Page last updated: 2024-11-12

gsk188909

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Description

GSK188909: a potent and selective non-peptidic BACE-1 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID15981486
CHEMBL ID253641
SCHEMBL ID5222560
MeSH IDM0507873

Synonyms (14)

Synonym
bdbm26788
gsk188909
bmcl181022 compound 23
3-(1,1-dioxo-1$l^{6},2-thiazinan-2-yl)-5-(ethylamino)-2-fluoro-n-[(2s,3r)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethyl)phenyl]methyl}amino)butan-2-yl]benzamide
CHEMBL253641
SCHEMBL5222560
unii-fc2vw8ejd2
3-(1,1-dioxotetrahydro-2h-1,2-thiazin-2-yl)-5-(ethylamino)-2-fluoro-n-((1s,2r)-2-hydroxy-1-(phenylmethyl)-3-(((3-(trifluoromethyl)phenyl)methyl)amino)propyl)benzamide
n-((2-(4-(2-ethyl-4,6-dimethyl-1h-imidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)carbamoyl)-4-methylbenzenesulfonamide
5-(ethylamino)-2-fluoro-n-((1s,2r)-2-hydroxy-1-(phenylmethyl)-3-(((3-(trifluoromethyl)phenyl)methyl)amino)propyl)-3-(tetrahydro-1,1-dioxido-2h-1,2-thiazin-2-yl)benzamide
benzamide, 5-(ethylamino)-2-fluoro-n-((1s,2r)-2-hydroxy-1-(phenylmethyl)-3-(((3-(trifluoromethyl)phenyl)methyl)amino)propyl)-3-(tetrahydro-1,1-dioxido-2h-1,2-thiazin-2-yl)-
fc2vw8ejd2 ,
dgeilirhsdutdk-xtepfmgcsa-n
3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)-2-fluoro-n-[(2s,3r)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]benzamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Amongst them, GSK188909 (compound 2) had favorable pharmacokinetics and was the first orally bioavailable inhibitor reported to demonstrate brain amyloid lowering in an animal model."( Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Charrier, N; Clarke, B; Cutler, L; Demont, E; Dingwall, C; Dunsdon, R; Hawkins, J; Howes, C; Hubbard, J; Hussain, I; Maile, G; Matico, R; Mosley, J; Naylor, A; O'Brien, A; Redshaw, S; Rowland, P; Smith, KJ; Soleil, V; Sweitzer, S; Theobald, P; Vesey, D; Walter, DS; Wayne, G, 2009
)
0.71

Dosage Studied

ExcerptRelevanceReference
" Encouragingly, subchronic dosing of GSK188909 in the absence of a p-glycoprotein inhibitor also lowers brain Abeta."( Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.
Buck, T; Cutler, L; Davis, JB; Demont, E; Dingwall, C; Gonzalez, MI; Harrison, D; Hawkins, J; Hille, C; Howes, C; Hussain, I; Jeffrey, P; Michel, A; Naylor, A; Redshaw, S; Walter, D; Wayne, G, 2007
)
0.61
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)100.00000.00011.774010.0000AID398148
Cathepsin DHomo sapiens (human)IC50 (µMol)1.09780.00000.931610.0000AID1798729; AID1799029; AID314038
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)1.00000.00011.753610.0000AID398152; AID398153
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)6.20000.00002.015110.0000AID398151
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)9.00000.00002.800510.0000AID398149
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)10.00000.00002.398310.0000AID398150
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00200.00030.38877.0000AID398145
Beta-secretase 1Homo sapiens (human)IC50 (µMol)0.24540.00061.619410.0000AID1798729; AID1799029; AID314036; AID314040; AID314041; AID314042; AID314043; AID398145; AID398146; AID398147
Beta-secretase 2Homo sapiens (human)IC50 (µMol)0.60260.00090.64922.8800AID1798729; AID1799029; AID314037
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (70)

Processvia Protein(s)Taxonomy
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
autophagosome assemblyCathepsin DHomo sapiens (human)
proteolysisCathepsin DHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IICathepsin DHomo sapiens (human)
insulin receptor recyclingCathepsin DHomo sapiens (human)
lipoprotein catabolic processCathepsin DHomo sapiens (human)
positive regulation of apoptotic processCathepsin DHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processCathepsin DHomo sapiens (human)
regulation of establishment of protein localizationCathepsin DHomo sapiens (human)
insulin catabolic processCathepsin DHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
proteolysisBeta-secretase 1Homo sapiens (human)
membrane protein ectodomain proteolysisBeta-secretase 1Homo sapiens (human)
response to lead ionBeta-secretase 1Homo sapiens (human)
protein processingBeta-secretase 1Homo sapiens (human)
amyloid-beta formationBeta-secretase 1Homo sapiens (human)
amyloid precursor protein catabolic processBeta-secretase 1Homo sapiens (human)
positive regulation of neuron apoptotic processBeta-secretase 1Homo sapiens (human)
amyloid-beta metabolic processBeta-secretase 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painBeta-secretase 1Homo sapiens (human)
prepulse inhibitionBeta-secretase 1Homo sapiens (human)
cellular response to copper ionBeta-secretase 1Homo sapiens (human)
cellular response to manganese ionBeta-secretase 1Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionBeta-secretase 1Homo sapiens (human)
signaling receptor ligand precursor processingBeta-secretase 1Homo sapiens (human)
cellular response to amyloid-betaBeta-secretase 1Homo sapiens (human)
amyloid fibril formationBeta-secretase 1Homo sapiens (human)
proteolysisBeta-secretase 2Homo sapiens (human)
membrane protein ectodomain proteolysisBeta-secretase 2Homo sapiens (human)
protein processingBeta-secretase 2Homo sapiens (human)
peptide hormone processingBeta-secretase 2Homo sapiens (human)
melanosome organizationBeta-secretase 2Homo sapiens (human)
glucose homeostasisBeta-secretase 2Homo sapiens (human)
negative regulation of amyloid precursor protein biosynthetic processBeta-secretase 2Homo sapiens (human)
amyloid-beta metabolic processBeta-secretase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (42)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
cysteine-type endopeptidase activityCathepsin DHomo sapiens (human)
protein bindingCathepsin DHomo sapiens (human)
peptidase activityCathepsin DHomo sapiens (human)
aspartic-type peptidase activityCathepsin DHomo sapiens (human)
aspartic-type endopeptidase activityCathepsin DHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
amyloid-beta bindingBeta-secretase 1Homo sapiens (human)
endopeptidase activityBeta-secretase 1Homo sapiens (human)
aspartic-type endopeptidase activityBeta-secretase 1Homo sapiens (human)
protein bindingBeta-secretase 1Homo sapiens (human)
peptidase activityBeta-secretase 1Homo sapiens (human)
beta-aspartyl-peptidase activityBeta-secretase 1Homo sapiens (human)
enzyme bindingBeta-secretase 1Homo sapiens (human)
protein serine/threonine kinase bindingBeta-secretase 1Homo sapiens (human)
aspartic-type endopeptidase activityBeta-secretase 2Homo sapiens (human)
protein bindingBeta-secretase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
collagen-containing extracellular matrixCathepsin DHomo sapiens (human)
extracellular regionCathepsin DHomo sapiens (human)
extracellular spaceCathepsin DHomo sapiens (human)
lysosomeCathepsin DHomo sapiens (human)
lysosomal membraneCathepsin DHomo sapiens (human)
endosome membraneCathepsin DHomo sapiens (human)
endosome lumenCathepsin DHomo sapiens (human)
specific granule lumenCathepsin DHomo sapiens (human)
melanosomeCathepsin DHomo sapiens (human)
lysosomal lumenCathepsin DHomo sapiens (human)
membrane raftCathepsin DHomo sapiens (human)
collagen-containing extracellular matrixCathepsin DHomo sapiens (human)
extracellular exosomeCathepsin DHomo sapiens (human)
tertiary granule lumenCathepsin DHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin DHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
lysosomeBeta-secretase 1Homo sapiens (human)
endosomeBeta-secretase 1Homo sapiens (human)
early endosomeBeta-secretase 1Homo sapiens (human)
late endosomeBeta-secretase 1Homo sapiens (human)
multivesicular bodyBeta-secretase 1Homo sapiens (human)
endoplasmic reticulum lumenBeta-secretase 1Homo sapiens (human)
Golgi apparatusBeta-secretase 1Homo sapiens (human)
trans-Golgi networkBeta-secretase 1Homo sapiens (human)
plasma membraneBeta-secretase 1Homo sapiens (human)
synaptic vesicleBeta-secretase 1Homo sapiens (human)
cell surfaceBeta-secretase 1Homo sapiens (human)
endosome membraneBeta-secretase 1Homo sapiens (human)
membraneBeta-secretase 1Homo sapiens (human)
axonBeta-secretase 1Homo sapiens (human)
dendriteBeta-secretase 1Homo sapiens (human)
neuronal cell bodyBeta-secretase 1Homo sapiens (human)
membrane raftBeta-secretase 1Homo sapiens (human)
recycling endosomeBeta-secretase 1Homo sapiens (human)
Golgi-associated vesicle lumenBeta-secretase 1Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseBeta-secretase 1Homo sapiens (human)
endosomeBeta-secretase 1Homo sapiens (human)
plasma membraneBeta-secretase 1Homo sapiens (human)
trans-Golgi networkBeta-secretase 1Homo sapiens (human)
endoplasmic reticulumBeta-secretase 2Homo sapiens (human)
Golgi apparatusBeta-secretase 2Homo sapiens (human)
plasma membraneBeta-secretase 2Homo sapiens (human)
membraneBeta-secretase 2Homo sapiens (human)
melanosome membraneBeta-secretase 2Homo sapiens (human)
plasma membraneBeta-secretase 2Homo sapiens (human)
trans-Golgi networkBeta-secretase 2Homo sapiens (human)
endosomeBeta-secretase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID398154Intrinsic clearance in mouse liver microsomes measured per gram of liver2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398143AUC/dose in rat at 3 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398157Lipophilicity, log D at pH 7.42009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398155Intrinsic clearance in rat liver microsomes measured per gram of liver2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398168AUC/dose in rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314042Inhibition of BACE1 assessed as amyloid beta40 production in human SHSY5Y-APP-swe cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398150Inhibition of CYP2C192009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398146Inhibition of BACE in human SHSY5Y cells expressing wild-type APP assessed as inhibition of intracellular amyloid beta-402009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314045Decrease in amyloid beta42 in TASTPM mouse brain at 250 mg/kg, po after 5 days2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398167Half life in rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314036Inhibition of BACE1 expressed in CHO cells by FRET assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID314046Decrease in amyloid beta40 in TASTPM mouse brain at 250 mg/kg, po after 5 days in presence of Pgp inhibitor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398153Inhibition of CYP3A4 using 7-benzyloxyquinoline as substrate2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398156Intrinsic clearance in human liver microsomes measured per gram of liver2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314043Inhibition of BACE1 assessed as amyloid beta42 production in human SHSY5Y-APP-swe cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398152Inhibition of CYP3A4 using diethoxyfluorescein as substrate2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398145Inhibition of BACE2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398160Volume of distribution at steady state in iv dosed rat2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314047Decrease in amyloid beta42 in TASTPM mouse brain at 250 mg/kg, po after 5 days in presence of Pgp inhibitor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398162Bioavailability in ipv dosed rat2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398149Inhibition of CYP2C92009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314044Decrease in amyloid beta40 in TASTPM mouse brain at 250 mg/kg, po after 5 days2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398161Half life in iv dosed rat2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398165Half life in rat at 3 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398151Inhibition of CYP2D62009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398147Inhibition of BACE in human SHSY5Y cells expressing swedish-mutant APP assessed as inhibition of intracellular amyloid beta-402009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398159Blood clearance in iv dosed rat administered as saline containing kleptose2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314040Inhibition of BACE1 assessed as amyloid beta40 production in human SHSY5Y-APP-wt cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID314041Inhibition of BACE1 assessed as amyloid beta42 production in human SHSY5Y-APP-wt cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398164Oral bioavailability in rat at 3 mg/kg2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID398148Inhibition of CYP1A22009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314037Inhibition of BACE2 expressed in CHO cells by FRET assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID398166Oral bioavailability in rat at 10 mg/kg administered as tween solution containing aqueous methylcellulose2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
AID314038Inhibition of Cathepsin D expressed in CHO cells by FRET assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID1798729Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2007.12.020: \\BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.\\2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
AID1799029Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2009.03.165: \\Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.\\2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (100.00)29.6817
2010's0 (0.00)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: 12.56

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 Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]