Page last updated: 2024-11-13

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

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

You're describing a rather specific chemical compound, (r)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline. This complex name breaks down into several key components:

* **(r)-:** This indicates the molecule is a chiral compound, meaning it exists in two mirror-image forms (enantiomers). The r prefix denotes a specific configuration of these enantiomers.
* **4-cyclopropyl:** This refers to a cyclopropane ring attached at the 4th position of the main ring structure.
* **7,8-difluoro:** Two fluorine atoms are present at the 7th and 8th positions.
* **5-(4-(trifluoromethyl)phenylsulfonyl):** A complex substituent at the 5th position:
* **phenylsulfonyl:** A benzene ring with a sulfonyl (-SO2-) group attached.
* **4-(trifluoromethyl):** A trifluoromethyl group (-CF3) is attached at the 4th position of the benzene ring.
* **4,5-dihydro-1H-pyrazolo[4,3-c]quinoline:** The base structure. It's a fused ring system derived from pyrazolo[4,3-c]quinoline with hydrogen atoms added at the 4th and 5th positions.

**Why is this compound important for research?**

The exact significance of this specific compound would depend on the research context. However, its complex structure and presence of fluorine atoms suggest several potential areas of interest:

* **Pharmaceutical Research:** The presence of fluorine atoms is often linked to improved drug properties, such as increased metabolic stability and better penetration of cell membranes.
* **Material Science:** The compound's structure could be interesting for creating new materials with specific properties.
* **Synthetic Chemistry:** The synthesis and characterization of this compound itself could be an important research objective, especially if it's a novel molecule with unique properties.

**To understand the specific importance of this compound, you would need more context:**

* **What is the specific research area?** Is it drug discovery, material science, or something else?
* **What are the intended applications of the compound?** Is it a potential drug candidate, a building block for new materials, or a synthetic target for studying chemical reactions?

Without this information, it's impossible to say exactly why this compound is important.

(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 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The poor absolute oral bioavailability of the compound in fasted dogs (F ∼11%) is attributed to poor aqueous solubility."( 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.
Bullock, J; Goldbach, E; Gullapalli, RP; Hoffman, W; Liversidge, GG; Merisko-Liversidge, E; Quinn, K; Sauer, JM; Tonn, G; Wong, A, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Presenilin-1Homo sapiens (human)IC50 (µMol)0.00310.00010.23785.6800AID754316; AID754317; AID755855; AID755856
Presenilin-2Homo sapiens (human)IC50 (µMol)0.00310.00010.24355.6800AID754316; AID754317; AID755855; AID755856
Gamma-secretase subunit APH-1BHomo sapiens (human)IC50 (µMol)0.00310.00010.24355.6800AID754316; AID754317; AID755855; AID755856
NicastrinHomo sapiens (human)IC50 (µMol)0.00310.00010.24355.6800AID754316; AID754317; AID755855; AID755856
Gamma-secretase subunit APH-1AHomo sapiens (human)IC50 (µMol)0.00310.00010.24355.6800AID754316; AID754317; AID755855; AID755856
Gamma-secretase subunit PEN-2Homo sapiens (human)IC50 (µMol)0.00310.00010.24425.6800AID754316; AID754317; AID755855; AID755856
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Presenilin-1Homo sapiens (human)ED500.00110.00110.00340.0078AID754313
Presenilin-2Homo sapiens (human)ED500.00110.00110.00340.0078AID754313
Gamma-secretase subunit APH-1BHomo sapiens (human)ED500.00110.00110.00340.0078AID754313
NicastrinHomo sapiens (human)ED500.00110.00110.00340.0078AID754313
Gamma-secretase subunit APH-1AHomo sapiens (human)ED500.00110.00110.00340.0078AID754313
Gamma-secretase subunit PEN-2Homo sapiens (human)ED500.00110.00110.01200.0360AID754313
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (107)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityPresenilin-1Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisPresenilin-1Homo sapiens (human)
cell-cell adhesionPresenilin-1Homo sapiens (human)
autophagosome assemblyPresenilin-1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPresenilin-1Homo sapiens (human)
blood vessel developmentPresenilin-1Homo sapiens (human)
cell fate specificationPresenilin-1Homo sapiens (human)
somitogenesisPresenilin-1Homo sapiens (human)
neuron migrationPresenilin-1Homo sapiens (human)
positive regulation of receptor recyclingPresenilin-1Homo sapiens (human)
negative regulation of protein phosphorylationPresenilin-1Homo sapiens (human)
positive regulation of protein phosphorylationPresenilin-1Homo sapiens (human)
heart loopingPresenilin-1Homo sapiens (human)
positive regulation of L-glutamate import across plasma membranePresenilin-1Homo sapiens (human)
hematopoietic progenitor cell differentiationPresenilin-1Homo sapiens (human)
astrocyte activation involved in immune responsePresenilin-1Homo sapiens (human)
T cell activation involved in immune responsePresenilin-1Homo sapiens (human)
neural retina developmentPresenilin-1Homo sapiens (human)
protein glycosylationPresenilin-1Homo sapiens (human)
membrane protein ectodomain proteolysisPresenilin-1Homo sapiens (human)
mitochondrial transportPresenilin-1Homo sapiens (human)
DNA damage responsePresenilin-1Homo sapiens (human)
response to oxidative stressPresenilin-1Homo sapiens (human)
Notch receptor processingPresenilin-1Homo sapiens (human)
learning or memoryPresenilin-1Homo sapiens (human)
memoryPresenilin-1Homo sapiens (human)
post-embryonic developmentPresenilin-1Homo sapiens (human)
regulation of gene expressionPresenilin-1Homo sapiens (human)
positive regulation of gene expressionPresenilin-1Homo sapiens (human)
negative regulation of gene expressionPresenilin-1Homo sapiens (human)
regulation of neuron projection developmentPresenilin-1Homo sapiens (human)
protein transportPresenilin-1Homo sapiens (human)
choline transportPresenilin-1Homo sapiens (human)
synaptic vesicle targetingPresenilin-1Homo sapiens (human)
protein processingPresenilin-1Homo sapiens (human)
cerebellum developmentPresenilin-1Homo sapiens (human)
cerebral cortex cell migrationPresenilin-1Homo sapiens (human)
Cajal-Retzius cell differentiationPresenilin-1Homo sapiens (human)
dorsal/ventral neural tube patterningPresenilin-1Homo sapiens (human)
embryonic limb morphogenesisPresenilin-1Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processPresenilin-1Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisPresenilin-1Homo sapiens (human)
positive regulation of tumor necrosis factor productionPresenilin-1Homo sapiens (human)
amyloid-beta formationPresenilin-1Homo sapiens (human)
intracellular signal transductionPresenilin-1Homo sapiens (human)
locomotionPresenilin-1Homo sapiens (human)
positive regulation of protein import into nucleusPresenilin-1Homo sapiens (human)
regulation of phosphorylationPresenilin-1Homo sapiens (human)
amyloid precursor protein metabolic processPresenilin-1Homo sapiens (human)
amyloid precursor protein catabolic processPresenilin-1Homo sapiens (human)
myeloid dendritic cell differentiationPresenilin-1Homo sapiens (human)
positive regulation of apoptotic processPresenilin-1Homo sapiens (human)
negative regulation of apoptotic processPresenilin-1Homo sapiens (human)
negative regulation of neuron apoptotic processPresenilin-1Homo sapiens (human)
skin morphogenesisPresenilin-1Homo sapiens (human)
positive regulation of glycolytic processPresenilin-1Homo sapiens (human)
positive regulation of DNA-templated transcriptionPresenilin-1Homo sapiens (human)
astrocyte activationPresenilin-1Homo sapiens (human)
regulation of synaptic plasticityPresenilin-1Homo sapiens (human)
thymus developmentPresenilin-1Homo sapiens (human)
neuron developmentPresenilin-1Homo sapiens (human)
skeletal system morphogenesisPresenilin-1Homo sapiens (human)
brain morphogenesisPresenilin-1Homo sapiens (human)
epithelial cell proliferationPresenilin-1Homo sapiens (human)
negative regulation of axonogenesisPresenilin-1Homo sapiens (human)
synapse organizationPresenilin-1Homo sapiens (human)
positive regulation of coagulationPresenilin-1Homo sapiens (human)
T cell receptor signaling pathwayPresenilin-1Homo sapiens (human)
sequestering of calcium ionPresenilin-1Homo sapiens (human)
neuron apoptotic processPresenilin-1Homo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisPresenilin-1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicPresenilin-1Homo sapiens (human)
regulation of resting membrane potentialPresenilin-1Homo sapiens (human)
regulation of canonical Wnt signaling pathwayPresenilin-1Homo sapiens (human)
positive regulation of dendritic spine developmentPresenilin-1Homo sapiens (human)
neuron cellular homeostasisPresenilin-1Homo sapiens (human)
calcium ion transmembrane transportPresenilin-1Homo sapiens (human)
apoptotic signaling pathwayPresenilin-1Homo sapiens (human)
regulation of synaptic vesicle cyclePresenilin-1Homo sapiens (human)
L-glutamate import across plasma membranePresenilin-1Homo sapiens (human)
regulation of postsynapse organizationPresenilin-1Homo sapiens (human)
protein catabolic process at postsynapsePresenilin-1Homo sapiens (human)
cellular response to amyloid-betaPresenilin-1Homo sapiens (human)
negative regulation of core promoter bindingPresenilin-1Homo sapiens (human)
positive regulation of amyloid fibril formationPresenilin-1Homo sapiens (human)
neuron projection maintenancePresenilin-1Homo sapiens (human)
negative regulation of ubiquitin-dependent protein catabolic processPresenilin-1Homo sapiens (human)
negative regulation of apoptotic signaling pathwayPresenilin-1Homo sapiens (human)
calcium ion homeostasisPresenilin-1Homo sapiens (human)
Notch signaling pathwayPresenilin-1Homo sapiens (human)
response to hypoxiaPresenilin-2Homo sapiens (human)
membrane protein ectodomain proteolysisPresenilin-2Homo sapiens (human)
Notch receptor processingPresenilin-2Homo sapiens (human)
protein processingPresenilin-2Homo sapiens (human)
amyloid-beta formationPresenilin-2Homo sapiens (human)
intracellular signal transductionPresenilin-2Homo sapiens (human)
amyloid precursor protein catabolic processPresenilin-2Homo sapiens (human)
regulation of calcium import into the mitochondrionPresenilin-2Homo sapiens (human)
mitochondrion-endoplasmic reticulum membrane tetheringPresenilin-2Homo sapiens (human)
calcium ion homeostasisPresenilin-2Homo sapiens (human)
Notch signaling pathwayPresenilin-2Homo sapiens (human)
protein processingGamma-secretase subunit APH-1BHomo sapiens (human)
Notch receptor processingGamma-secretase subunit APH-1BHomo sapiens (human)
positive regulation of endopeptidase activityGamma-secretase subunit APH-1BHomo sapiens (human)
protein processingGamma-secretase subunit APH-1BHomo sapiens (human)
membrane protein intracellular domain proteolysisGamma-secretase subunit APH-1BHomo sapiens (human)
amyloid-beta formationGamma-secretase subunit APH-1BHomo sapiens (human)
amyloid precursor protein catabolic processGamma-secretase subunit APH-1BHomo sapiens (human)
Notch signaling pathwayGamma-secretase subunit APH-1BHomo sapiens (human)
myeloid cell homeostasisNicastrinHomo sapiens (human)
proteolysisNicastrinHomo sapiens (human)
membrane protein ectodomain proteolysisNicastrinHomo sapiens (human)
dopamine receptor signaling pathwayNicastrinHomo sapiens (human)
glutamate receptor signaling pathwayNicastrinHomo sapiens (human)
Notch signaling pathwayNicastrinHomo sapiens (human)
Notch receptor processingNicastrinHomo sapiens (human)
learning or memoryNicastrinHomo sapiens (human)
positive regulation of endopeptidase activityNicastrinHomo sapiens (human)
protein processingNicastrinHomo sapiens (human)
cerebellum developmentNicastrinHomo sapiens (human)
central nervous system myelinationNicastrinHomo sapiens (human)
adult behaviorNicastrinHomo sapiens (human)
membrane protein intracellular domain proteolysisNicastrinHomo sapiens (human)
amyloid-beta formationNicastrinHomo sapiens (human)
T cell proliferationNicastrinHomo sapiens (human)
amyloid precursor protein metabolic processNicastrinHomo sapiens (human)
amyloid precursor protein biosynthetic processNicastrinHomo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic processNicastrinHomo sapiens (human)
amyloid precursor protein catabolic processNicastrinHomo sapiens (human)
epithelial cell proliferationNicastrinHomo sapiens (human)
neuron apoptotic processNicastrinHomo sapiens (human)
cellular response to calcium ionNicastrinHomo sapiens (human)
regulation of long-term synaptic potentiationNicastrinHomo sapiens (human)
short-term synaptic potentiationNicastrinHomo sapiens (human)
metanephros developmentGamma-secretase subunit APH-1AHomo sapiens (human)
membrane protein ectodomain proteolysisGamma-secretase subunit APH-1AHomo sapiens (human)
Notch receptor processingGamma-secretase subunit APH-1AHomo sapiens (human)
positive regulation of endopeptidase activityGamma-secretase subunit APH-1AHomo sapiens (human)
protein processingGamma-secretase subunit APH-1AHomo sapiens (human)
membrane protein intracellular domain proteolysisGamma-secretase subunit APH-1AHomo sapiens (human)
amyloid-beta formationGamma-secretase subunit APH-1AHomo sapiens (human)
amyloid precursor protein metabolic processGamma-secretase subunit APH-1AHomo sapiens (human)
amyloid precursor protein catabolic processGamma-secretase subunit APH-1AHomo sapiens (human)
Notch signaling pathwayGamma-secretase subunit APH-1AHomo sapiens (human)
membrane protein ectodomain proteolysisGamma-secretase subunit PEN-2Homo sapiens (human)
Notch signaling pathwayGamma-secretase subunit PEN-2Homo sapiens (human)
Notch receptor processingGamma-secretase subunit PEN-2Homo sapiens (human)
positive regulation of endopeptidase activityGamma-secretase subunit PEN-2Homo sapiens (human)
protein processingGamma-secretase subunit PEN-2Homo sapiens (human)
membrane protein intracellular domain proteolysisGamma-secretase subunit PEN-2Homo sapiens (human)
amyloid-beta formationGamma-secretase subunit PEN-2Homo sapiens (human)
amyloid precursor protein metabolic processGamma-secretase subunit PEN-2Homo sapiens (human)
amyloid precursor protein catabolic processGamma-secretase subunit PEN-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
endopeptidase activityPresenilin-1Homo sapiens (human)
aspartic-type endopeptidase activityPresenilin-1Homo sapiens (human)
calcium channel activityPresenilin-1Homo sapiens (human)
protein bindingPresenilin-1Homo sapiens (human)
beta-catenin bindingPresenilin-1Homo sapiens (human)
PDZ domain bindingPresenilin-1Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleavingPresenilin-1Homo sapiens (human)
cadherin bindingPresenilin-1Homo sapiens (human)
ATPase bindingPresenilin-1Homo sapiens (human)
growth factor receptor bindingPresenilin-1Homo sapiens (human)
protein bindingPresenilin-2Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleavingPresenilin-2Homo sapiens (human)
protein bindingGamma-secretase subunit APH-1BHomo sapiens (human)
protein-macromolecule adaptor activityGamma-secretase subunit APH-1BHomo sapiens (human)
endopeptidase activator activityGamma-secretase subunit APH-1BHomo sapiens (human)
protein bindingNicastrinHomo sapiens (human)
protein-macromolecule adaptor activityNicastrinHomo sapiens (human)
aspartic endopeptidase activity, intramembrane cleavingNicastrinHomo sapiens (human)
ATPase bindingNicastrinHomo sapiens (human)
growth factor receptor bindingNicastrinHomo sapiens (human)
protein bindingGamma-secretase subunit APH-1AHomo sapiens (human)
enzyme bindingGamma-secretase subunit APH-1AHomo sapiens (human)
protein-macromolecule adaptor activityGamma-secretase subunit APH-1AHomo sapiens (human)
endopeptidase activator activityGamma-secretase subunit APH-1AHomo sapiens (human)
protein bindingGamma-secretase subunit PEN-2Homo sapiens (human)
enzyme bindingGamma-secretase subunit PEN-2Homo sapiens (human)
endopeptidase activator activityGamma-secretase subunit PEN-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (46)

Processvia Protein(s)Taxonomy
smooth endoplasmic reticulumPresenilin-1Homo sapiens (human)
dendritePresenilin-1Homo sapiens (human)
Golgi membranePresenilin-1Homo sapiens (human)
kinetochorePresenilin-1Homo sapiens (human)
nucleusPresenilin-1Homo sapiens (human)
nuclear outer membranePresenilin-1Homo sapiens (human)
nucleoplasmPresenilin-1Homo sapiens (human)
mitochondrionPresenilin-1Homo sapiens (human)
mitochondrial inner membranePresenilin-1Homo sapiens (human)
endoplasmic reticulumPresenilin-1Homo sapiens (human)
endoplasmic reticulum membranePresenilin-1Homo sapiens (human)
smooth endoplasmic reticulumPresenilin-1Homo sapiens (human)
rough endoplasmic reticulumPresenilin-1Homo sapiens (human)
Golgi apparatusPresenilin-1Homo sapiens (human)
centrosomePresenilin-1Homo sapiens (human)
plasma membranePresenilin-1Homo sapiens (human)
cell cortexPresenilin-1Homo sapiens (human)
synaptic vesiclePresenilin-1Homo sapiens (human)
cell surfacePresenilin-1Homo sapiens (human)
membranePresenilin-1Homo sapiens (human)
aggresomePresenilin-1Homo sapiens (human)
cell junctionPresenilin-1Homo sapiens (human)
growth conePresenilin-1Homo sapiens (human)
neuromuscular junctionPresenilin-1Homo sapiens (human)
early endosome membranePresenilin-1Homo sapiens (human)
nuclear membranePresenilin-1Homo sapiens (human)
ciliary rootletPresenilin-1Homo sapiens (human)
azurophil granule membranePresenilin-1Homo sapiens (human)
sarcolemmaPresenilin-1Homo sapiens (human)
presynaptic membranePresenilin-1Homo sapiens (human)
neuron projectionPresenilin-1Homo sapiens (human)
neuronal cell bodyPresenilin-1Homo sapiens (human)
dendritic shaftPresenilin-1Homo sapiens (human)
membrane raftPresenilin-1Homo sapiens (human)
postsynapsePresenilin-1Homo sapiens (human)
glutamatergic synapsePresenilin-1Homo sapiens (human)
protein-containing complexPresenilin-1Homo sapiens (human)
gamma-secretase complexPresenilin-1Homo sapiens (human)
Golgi membranePresenilin-2Homo sapiens (human)
kinetochorePresenilin-2Homo sapiens (human)
nuclear inner membranePresenilin-2Homo sapiens (human)
early endosomePresenilin-2Homo sapiens (human)
endoplasmic reticulumPresenilin-2Homo sapiens (human)
endoplasmic reticulum membranePresenilin-2Homo sapiens (human)
Golgi apparatusPresenilin-2Homo sapiens (human)
centrosomePresenilin-2Homo sapiens (human)
plasma membranePresenilin-2Homo sapiens (human)
synaptic vesiclePresenilin-2Homo sapiens (human)
membranePresenilin-2Homo sapiens (human)
presynaptic membranePresenilin-2Homo sapiens (human)
protein-containing complexPresenilin-2Homo sapiens (human)
gamma-secretase complexPresenilin-2Homo sapiens (human)
Golgi membraneGamma-secretase subunit APH-1BHomo sapiens (human)
endoplasmic reticulum membraneGamma-secretase subunit APH-1BHomo sapiens (human)
plasma membraneGamma-secretase subunit APH-1BHomo sapiens (human)
endosome membraneGamma-secretase subunit APH-1BHomo sapiens (human)
membraneGamma-secretase subunit APH-1BHomo sapiens (human)
transport vesicleGamma-secretase subunit APH-1BHomo sapiens (human)
gamma-secretase complexGamma-secretase subunit APH-1BHomo sapiens (human)
endoplasmic reticulumGamma-secretase subunit APH-1BHomo sapiens (human)
Golgi membraneNicastrinHomo sapiens (human)
lysosomal membraneNicastrinHomo sapiens (human)
early endosomeNicastrinHomo sapiens (human)
endoplasmic reticulumNicastrinHomo sapiens (human)
endoplasmic reticulum membraneNicastrinHomo sapiens (human)
Golgi apparatusNicastrinHomo sapiens (human)
plasma membraneNicastrinHomo sapiens (human)
focal adhesionNicastrinHomo sapiens (human)
synaptic vesicleNicastrinHomo sapiens (human)
endosome membraneNicastrinHomo sapiens (human)
membraneNicastrinHomo sapiens (human)
azurophil granule membraneNicastrinHomo sapiens (human)
sarcolemmaNicastrinHomo sapiens (human)
melanosomeNicastrinHomo sapiens (human)
presynaptic membraneNicastrinHomo sapiens (human)
extracellular exosomeNicastrinHomo sapiens (human)
gamma-secretase complexNicastrinHomo sapiens (human)
plasma membraneNicastrinHomo sapiens (human)
Golgi membraneGamma-secretase subunit APH-1AHomo sapiens (human)
early endosomeGamma-secretase subunit APH-1AHomo sapiens (human)
endoplasmic reticulumGamma-secretase subunit APH-1AHomo sapiens (human)
endoplasmic reticulum membraneGamma-secretase subunit APH-1AHomo sapiens (human)
Golgi apparatusGamma-secretase subunit APH-1AHomo sapiens (human)
plasma membraneGamma-secretase subunit APH-1AHomo sapiens (human)
synaptic vesicleGamma-secretase subunit APH-1AHomo sapiens (human)
endosome membraneGamma-secretase subunit APH-1AHomo sapiens (human)
membraneGamma-secretase subunit APH-1AHomo sapiens (human)
Golgi cisterna membraneGamma-secretase subunit APH-1AHomo sapiens (human)
presynaptic membraneGamma-secretase subunit APH-1AHomo sapiens (human)
gamma-secretase complexGamma-secretase subunit APH-1AHomo sapiens (human)
endoplasmic reticulumGamma-secretase subunit APH-1AHomo sapiens (human)
Golgi membraneGamma-secretase subunit PEN-2Homo sapiens (human)
endoplasmic reticulumGamma-secretase subunit PEN-2Homo sapiens (human)
endoplasmic reticulum membraneGamma-secretase subunit PEN-2Homo sapiens (human)
Golgi apparatusGamma-secretase subunit PEN-2Homo sapiens (human)
plasma membraneGamma-secretase subunit PEN-2Homo sapiens (human)
endosome membraneGamma-secretase subunit PEN-2Homo sapiens (human)
membraneGamma-secretase subunit PEN-2Homo sapiens (human)
Golgi cisterna membraneGamma-secretase subunit PEN-2Homo sapiens (human)
presynaptic membraneGamma-secretase subunit PEN-2Homo sapiens (human)
gamma-secretase complexGamma-secretase subunit PEN-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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]

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
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.43 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.43)

All Compounds (24.57)

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%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]