Page last updated: 2024-12-05

donepezil hydrochloride

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

Description

donepezil hydrochloride : A racemate comprising equimolar amounts of (R)- and (S)- donepezil hydrochloride. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5741
CHEMBL ID1678
CHEBI ID4696
SCHEMBL ID1815
MeSH IDM0206791

Synonyms (117)

Synonym
AC-913
2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1h-inden-1-one hydrochloride
donepezil (hydrochloride)
HY-B0034
aricept d
memac
donepezil hydrochloride
aricept odt
e-2022 ,
bnag
eranz
e-2020 ,
aricept evess
memorit
e 2020 (pharmaceutical)
1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine hcl
e 2020
(+-)-2-((1-benzyl-4-piperidyl)methyl)-5,6-dimethoxy-1-indanone hydrochloride
donepezil hydrochloride [usan]
c24h29no3.hcl
1h-inden-1-one, 2,3-dihydro-5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)-, hydrochloride
MLS000758276
smr000449292
chembl1678 ,
120011-70-3
donepezil hydrochloride (jp17/usp)
aricept (tn)
D00670
nsc737535
(+-)-2,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1h-inden-1-one hydrochloride
nsc-737535
MLS001401387
1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine hydrochloride
AKOS000277343
nsc-758882
adlarity
donepezil hcl
chebi:4696
A804411
2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydro-1h-inden-1-one hydrochloride
tox21_112534
dtxsid0046698 ,
cas-120011-70-3
dtxcid8026698
pharmakon1600-01504403
nsc758882
D4099
2-(1-benzyl-4-piperidylmethyl)-5,6-dimethoxy-1-indanone hydrochloride
CCG-101043
unii-3o2t2pj89d
3o2t2pj89d ,
donepezil hydrochloride [usan:usp]
FT-0602354
FT-0625589
CS-0863
S2462
AKOS016340656
donepezil hydrochloride [jan]
donepezil hydrochloride component of namzaric
donepezil hydrochloride [who-dd]
namzaric component donepezil hydrochloride
donepezil hydrochloride [mart.]
donepezil hydrochloride [orange book]
donepezil hydrochloride [usp-rs]
donepezil hydrochloride [usp monograph]
donepezil hydrochloride [mi]
(+/-)-2-((1-benzyl-4-piperidyl)methyl)-5,6-dimethoxy-1-indanone hydrochloride
donepezil hydrochloride [vandf]
donepezil hydrochloride [ep monograph]
CCG-213309
XWAIAVWHZJNZQQ-UHFFFAOYSA-N
NC00293
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1h-inden-1-one hydrochloride
SCHEMBL1815
tox21_112534_1
NCGC00167537-02
KS-1051
Q-201040
2-(1-benzyl-piperidin-4-ylmethyl)-5,6-dimethoxy-indan-1-one hydrochloride
Q-100096
(r)(+) dichlorophenyl amino alcohol
e2020;e-2020
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;hydrochloride
mfcd00881312
donepezil hydrochloride monohydrate, >=98% (hplc)
donepezil hydrochloride 1.0 mg/ml in methanol (as free base)
donepezil hydrochloride; 1h-inden-1-one, 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-, hydrochloride (9ci); aricept; aricept d; bnag; e 2020
donepezilhcl
1h-inden-1-one, 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-, hydrochloride (1:1)
110119-84-1
BCP24884
donepezil hcl (aricept)
donepezil hydrochloride,(s)
Q27106438
2,3-dihydro-5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)-1h-inden-1-one hcl
BCP02205
AMY40527
120011-70-3 (hcl)
2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]-1h-inden-1-one
donepezil hcl - bio-x
BD164380
HB2083
donepezil,hcl
EN300-269733
donepezil, hcl
donepezil hydrochloride (usp monograph)
(2rs)-2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydro-1h-inden-1-one monohydrochloride
rac-1-benzyl-4-((5,6-dimethoxy-1-oxo-2,3-dihydro-1h-inden-2-yl)methyl)piperidinium chloride
donepezil hydrochloride (mart.)
rac-2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxyindan-1-one hydrochloride
donepezil hydrochloride (ep monograph)
ariceptodt
donepezil hydrochloride10mg
donepezil hydrochloride (usp-rs)
donepezil hydrochloride (usan:usp)
donepezil hydrochloride5 mg
donepezil hyrochloride5mg

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Intravenous and oral 6-h blood sampling profiles in old (30 months old) and young (7 months old) rats revealed pharmacokinetic changes similar to those in humans with an approximately 40% increase in C(max) of galantamine and prolonged t(1/2) (1."( Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
Aw, CC; Browne, ER; Chen, CP; Goh, CW; Lee, JH, 2011
)
0.37

Bioavailability

ExcerptReferenceRelevance
"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 (32)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
acetylcholinesteraseHomo sapiens (human)Potency0.33940.002541.796015,848.9004AID1347395; AID1347397; AID1347398; AID1347399
USP1 protein, partialHomo sapiens (human)Potency79.43280.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686978
GLI family zinc finger 3Homo sapiens (human)Potency33.49150.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency12.91690.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency7.49780.000657.913322,387.1992AID1259378
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.67300.01237.983543.2770AID1346984; AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency9.25150.003041.611522,387.1992AID1159552; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.15670.001530.607315,848.9004AID1224841; AID1224842; AID1259401
pregnane X nuclear receptorHomo sapiens (human)Potency15.84890.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.05000.000229.305416,493.5996AID743075; AID743078; AID743079; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency17.37680.00108.379861.1304AID1645840
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency10.59010.001019.414170.9645AID743191
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency14.96010.001723.839378.1014AID743083
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency39.81073.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency12.58930.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency27.66440.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency8.46780.000627.21521,122.0200AID743202; AID743219
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency14.12540.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency14.12540.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency14.12540.15855.287912.5893AID540303
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[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)
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)0.07090.00000.94539.9400AID1198359; AID501762; AID603289; AID638225; AID719018; AID739639; AID753136; AID757776
AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC50 (µMol)0.00570.00570.42855.1200AID404434
CholinesteraseHomo sapiens (human)IC50 (µMol)7.18300.00001.559910.0000AID404844; AID44437
AcetylcholinesteraseMus musculus (house mouse)IC50 (µMol)0.00570.00071.11818.4000AID31781
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)0.04310.00000.933210.0000AID1173565; AID1467548; AID404843; AID592640; AID621448
Acetylcholinesterase Bos taurus (cattle)IC50 (µMol)0.00810.00000.61068.7000AID404842
CholinesteraseEquus caballus (horse)IC50 (µMol)4.68000.00002.22149.4000AID1126596; AID1497848; AID621449; AID719017; AID753135
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC50 (µMol)7.13800.00041.48119.8700AID44437
Carboxylic ester hydrolase Equus caballus (horse)IC50 (µMol)3.60000.00512.69848.5000AID592641
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
amyloid-beta bindingAcetylcholinesterase Bos taurus (cattle)
protein bindingAcetylcholinesterase Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesterase Bos taurus (cattle)
side of membraneAcetylcholinesterase Bos taurus (cattle)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (144)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347154Primary 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.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID621449Inhibition of equine BuChE by Ellman's method2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation.
AID1357834Cognitive enhancing effect in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment increase in time spent in target quadrant by measuring increase in number of platform crossings at 1.3 mg/kg/day, po starting from day 1 of amyl2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID44437Butyrylcholinesterase1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
AID1220488Oral bioavailability in human at 2 mg single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220513Blood clearance in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220479Inhibition of cholinesterase activity in 7 months-old Lister Hooded rat brain at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1332153Effective permeability of the compound at pH 7.4 by BBB-PAMPA method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents.
AID404847Inhibition of human AChE assessed as reduction of thioflavin T fluorescence at 100 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID1220499Drug uptake in 7 months-old Lister Hooded rat blood at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID404843Inhibition of human erythrocyte AChE by Ellman's assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID1220501Ratio of brain to blood in 7 months-old Lister Hooded rat blood at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220480Inhibition of cholinesterase activity in 7 months-old Lister Hooded rat plasma at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID592643Inhibition of human AChE-induced amyloid beta (1-40) aggregation at 100 uM after 24 hrs by thioflavin T based fluorometric assay2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors.
AID1220493Inhibition of cholinesterase activity in old F344 rat brain at 2.5 mg/kg, po after 1 hr treatment relative to 7 months-old Lister Hooded rat2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1198359Inhibition of electric eel AChE using acetylthiocholine substrate by Ellman's reagent based method2015European journal of medicinal chemistry, Mar-26, Volume: 93Benzofuran-derived benzylpyridinium bromides as potent acetylcholinesterase inhibitors.
AID621451Inhibition of human AChE-induced amyloid beta (1-40) aggregation at 100 uM after 24 hrs by thioflavin T-based fluorometric assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation.
AID1515409Inhibition of AChE in Swiss mouse brain homogenate using acetylthiocholine iodide as substrate by Ellman's assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor.
AID1357832Toxicity in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as effect on number of arm entries at 1.3 mg/kg/day, po starting from day 1 of amyloid beta (1 to 42) oligomer treatment and measured on day 7 by Y-maze 2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID638225Inhibition of electric eel AChE using acetylcholine as substrate measured every sec for 2 mins by Ellman's method2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3″]-2,3-dihydro-1H-inden-1″-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole.
AID1220474Cmax in 30 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220457Volume of distribution in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220469Volume of distribution in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220486Volume of distribution in human at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220472Dose normalized AUC (0 to t) in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220466Oral bioavailability in 7 months-old Lister Hooded rat at 3 mg/kg2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1357831Cognitive enhancing effect in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as reduction in spontaneous alternation behaviors at 1.3 mg/kg/day, po starting from day 1 of amyloid beta (1 to 42) oligomer treatment2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID603289Inhibition of electric eel AChE by modified Ellman method2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis and discovery of novel hexacyclic cage compounds as inhibitors of acetylcholinesterase.
AID1730631Reversal of scopolamine-induced memory impairment in Kunming mouse assessed as decrease in number of errors at 10 mg/kg, po treated 1 hr before training trial measured 24 hrs after training trial by step-down passive avoidance test2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1220473Dose normalized AUC (0 to infinity) in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220470Half life in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1357836Cognitive enhancing effect in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as induction of fewer entries into dark compartment at 1.3 mg/kg, po starting from day 1 of amyloid beta (1 to 42) oligomer treatment a2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID1126594Inhibition of electric eel AChE type VI-S using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins prior to substrate challenge for 15 mins by Ellman's method2014European journal of medicinal chemistry, May-06, Volume: 78Novel structural hybrids of pyrazolobenzothiazines with benzimidazoles as cholinesterase inhibitors.
AID1220512Cmax in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1515413In vivo inhibition of BuChE in Swiss mouse liver at 3 to 6 mg/kg, iv by Ellman's assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor.
AID1220478Oral bioavailability in 30 months-old Lister Hooded rat at 3 mg/kg2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID739639Inhibition of electric eel AChE after 30 mins by Ellman's method2013Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
A one-pot domino synthesis and discovery of highly functionalized dihydrobenzo[b]thiophenes as AChE inhibitors.
AID1220476Dose normalized AUC (0 to t) in 30 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220463Tmax in 7 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID592640Inhibition of human AChE incubated with compounf for 5 mins before addition of substrate acetylthiocholine iodide by Ellman's method2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors.
AID1220464Dose normalized AUC (0 to t) in 7 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID753136Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins prior to substrate addition by Ellman's method2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and evaluation of 4-substituted coumarins as novel acetylcholinesterase inhibitors.
AID1220465Dose normalized AUC (0 to infinity) in 7 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID31781Inhibitory activity against acetylcholinesterase1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
AID1357833Memory enhancing effect in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as increase in preferential index in retention session of 1 hr at 1.3 mg/kg/day, po starting from day 1 of amyloid beta (1 to 42) oligomer2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID621448Inhibition of human AChE by Ellman's assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation.
AID621450Selectivity index, ratio of IC50 for human AChE to IC50 for equine BuChE2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation.
AID1220494Inhibition of acetylcholinesterase activity in 7 months-old Lister Hooded rat plasma at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220498Inhibition of cholinesterase activity in 30 months-old Lister Hooded rat plasma assessed as percent enhancement of inhibition at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID404848Inhibition of human recombinant AChE-induced amyloid beta 1-40 aggregation at 100 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID1357829Neuroprotective activity amyloid beta (1 to 42) oligomer-induced memory impaired Kunming mouse assessed as reduction in apoptotic cells in CA1 and CA3 hipocampal neurons at 1.3 mg/kg, po starting from day 1 of amyloid beta (1 to 42) oligomer treatment and2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID592641Inhibition of equine BChE incubated with compounf for 5 mins before addition of substrate S-butyrylthiocholine iodide by Ellman's method2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors.
AID757776Inhibition of electric eel AChE after 30 mins by Ellman's method2013European journal of medicinal chemistry, Jul, Volume: 65An atom economic synthesis and AChE inhibitory activity of novel dispiro 7-aryltetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole and 4-aryloctahydroindolizine N-methylpiperidin-4-one hybrid heterocycles.
AID1220460Dose normalized AUC (0 to t) in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220458Half life in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220467Cmax in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220461Dose normalized AUC (0 to infinity) in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID719015Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.
AID404842Inhibition of bovine erythrocyte AChE by Ellman's assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID1497848Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate pretreated for 15 mins followed by substrate addition measured for 6 mins by Ellman's method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID1467548Inhibition of AChE (unknown origin) using acetylcholine as substrate preincubated for 15 mins followed by substrate addition measured every minute by spectrophotometric analysis2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
One-pot microwave assisted stereoselective synthesis of novel dihydro-2'H-spiro[indene-2,1'-pyrrolo-[3,4-c]pyrrole]-tetraones and evaluation of their antimycobacterial activity and inhibition of AChE.
AID1220491Drug excretion in human feces at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1515412In vivo inhibition of AChE in Swiss mouse brain assessed as enzyme activity at 3 mg/kg, iv by Ellman's assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor.
AID1357837Neuroprotective activity in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as reduction in neural degeneration in CA1 region at 1.3 mg/kg, po starting from day 1 of amyloid beta (1 to 42) oligomer treatment and m2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID1220489Drug excretion in human urine at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1472432Reversal of scopolamine-induced memory impairment in C57BL/6J mouse assessed as decrease in traveled distance to reach the escape platform at 10 mg/kg, ip administered 60 mins prior to test post scopolamine challenge measured on day 7 by Morris water maze2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
AID621452Inhibition of amyloid beta (1 to 40) self-aggregation at 100 uM after 24 hrs by thioflavin T-based fluorometric assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation.
AID404434Inhibition of Torpedo californica AChE2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
AID1220487Clearance in human at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220485Half life in human at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220459Mean residence time in 7 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1730630Reversal of scopolamine-induced memory impairment in Kunming mouse assessed as increase in latency time at 10 mg/kg, po treated 1 hr before training trial measured 24 hrs after training trial by step-down passive avoidance test2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1220502Drug uptake in 30 months-old Lister Hooded rat blood at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID719018Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.
AID1515416Inhibition of AChE in Swiss mouse liver homogenate using acetylthiocholine iodide as substrate by Ellman's assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor.
AID1220490Drug excretion in human urine assessed as unchanged drug level at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1472429Reversal of scopolamine-induced memory loss in C57BL/6J mouse assessed as decrease in escape latency time at 10 mg/kg, ip administered 60 mins prior to test post scopolamine-challenge measured on day 7 by Morris water maze test2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
AID1220477Dose normalized AUC (0 to infinity) in 30 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220481Inhibition of acetylcholinesterase activity in 7 months-old Lister Hooded rat brain at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220471Mean residence time in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID501762Inhibition of electric eel AChE by Ellman's method2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Design, synthesis and anticholinesterase activity of a novel series of 1-benzyl-4-((6-alkoxy-3-oxobenzofuran-2(3H)-ylidene) methyl) pyridinium derivatives.
AID1220483Plasma protein binding in human at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1515411Inhibition of BuChE in Swiss mouse liver homogenate by Ellman's assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor.
AID1220500Drug uptake in 7 months-old Lister Hooded rat assessed as corrected brain concentration at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID753135Inhibition of equine serum BChE using butylthiocholine iodide as substrate preincubated for 10 mins prior to substrate addition by Ellman's method2013European journal of medicinal chemistry, Jun, Volume: 64Synthesis and evaluation of 4-substituted coumarins as novel acetylcholinesterase inhibitors.
AID1220462Cmax in 7 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220468Blood clearance in 30 months-old Lister Hooded rat at 1 mg/kg, iv infusion for 1 hr2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220492Inhibition of cholinesterase activity in F344 rat brain at 2.5 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID229262Ratio of IC50 for BuChE to AChE1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
AID1472436Reversal of scopolamine-induced hyperlocomotion in C57BL/6J mouse assessed as speed of swimming at 10 mg/kg, ip administered 60 mins prior to test post scopolamine challenge measured on day 7 by Morris water maze test (Rvb = 0.20 meter/s)2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
AID1220503Drug uptake in 30 months-old Lister Hooded rat assessed as corrected brain concentration at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1220484Tmax in human at 2 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1357838Neuroprotective activity in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as reduction in neuronal degeneration by measuring clear and intact neurons in CA1 and CA3 region at 1.3 mg/kg, po starting from day 1 of2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID404844Inhibition of human serum BChE by Ellman's assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
AID1220475Tmax in 30 months-old Lister Hooded rat at 3 mg/kg, po2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID719017Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate by Ellman's method2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.
AID1220504Ratio of brain to blood in 30 months-old Lister Hooded rat blood at 3 mg/kg, po after 1 hr treatment2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
AID1357839Neuroprotective activity in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as reduction in neuronal degeneration by measuring reduction in degenerative changes in nucleus of CA1 and CA3 region at 1.3 mg/kg, po st2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID1126596Inhibition of BuChE in equine serum using butyrylthiocholine chloride as substrate preincubated with enzyme for 10 mins prior to substrate challenge for 15 mins by Ellman's method2014European journal of medicinal chemistry, May-06, Volume: 78Novel structural hybrids of pyrazolobenzothiazines with benzimidazoles as cholinesterase inhibitors.
AID1173565Inhibition of AChE (unknown origin) assessed as inhibition of acetylcholine hydrolysis preincubated for 15 mins by Ellman method2014Journal of natural products, Dec-26, Volume: 77, Issue:12
Anithiactins A-C, modified 2-phenylthiazoles from a mudflat-derived Streptomyces sp.
AID1357835Cognitive enhancing effect in Kunming mouse model of amyloid beta (1 to 42) oligomer-induced memory impairment assessed as longer escape latency at 1.3 mg/kg, po starting from day 1 of amyloid beta (1 to 42) oligomer treatment and measured on day 7 by pas2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (36)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (2.78)18.2507
2000's3 (8.33)29.6817
2010's25 (69.44)24.3611
2020's7 (19.44)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 78.20

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index78.20 (24.57)
Research Supply Index3.61 (2.92)
Research Growth Index5.50 (4.65)
Search Engine Demand Index131.09 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (78.20)

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%
Other36 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]