Ser396 position in NGF-differentiated rat PC12 cells after 4 hrs by Western blot analysis relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498251 | Inhibition of beta-hexosaminidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498235 | Inhibition of Kluyveromyces lactis glycoside hydrolase beta-galactosidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498261 | Decrease in pSer396 immunoreactivity in Sprague-Dawley rat brain pyramidal cell layer of CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498236 | Selectivity for human O-GlcNAcase over human lysosomal beta-hexosaminidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1860598 | Ratio of drug level in ICR mouse brain to plasma at 50 mg/kg, ip after 24 hrs by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1558053 | Elevation of O-protein in rat brain at 10 mg/kg, po measured after 24 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1624736 | Inhibition of human OGA | 2019 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
| Ac |
| AID498260 | Decrease in pThr231 immunoreactivity in Sprague-Dawley rat brain epitops of CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498247 | Reduction in tau protein phosphorylation at Thr231 position in NGF-differentiated rat PC12 cells at 100 uM after 4 hrs by Western blot analysis relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558078 | Elevation of O-protein in rat brain at 3 mg/kg, po measured after 24 hrs relative to control | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558109 | Inhibition of Cav1.2 (unknown origin) | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498240 | Inhibition of Canavalia ensiformis alpha-mannosidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498255 | Increase in O-GlcNAc immunoreactivity in Sprague-Dawley rat brain CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498238 | Inhibition of human O-GlcNAcase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498246 | Reduction in tau protein phosphorylation at Ser396 position in NGF-differentiated rat PC12 cells at 100 uM after 4 hrs by Western blot analysis relative to control | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558082 | Ratio of drug uptake in rat brain to plasma at 3 mg/kg, po measured after 24 hrs | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID498262 | Decrease in pThr231 immunoreactivity in Sprague-Dawley rat brain pyramidal cell layer of CA1 region at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1371343 | Selectivity ratio of Ki for human lysosomal beta-hexosaminidase to Ki for recombinant human O-GlcNAcase | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
| AID498241 | Inhibition of Thermotoga maritima alpha-galactosidase | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558113 | Activation of PXR (unknown origin) assessed as CYP3A4 induction | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1558060 | Ratio of Cmax in brain to plasma in rat at 10 mg/kg, po | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1860596 | AUClast in ICR mouse plasma at 50 mg/kg, ip after 24 hrs by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1860586 | Cytotoxicity against mouse HT-22 cells assessed as cell viability at 10 uM after 18 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID1860606 | Anti-alzheimer activity in mouse model assessed as decrease in amyloid beta level in brain at 50 mg/kg, ip for 3 days by ELISA relative to control | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID498243 | Induction of O-GlcNAc level in NGF-differentiated rat PC12 cells after 24 hrs by Western blot analysis | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498258 | Increase in O-GlcNAc immunoreactivity in Sprague-Dawley rat brain perikaryon at 200 mg/kg, po by DAPI staining | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID1558057 | Inhibition of recombinant human OGA expressed in Escherichia coli assessed as inhibitory constant using 4-MUGlcNAc as substrate incubated for 20 mins by fluorescence based assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies. |
| AID1860587 | Permeability of compound by PAMPA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Structure-based discovery and development of novel O-GlcNAcase inhibitors for the treatment of Alzheimer's disease. |
| AID498244 | Induction of O-GlcNAc level in NGF-differentiated rat PC12 cells after 24 hrs by densitometric analysis | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID498254 | Increase in pSer396 immunoreactivity in NGF-differentiated rat PC12 cells after 4 hrs by Western blot analysis | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2008 | Nature chemical biology, Aug, Volume: 4, Issue:8
| A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |