Assay ID | Title | Year | Journal | Article |
AID755798 | Hepatic toxicity in cynomolgus monkey administered for 1 year as repeated-dosing | 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 |
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 |
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 |
AID755830 | Drug uptake in FVB mouse brain at 3 mg/kg, po 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 |
AID755823 | Plasma concentration in FVB mouse at 10 mg/kg, po 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 |
AID755801 | Toxicity in FVB mouse assessed as thymus atrophy compound administered orally bid for 7 days | 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 |
AID755805 | Toxicity in FVB mouse assessed as effect on Hes-1 mRNA level in thymus 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 |
AID755838 | Systemic clearance in rat | 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 |
AID755809 | Reduction in amyloid beta (x to 40) in po dosed FVB mouse brain 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 |
AID755827 | Plasma concentration in FVB mouse at 3 mg/kg, po 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 |
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 |
AID755829 | AUC (0 to 3 hrs) in FVB mouse brain at 3 mg/kg, po | 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 |
AID755820 | Fraction unbound in FVB mouse plasma at 10 mg/kg, po 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 |
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. |
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 |
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 |
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 |
AID755821 | AUC (0 to 3 hrs) in FVB mouse plasma at 10 mg/kg, po | 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 |
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. |
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 |
AID755800 | Reduction in amyloid beta in CSF of po dosed healthy human administered as gelatin capsule measured after 5 hrs post administration | 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 |
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 |
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 |
AID755841 | Aqueous solubility of the compound | 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 |
AID755835 | AUC (0 to 3 hrs) in FVB mouse brain at 1 mg/kg, po | 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 |
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 |
AID755804 | Toxicity in FVB mouse assessed as effect on Hes-1 mRNA level in thymus 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 |
AID755807 | Toxicity in FVB mouse assessed as effect on Hes-1 mRNA level in thymus 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 |
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 |
AID755836 | Drug uptake in FVB mouse brain at 1 mg/kg, po 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 |
AID755797 | Hepatic toxicity in rat administered for 6 months as repeated-dosing | 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 |
AID755831 | Fraction unbound in FVB mouse brain at 3 mg/kg, po 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 |
AID755826 | Drug uptake in FVB mouse brain at 10 mg/kg, po 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 |
AID755806 | Toxicity in FVB mouse assessed as effect on Hes-1 mRNA level in thymus 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 |
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 |
AID755832 | AUC (0 to 3 hrs) in FVB mouse plasma at 1 mg/kg, po | 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 |
AID755825 | AUC (0 to 3 hrs) in FVB mouse plasma at 3 mg/kg, po | 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 |
AID755822 | AUC (0 to 3 hrs) in FVB mouse brain at 10 mg/kg, po | 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 |
AID755814 | Fraction unbound in FVB mouse plasma at 30 mg/kg, po 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 |
AID755824 | Fraction unbound in FVB mouse brain at 10 mg/kg, po 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 |
AID755808 | Reduction in amyloid beta (x to 40) in FVB mouse cortex at 30 mg/kg, po administered as single dose measured at 6 hrs post administration | 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 |
AID755842 | Octanol-water partition co-efficient, log P of the compound by shake-flask method | 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. |
AID755817 | AUC (0 to 3 hrs) in FVB mouse brain at 30 mg/kg, po | 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 |
AID755816 | Plasma concentration in FVB mouse at 30 mg/kg, po 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 |
AID755857 | Systemic clearance in rat relative to hepatic blood flow | 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 |
AID755833 | Fraction unbound in FVB mouse plasma at 1 mg/kg, po 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 |
AID755815 | AUC (0 to 3 hrs) in FVB mouse plasma at 30 mg/kg, po | 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 |
AID755803 | Selectivity ratio of EC25 for Reduction in amyloid beta (x to 40) brain to EC25 for change in Hes-1 mRNA level in thymus in po dosed FVB mouse | 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 |
AID755802 | Toxicity in FVB mouse assessed as goblet cell hyperplasia in intestine compound administered orally bid for 7 days | 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 |
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 |
AID755819 | Fraction unbound in FVB mouse brain at 30 mg/kg, po 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 |
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 |
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. |
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 |
AID755837 | Fraction unbound in FVB mouse brain at 1 mg/kg, po 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 |
AID755818 | Drug uptake in FVB mouse brain at 30 mg/kg, po 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 |
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 |
AID755828 | Fraction unbound in FVB mouse plasma at 3 mg/kg, po 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 |
AID755799 | Hepatic toxicity in po dosed healthy human administered as gelatin capsule | 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 |
AID755834 | Plasma concentration in FVB mouse at 1 mg/kg, po 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 |
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 |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |