Compounds > (r)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1h-pyrazolo(4,3-c)quinoline
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(r)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1h-pyrazolo(4,3-c)quinoline

Description

(R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo(4,3-c)quinoline: gamma secretase inhibitor; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID53308121
CHEMBL ID2396778
SCHEMBL ID486044
MeSH IDM0574836

Synonyms (19)

Synonym
CHEMBL2396778 ,
elnd-006
1h-pyrazolo(4,3-c)quinoline, 4-cyclopropyl-7,8-difluoro-4,5-dihydro-5-((4-(trifluoromethyl)phenyl)sulfonyl)-, (4r)-
(r)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1h-pyrazolo(4,3-c)quinoline
elnd006
959997-22-9
unii-7f5qgv49gl
7f5qgv49gl ,
(4r)-4-cyclopropyl-7,8-difluoro-5-[4-(trifluoromethyl)benzenesulfonyl]-1h,4h,5h-pyrazolo[4,3-c]quinoline
gtpl7337
(r)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1h-pyrazolo[4,3-c]quinoline
SCHEMBL486044
DTXSID40242063
elnd0006
1333990-84-3
(r)-4-cyclopropyl-7,8-difluoro-5-((4-(trifluoromethyl)phenyl)sulfonyl)-4,5-dihydro-1h-pyrazolo[4,3-c]quinoline
Q27077173
bdbm50492093
(4r)-4-cyclopropyl-7,8-difluoro-5-[4-(trifluoromethyl)phenyl]sulfonyl-1,4-dihydropyrazolo[4,3-c]quinoline

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Presenilin-1Homo sapiens (human)IC500.0031AID754316; AID754317; AID755855; AID755856
Presenilin-2Homo sapiens (human)IC500.0031AID754316; AID754317; AID755855; AID755856
Gamma-secretase subunit APH-1BHomo sapiens (human)IC500.0031AID754316; AID754317; AID755855; AID755856
NicastrinHomo sapiens (human)IC500.0031AID754316; AID754317; AID755855; AID755856
Gamma-secretase subunit APH-1AHomo sapiens (human)IC500.0031AID754316; AID754317; AID755855; AID755856
Gamma-secretase subunit PEN-2Homo sapiens (human)IC500.0031AID754316; AID754317; AID755855; AID755856

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Presenilin-1Homo sapiens (human)ED500.0011AID754313
Presenilin-2Homo sapiens (human)ED500.0011AID754313
Gamma-secretase subunit APH-1BHomo sapiens (human)ED500.0011AID754313
NicastrinHomo sapiens (human)ED500.0011AID754313
Gamma-secretase subunit APH-1AHomo sapiens (human)ED500.0011AID754313
Gamma-secretase subunit PEN-2Homo sapiens (human)ED500.0011AID754313

Bioassays (65)

Assay IDTitleYearJournalArticle
AID755798Hepatic toxicity in cynomolgus monkey administered for 1 year as repeated-dosing2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755851Selctivity 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) secretion2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755847Oxidative metabolism in human liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755830Drug uptake in FVB mouse brain at 3 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755823Plasma concentration in FVB mouse at 10 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755801Toxicity in FVB mouse assessed as thymus atrophy compound administered orally bid for 7 days2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755805Toxicity 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 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755838Systemic clearance in rat2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755809Reduction in amyloid beta (x to 40) in po dosed FVB mouse brain administered as single dose measured at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755827Plasma concentration in FVB mouse at 3 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755813Reduction in amyloid beta (x to 40) in FVB mouse cortex at 1 mg/kg, po administered as single dose measured at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755829AUC (0 to 3 hrs) in FVB mouse brain at 3 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755843Glucuronidation metabolism in human liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755820Fraction unbound in FVB mouse plasma at 10 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID754316Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
ISSN: 1464-3405		Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
AID755810Reduction in amyloid beta (x to 40) in FVB mouse cortex at 10 mg/kg, po administered as single dose measured at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755844Glucuronidation metabolism in rat liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755852Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755821AUC (0 to 3 hrs) in FVB mouse plasma at 10 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID754313Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
ISSN: 1464-3405		Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
AID755848Oxidative metabolism in rat liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755800Reduction in amyloid beta in CSF of po dosed healthy human administered as gelatin capsule measured after 5 hrs post administration2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755845Glucuronidation metabolism in dog liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755855Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755841Aqueous solubility of the compound2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755835AUC (0 to 3 hrs) in FVB mouse brain at 1 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755850Oxidative metabolism in mouse liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755804Toxicity 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 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755807Toxicity 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 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755812Reduction in amyloid beta (x to 40) in FVB mouse cortex at 3 mg/kg, po administered as single dose measured at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755836Drug uptake in FVB mouse brain at 1 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755797Hepatic toxicity in rat administered for 6 months as repeated-dosing2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755831Fraction unbound in FVB mouse brain at 3 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755826Drug uptake in FVB mouse brain at 10 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755806Toxicity 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 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755849Oxidative metabolism in dog liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755832AUC (0 to 3 hrs) in FVB mouse plasma at 1 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755825AUC (0 to 3 hrs) in FVB mouse plasma at 3 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755822AUC (0 to 3 hrs) in FVB mouse brain at 10 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755814Fraction unbound in FVB mouse plasma at 30 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755824Fraction unbound in FVB mouse brain at 10 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755808Reduction in amyloid beta (x to 40) in FVB mouse cortex at 30 mg/kg, po administered as single dose measured at 6 hrs post administration2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755842Octanol-water partition co-efficient, log P of the compound by shake-flask method2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID754315Ratio 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 substrate2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
ISSN: 1464-3405		Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
AID755817AUC (0 to 3 hrs) in FVB mouse brain at 30 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755816Plasma concentration in FVB mouse at 30 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755857Systemic clearance in rat relative to hepatic blood flow2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755833Fraction unbound in FVB mouse plasma at 1 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755815AUC (0 to 3 hrs) in FVB mouse plasma at 30 mg/kg, po2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755803Selectivity 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 mouse2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755802Toxicity in FVB mouse assessed as goblet cell hyperplasia in intestine compound administered orally bid for 7 days2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755853Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755819Fraction unbound in FVB mouse brain at 30 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755846Glucuronidation metabolism in mouse liver microsomes assessed as compound remaining2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID754317Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
ISSN: 1464-3405		Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
AID755856Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755837Fraction unbound in FVB mouse brain at 1 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755818Drug uptake in FVB mouse brain at 30 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755811Reduction in amyloid beta (x to 40) in FVB mouse cortex at 30 mg/kg, po administered as single dose measured at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755828Fraction unbound in FVB mouse plasma at 3 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755799Hepatic toxicity in po dosed healthy human administered as gelatin capsule2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755834Plasma concentration in FVB mouse at 1 mg/kg, po at 3 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID755854Selctivity 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 protein2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
ISSN: 1520-4804		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
AID754312Ratio of IC50 for gamma-secretase in CHO cells using Notch as substrate to ED50 for gamma-secretase in HEK293 cells using APP as substrate2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
ISSN: 1464-3405		Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
AID754314Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
ISSN: 1464-3405		Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (100.00)24.3611
2020's0 (0.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
propranolol
1
naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic		2013201311.0medium000010
ly 450139
1
peptide2013201311.0high000010
begacestat
2
2013201311.0high000020
bms 708163
2
oxadiazole;
ring assembly		2013201311.0high000020
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
47,XX,+210
2
201520178.0high000020
Acute Confusional Senile Dementia0
1
2011201113.0medium000010
Alzheimer Disease0
1
2011201113.0medium000010
Disease Models, Animal0
2
201520178.0high000020
Down Syndrome0
2
201520178.0high000020
Neuroblastoma0
1
201720177.0medium000010

Bioavailability (1)

ArticleYear
A formulation strategy for gamma secretase inhibitor ELND006, a BCS class II compound: development of a nanosuspension formulation with improved oral bioavailability and reduced food effects in dogs.
Journal of pharmaceutical sciences, , Volume: 101, Issue:4		2012