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. |
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. |
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. |
AID669480 | Selectivity ratio of IC50 for rat recombinant KAT2 to IC50 for human recombinant KAT2 | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID727189 | Inhibition of human KAT1 using L-kynurenine as substrate measured after 16 hrs by SpectraMax plate reader analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID669468 | Drug level in Sprague-Dawley rat cerebrospinal fluid at 10 mg/kg, sc after 0.25 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669477 | Inhibition of human KAT1 | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669470 | Free plasma concentration in Sprague-Dawley rat at 10 mg/kg, sc after 0.25 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669483 | Ratio of free drug level in cerebrospinal fluid to brain in Sprague-Dawley rat at 10 mg/kg, sc after 0.25 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID727185 | fAUC in Sprague-Dawley rat brain at 10 mg/kg, sc by equilibrium dialysis method | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID727182 | Ratio of Kinact to Ki for rat KAT2 using L-kynurenine as substrate by SpectraMax plate reader analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID738356 | Inhibition of human KAT2 using L-kynurenine as substrate measured every 5 mins for 16 hours by UV-visible spectra analysis | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency. |
AID669482 | Ratio of free drug level in plasma to brain in Sprague-Dawley rat at 10 mg/kg, sc after 0.25 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID727191 | Inhibition of human KAT2 using L-kynurenine as substrate measured after 15-20 hrs by SpectraMax plate reader analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID727183 | Unbound fraction in Sprague-Dawley rat brain at 10 mg/kg, sc by equilibrium dialysis method | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID727179 | Binding affinity to C-terminal hexa histidine tagged full length human KAT2 K240S/F241G mutant harboring C-terminal thrombin cleavage site at 1 mM after 2 hrs by X-ray crystallography in presence of 2 mM PLP | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID669471 | Fraction unbound in rat brain at 1 uM by equilibrium dialysis method | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669481 | Lipophilicity, log D of the compound | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669476 | Inhibition of rat recombinant KAT2 assessed as conversion of L-kynurenine into kynurenic acid after 15 to 20 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID727186 | Inhibition of human KAT3 using L-kynurenine as substrate measured after 24 hrs by SpectraMax plate reader analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID669472 | Fraction unbound in rat plasma at 1 uM by equilibrium dialysis method | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669539 | Reduction of kynurenine level in freely moving Sprague-Dawley rat dialysates from prefrontal cortex at 10 mg/kg, sc after 20 hrs by microdialysis analysis | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID727188 | Ratio of Kinact to Ki for human KAT2 using L-kynurenine as substrate by SpectraMax plate reader analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID669478 | Inhibition of human KAT3 | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669474 | Ratio of Kinact to Ki for human recombinant KAT2 using L-kynurenine as substrate | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID738357 | Inhibition of human KAT2 using L-kynurenine as substrate after 15 to 20 hrs by UV-visible spectra analysis | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency. |
AID738355 | Ratio of Kinact to Ki for inhibition of human KAT2 | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency. |
AID727190 | Irreversible inhibition of human KAT2 using L-kynurenine as substrate measured every 5 mins over 16 hrs by SpectraMax plate reader analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID727180 | Decrease in extracellular KYNA level in Sprague-Dawley rat prefrontal cortex at 10 mg/kg, sc measured for 4 hrs by microdialysis method | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID669479 | Inhibition of human KAT4 | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669469 | Free brain concentration in Sprague-Dawley rat at 10 mg/kg, sc after 0.25 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID727187 | AUC in Sprague-Dawley rat brain at 10 mg/kg, sc by LC-MS/MS analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
AID669475 | Inhibition of human recombinant KAT2 assessed as conversion of L-kynurenine into kynurenic acid after 15 to 20 hrs | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669473 | Ratio of Kinact to Ki for rat recombinant KAT2 using L-kynurenine as substrate | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
AID669484 | Reduction of kynurenine level in freely moving Sprague-Dawley rat dialysates from prefrontal cortex at 10 mg/kg, sc after 1 hr by microdialysis analysis relative to control | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
| Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |