Assay ID | Title | Year | Journal | Article |
AID1866586 | Antimalarial activity against Plasmodium falciparum 3D7 incubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by microdilution method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Boosting the Discovery of Small Molecule Inhibitors of Glucose-6-Phosphate Dehydrogenase for the Treatment of Cancer, Infectious Diseases, and Inflammation. |
AID701891 | Plasma protein binding in mouse at 1 uM | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701888 | Plasma protein binding in mouse at 10 uM | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701890 | Plasma protein binding in human at 10 uM | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701898 | Aqueous solubility in PBS buffer at pH 7.4 | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701883 | Toxicity against Fa2N-4 immortalized human hepatocytes | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701879 | Competitive inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase using glucose-6-phosphate as substrate by Lineweaver-Burk plot analysis | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701899 | Inhibition of human glucose-6-phosphate dehydrogenase after 90 mins by resazurin/diaphorasecoupled assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701892 | Blood brain barrier permeability of the compound at pH 7.4 by PAMPA | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701895 | Permeability of the compound at donor pH 5 by PAMPA | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701900 | Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 45 mins by orthogonal assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701880 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 cells assessed as Plasmodium falciparum growth inhibition after 72 hrs by isotopic drug sensitivity assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701887 | Stability in human plasma assessed as compound remaining after 3 hrs | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701894 | Permeability of the compound at donor pH 7.4 by PAMPA | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701878 | Mixed type inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase using NADP+ as substrate by Lineweaver-Burk plot analysis | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701884 | Stability in mouse liver microsomes assessed as compound remaining after 1 hr | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701886 | Stability in human liver microsomes assessed as compound remaining after 1 hr | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701893 | Permeability of the compound at donor pH 6.2 by PAMPA | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701903 | Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 2 hrs by resazurin/diaphorasecoupled assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701889 | Plasma protein binding in human at 1 uM | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID1866587 | Antimalarial activity against Chloroquine-resistant Plasmodium falciparum Dd2 incubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by microdilution method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Boosting the Discovery of Small Molecule Inhibitors of Glucose-6-Phosphate Dehydrogenase for the Treatment of Cancer, Infectious Diseases, and Inflammation. |
AID1352489 | Competitive inhibition of recombinant full length human G6PD expressed in Escherichia coli HB351 using G6P as substrate in presence of NADP+ by Lineweaver-Burk plot analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | First homology model of Plasmodium falciparum glucose-6-phosphate dehydrogenase: Discovery of selective substrate analog-based inhibitors as novel antimalarial agents. |
AID701896 | Aqueous solubility in pION's buffer at pH 6.2 | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID1352490 | Competitive inhibition of Plasmodium falciparum G6PD-6PGL using G6P as substrate in presence of NADP+ by Lineweaver-Burk plot analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | First homology model of Plasmodium falciparum glucose-6-phosphate dehydrogenase: Discovery of selective substrate analog-based inhibitors as novel antimalarial agents. |
AID701897 | Aqueous solubility in pION's buffer at pH 7.4 | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701885 | Stability in mouse plasma assessed as compound remaining after 3 hrs | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701881 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 cells assessed as Plasmodium falciparum growth inhibition after 72 hrs by isotopic drug sensitivity assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
AID701901 | Aqueous solubility in pION's buffer at pH 5 | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
| Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces paras |
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. |
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. |
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |