Page last updated: 2024-11-13

jnj 40418677

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

Cross-References

ID SourceID
PubMed CID52939724
CHEMBL ID2151284
SCHEMBL ID491938
MeSH IDM0562315

Synonyms (24)

Synonym
CHEMBL2151284 ,
SCHEMBL491938
1146594-87-7
jnj-40418677
2-(s)-(3,5-bis(4-(trifluoromethyl)phenyl)phenyl)-4-methylpentanoic acid
(1,1':3',1''-terphenyl)-5'-acetic acid, .alpha.-(2-methylpropyl)-4,4''-bis(trifluoromethyl)-, (.alpha.s)-
Z1CWW31SGG ,
unii-z1cww31sgg
(1,1':3',1''-terphenyl)-5'-acetic acid, alpha-(2-methylpropyl)-4,4''-bis(trifluoromethyl)-, (alphas)-
HY-100604
bdbm50114790
NCGC00370685-02
rqowddlkgbmjfx-qhcpkhfhsa-n
AS-16391
(s)-2-(4,4''-bis(trifluoromethyl)-[1,1':3',1''-terphenyl]-5'-yl)-4-methylpentanoic acid
NCGC00370685-06
Q27294866
(2s)-2-[3,5-bis[4-(trifluoromethyl)phenyl]phenyl]-4-methylpentanoic acid
AKOS037643428
jnj 40418677
jnj40418677
NCGC00370685-03
WVB59487
CS-0019757

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Both half-life and bioavailability were significantly improved, especially in dog, with robust brain Aβ42 lowering maintained in both transgenic mouse and rat."( Potent benzoazepinone γ-secretase modulators with improved bioavailability.
Ahearn, SP; Ball, R; Brown, WC; Deshmukh, SV; Diaz, D; Fischer, C; Hill, A; Hughes, B; Jeliazkova-Mecheva, VV; Kattar, S; Kelley, E; Kenific, CM; Li, C; Mampreian, DM; Methot, JL; Miller, TA; Moxham, C; Moy, LY; Munoz, B; Nuthall, H; Rivkin, A; Rosenau, A; Schell, A; Shah, S; Shearman, MS; Smotrov, N; Szewczak, AA; Zhou, H, 2015
)
0.42
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency23.91850.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency37.90830.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency23.91850.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency23.91850.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency23.91850.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency23.91850.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Presenilin-1Homo sapiens (human)IC50 (µMol)0.20000.00010.23785.6800AID1242093
Presenilin-2Homo sapiens (human)IC50 (µMol)0.20000.00010.24355.6800AID1242093
Gamma-secretase subunit APH-1BHomo sapiens (human)IC50 (µMol)0.20000.00010.24355.6800AID1242093
NicastrinHomo sapiens (human)IC50 (µMol)0.20000.00010.24355.6800AID1242093
Gamma-secretase subunit APH-1AHomo sapiens (human)IC50 (µMol)0.20000.00010.24355.6800AID1242093
Gamma-secretase subunit PEN-2Homo sapiens (human)IC50 (µMol)0.20000.00010.24425.6800AID1242093
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (150)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo 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 (30)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo 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 (58)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo 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 (28)

Assay IDTitleYearJournalArticle
AID1347163384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347171Orthogonal mCherry assay for qRT-PCR qHTS of selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347172Secondary qRT-PCR qHTS assay for selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347156DAPI mCherry counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347170Vero cells viability counterscreen for qRT-PCR qHTS assay of selected Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347164384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347158ZIKV-mCherry secondary qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID692103Inhibition of gamma secretase assessed as reduction in Abeta42 production2011Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs.
AID692119Antialzheimer activity in non-transgenic rat assessed as reduction in brain Abeta42 levels at 30 mg/kg, po measured after 4 hrs2011Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs.
AID1242093Modulation of gamma-secretase in human SKNBE-2 cells transfected with wild type APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Potent benzoazepinone γ-secretase modulators with improved bioavailability.
AID715387Modulation of gamma-secretase assessed as reduction in amyloid beta 42 level by cell based assay2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Optimization of a natural product-based class of γ-secretase modulators.
AID715390Modulation of gamma-secretase assessed as increase in amyloid beta 38 level at 800 nM by cell based assay relative to control2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Optimization of a natural product-based class of γ-secretase modulators.
AID715389Modulation of gamma-secretase assessed as reduction in amyloid beta 40 level by cell based assay2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Optimization of a natural product-based class of γ-secretase modulators.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (62.50)24.3611
2020's3 (37.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.31

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 Index12.31 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]