| Assay ID | Title | Year | Journal | Article |
|---|
| AID1872651 | Metabolic stability in human liver microsomes assessed as half life | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID755849 | Oxidative metabolism in dog liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID1872653 | Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 42 production by cell-free assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID1872654 | Ratio of drug concentration in Tg2576 mouse brain to plasma at 1 to 30 mg/kg, po | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID755855 | Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID475546 | Half life in rat microsomes | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID754313 | Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors. |
| AID475545 | Half life in human microsomes | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID348070 | Metabolic stability in monkey microsomes assessed as half life | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID475576 | Inhibition of gamma secretase-mediated total amyloid beta production in plasma of patient with Alzheimer's disease at 450 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID755850 | Oxidative metabolism in mouse liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID348066 | Metabolic stability in Tg2576 mouse microsomes assessed as half life | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID475574 | AUC in transgenic 2576 mouse brain at 10 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID731030 | Inhibition of gamma-secretase (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta40 secretion by ELISA | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Effect of helical conformation and side chain structure on γ-secretase inhibition by β-peptide foldamers: insight into substrate recognition. |
| AID475547 | Half life in mouse microsomes | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475569 | Inhibition of gamma secretase-mediated total amyloid beta production in healthy human plasma at 600 mg/kg, po administered as single dose | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID1628299 | Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloid beta 40 after 24 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases. |
| AID475579 | AUC in brain of patient with Alzheimer's disease at 450 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID348068 | Metabolic stability in human microsomes assessed as half life | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID475517 | Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID1872650 | Selectivity ratio, ratio of IC50 for gamma-secretase (unknown origin) to IC50for Notch (unknown origin) | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID1628301 | Selectivity ratio of IC50 for gamma secretase (unknown origin) mediated Notch M1726V mutant activation in CHO K1 cells to gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases. |
| AID754316 | Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors. |
| AID755846 | Glucuronidation metabolism in mouse liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID731029 | Inhibition of gamma-secretase (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta42 secretion by ELISA | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| Effect of helical conformation and side chain structure on γ-secretase inhibition by β-peptide foldamers: insight into substrate recognition. |
| AID754314 | Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors. |
| AID754317 | Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors. |
| AID755813 | Reduction in amyloid beta (x to 40) in FVB mouse cortex at 1 mg/kg, po administered as single dose measured at 3 hrs | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID755843 | Glucuronidation metabolism in human liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID1872652 | Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 40 production by cell-free assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID475570 | Ratio of drug level in plasma to CSF in healthy human at 600 mg/kg, po administered as single dose | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475577 | AUC in plasma of patient with Alzheimer's disease at 450 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID755812 | Reduction in amyloid beta (x to 40) in FVB mouse cortex at 3 mg/kg, po administered as single dose measured at 3 hrs | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID348072 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID755854 | Selctivity ratio of IC50 for partially purified human gamma-secretase-mediated cleavage of notch fusion protein to IC50 for partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID475548 | Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in transgenic 2576 mouse brain at 5 mg/kg, po after 4 hrs | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID755856 | Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID348069 | Metabolic stability in dog microsomes assessed as half life | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID755848 | Oxidative metabolism in rat liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID755852 | Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID755811 | Reduction in amyloid beta (x to 40) in FVB mouse cortex at 30 mg/kg, po administered as single dose measured at 3 hrs | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID475571 | Inhibition of gamma secretase-mediated total amyloid beta production in transgenic 2576 mouse plasma at 10 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475550 | Selectivity for gamma secretase-mediated amyloid beta (1 to 40) production over gamma secretase-mediated notch processing | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475551 | Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475573 | AUC in transgenic 2576 mouse plasma at 10 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475575 | AUC in transgenic 2576 mouse CSF at 10 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID755845 | Glucuronidation metabolism in dog liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID348053 | Inhibition of gamma-secretase expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID755851 | Selctivity ratio of ED50 for gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage to ED50 for gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID755844 | Glucuronidation metabolism in rat liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID475581 | Inhibition of gamma secretase-mediated total amyloid beta production in human plasma at 450 mg/kg measured at 2 hrs post-dose | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID348055 | Reduction of amyloid beta40 level in Tg2576 mouse brain at 5 mg/kg, po after 4 hrs | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID754312 | Ratio of IC50 for gamma-secretase in CHO cells using Notch as substrate to ED50 for gamma-secretase in HEK293 cells using APP as substrate | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors. |
| AID348067 | Metabolic stability in rat microsomes assessed as half life | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID475572 | Inhibition of gamma secretase-mediated total amyloid beta production in transgenic 2576 mouse brain at 10 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID1872655 | Toxicity in Sprague-Dawley rat assessed as maximum tolerated dose administered orally upto 28 days consecutively | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID755810 | Reduction in amyloid beta (x to 40) in FVB mouse cortex at 10 mg/kg, po administered as single dose measured at 3 hrs | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID475526 | Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID348057 | Reduction of amyloid beta42 level in Tg2576 mouse brain at 5 mg/kg, po after 4 hrs | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID755853 | Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID348060 | Selectivity ratio of EC50 for gamma-secretase to EC50 for mouse notch processing | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| AID1872649 | Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 40 production by cell-based assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Small molecules targeting γ-secretase and their potential biological applications. |
| AID1628300 | Inhibition of gamma secretase (unknown origin) mediated Notch M1726V mutant activation in CHO K1 cells after 48 hrs by chemiluminescence assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases. |
| AID755847 | Oxidative metabolism in human liver microsomes assessed as compound remaining | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
| AID754315 | Ratio of IC50 for gamma-secretase in human IMR32 cells using Notch as substrate to IC50 for gamma-secretase in human IMR-32 cells using APP as substrate | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
| Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors. |
| AID475578 | AUC in CSF of patient with Alzheimer's disease at 450 mg/kg | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475582 | Inhibition of gamma secretase-mediated total amyloid beta production in human CSF at 450 mg/kg measured at 1 to 24 hrs post-dose | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID475549 | Inhibition of gamma secretase-mediated amyloid beta (1 to 42) production in transgenic 2576 mouse brain at 5 mg/kg, po after 4 hrs | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. |
| AID1798946 | Cell-Based Assay for Amyloid-beta Accumulation from Article 10.1021/jm801252w: \\Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.\\ | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |