Page last updated: 2024-11-13

ass234

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Cross-References

ID SourceID
PubMed CID53378764
CHEMBL ID1929421
SCHEMBL ID6847307
MeSH IDM000598782

Synonyms (13)

Synonym
bdbm50359391
CHEMBL1929421 ,
n-[[5-[3-(1-benzylpiperidin-4-yl)propoxy]-1-methylindol-2-yl]methyl]-n-methylprop-2-yn-1-amine
ass234
gtpl7369
SCHEMBL6847307
us8999994, 6
bdbm153654
Q27074552
1334106-34-1
AKOS040750606
HY-121072
CS-0079412
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)0.35000.00000.94539.9400AID1076176; AID1421465; AID635870
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki0.14900.00121.25638.9000AID635876
CholinesteraseHomo sapiens (human)IC50 (µMol)2.09200.00001.559910.0000AID1195743; AID1540204; AID1545349; AID1656491; AID635875
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50 (µMol)0.04300.00040.764912.5000AID1421464; AID1555512; AID635878
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki0.01100.00081.09276.0000AID635886
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50 (µMol)0.00520.00071.979812.5000AID1421463; AID1555511; AID635877
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)0.01690.00002.37899.7700AID1076173; AID1195740; AID1540202; AID1545345; AID1545347; AID1656488
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)1.09330.00000.933210.0000AID1195742; AID1540200; AID1545348; AID1555507; AID1656490; AID635874
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)0.80930.00001.89149.5700AID1076172; AID1195741; AID1540203; AID1545346; AID1545351; AID1656489
Beta-secretase 1Homo sapiens (human)IC50 (µMol)0.46000.00061.619410.0000AID1555508
CholinesteraseEquus caballus (horse)IC50 (µMol)0.46000.00002.22149.4000AID1076175; AID1421466; AID635871
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki0.00260.00130.56224.5230AID1506088
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.00280.00000.490110.0000AID1506085
Histamine H3 receptorHomo sapiens (human)Ki0.08420.00010.33998.5110AID1540197; AID1545350
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (65)

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)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo 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)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo 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)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

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)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo 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)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo 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)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (47)

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)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo 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)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo 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)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (68)

Assay IDTitleYearJournalArticle
AID1540202Inhibition of human MAOA2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID1545349Inhibition of human plasma butyrylcholinesterase by Ellman's method2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID635883Time-dependent inhibition of rat liver mitochondrial MAO-B using phenylethylamine at 45 nM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID635885Irreversible inhibition of rat liver mitochondrial MAO-B using phenylethylamine as substrate assessed as substrate consumption at 100 nM measured up to 420 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1545350Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID635918Irreversible inhibition of rat liver mitochondrial MAO-A using 5-hydroxytriptamine as substrate assessed as substrate consumption at 10 nM preincubated for 30 mins measured up to 420 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1545348Inhibition of human acetylcholinesterase expressed in HEK 293 cells using acetylthiocholine iodide as substrate by Ellman's method2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID635878Inhibition of rat liver mitochondrial MAO-B using [14C]-phenylethylamine after 30 mins by scintillation counting2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID635880Irreversible inhibition of rat liver mitochondrial MAO-A using 5-hydroxytryptamine as substrate at 6 nM preincubated for 30 mins measured after three consecutive washes with buffer2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1555512Inhibition of rat liver mitochondrial MAOB using [14C]-PEA as substrate preincubated for 30 mins followed by substrate addition by liquid scintillation counting analysis2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID635882Reversible inhibition of rat liver mitochondrial MAO-B using phenylethylamine assessed as recovered enzyme activity at 45 nM preincubated for 30 mins measured after three consecutive washes with buffer2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1076175Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 25 mins by Ellman's method2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1506096Cognitive enhancing effect in amyloid beta (1 to 42)-induced dementia Balb/c mouse model assessed as protection against spatial memory impairment by measuring latency to find food on fourth day of test at 1 to 10 mg/kg, po qd via gavage for 17 days starti2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID635874Inhibition of cerebral human recombinant AchE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1076174Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1195741Inhibition of human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 15 mins2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
AID1195746Selectivity ratio of IC50 for recombinant human AChE expressed in HEK293 cells to IC50 for recombinant human BuChE expressed in HEK293 cells2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
AID635884Irreversible inhibition of rat liver mitochondrial MAO-A using 5-hydroxytriptamine as substrate assessed as substrate consumption at 10 nM measured up to 420 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1195745Selectivity ratio of IC50 for human MAO-A expressed in baculovirus infected BTI insect cells to IC50 for human MAO-B expressed in baculovirus infected BTI insect cells2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
AID1506085Displacement of (+)-[3H]pentazocine from human sigma1 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1506099Cognitive enhancing effect in amyloid beta (1 to 42)-induced dementia Balb/c mouse model assessed as protection against spatial memory impairment by measuring reduction in total errors to find food on third and fourth days of test at 1 to 10 mg/kg, po qd 2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID635876Mixed type inhibition of Electrophorus electricus AchE using acetylthiocholine as substrate by Line-Weaver Burk plot analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1656490Inhibition of human AChE2020Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
AID1506088Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1195742Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
AID1506089Selectivity ratio of Ki for sigma2 receptor in rat liver membranes to Ki for human sigma1 receptor expressed in HEK293 cell membranes2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1656491Inhibition of human BuChE2020Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
AID1540200Inhibition of human AChE2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID1555508Inhibition of BACE-1 (unknown origin)2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID635919Reversible inhibition of rat liver mitochondrial MAO-B using phenylethylamine as substrate assessed as substrate consumption at 100 nM preincubated for 30 mins measured up to 420 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1506092Cognitive enhancing effect in Balb/c mouse assessed as protection against amyloid beta (1 to 42) oligomers-induced memory damage at 1 to 10 mg/kg, po qd via gavage for 17 days starting from 24 hrs post amyloid beta (1 to 42) oligomer treatment measured on2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1540197Inhibition of human histamine H3 receptor2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID635888Inhibition of human AChE-induced amyloid beta (1 to 40) aggregation at 100 uM measured every 10 mins for 10 hrs by thioflavin T-based fluorometric analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1545347Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition by Amplex red reagent/horseradish peroxidase coupled fluorescence assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1555513Inhibition of beta amyloid (unknown origin) self-induced aggregation at 10 uM relative to control2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID1540203Inhibition of human MAOB2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID635870Inhibition of Electrophorus electricus AchE using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID635873Ratio of donepezil IC50 to compound IC50 for equine serum BuchE using butyrylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID635877Inhibition of rat liver mitochondrial MAO-A using [14C]-5-hydroxytryptamine after 30 mins by scintillation counting2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1421464Inhibition of rat liver mitochondrial MAOB using [14C]-PEA as substrate preincubated for 30 mins followed by substrate addition measured after 2 mins by liquid scintillation counting analysis2018European journal of medicinal chemistry, Oct-05, Volume: 158Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.
AID635875Inhibition of human serum BuchE using butyrylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID635886Non-competitive inhibition of rat liver mitochondrial MAO-B using phenylethylamine as substrate by Line-Weaver Burk plot analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1421466Inhibition of BuChE (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.
AID1506091In vivo antagonist activity at sigma1 receptor in sc dosed capsaicin-induced mechanical allodynia CD-1 mouse model assessed as increase in paw withdrawal latency pretreated for 30 mins followed by capsaicin treatment measured after 2 hrs2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1540204Inhibition of human BChE2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID1555511Inhibition of rat liver mitochondrial MAOA [14C]-5-HT as substrate preincubated for 30 mins followed by substrate addition by liquid scintillation counting analysis2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID1656489Inhibition of human MAO B2020Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
AID1555514Inhibition of AChE (unknown origin)-induced beta amyloid (unknown origin) aggregation at 100 uM relative to control2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID1545351Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition by Amplex red reagent/horseradish peroxidase coupled fluorescence assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID635872Selectivity ratio of IC50 for equine serum BuchE to IC50 for Electrophorus electricus AchE2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1421463Inhibition of rat liver mitochondrial MAOA using [14C]-5-HT as substrate preincubated for 30 mins followed by substrate addition measured after 10 mins by liquid scintillation counting analysis2018European journal of medicinal chemistry, Oct-05, Volume: 158Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.
AID1195740Inhibition of human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 15 mins2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
AID635887Inhibition of self-induced amyloid beta (1 to 42) aggregation at 10 uM measured every 10 mins for 10 hrs by thioflavin T-based fluorometric analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1555507Inhibition of AChE (unknown origin)2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID635820Irreversible inhibition of rat liver mitochondrial MAO-A using 5-hydroxytryptamine as substrate at 6 nM preincubated for 30 mins measured after three consecutive centrifugation2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID635879Selectivity ratio of IC50 for rat liver mitochondrial MAO-B to IC50 for rat liver mitochondrial MAO-A2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1076172Inhibition of human recombinant MAO-B using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1506087Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1076177Selectivity ratio of IC50 for human recombinant MAO-B to IC50 for human recombinant MAO-A2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1545346Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1421465Inhibition of AChE (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.
AID635881Time-dependent inhibition of rat liver mitochondrial MAO-A using 5-hydroxytryptamine at 6 nM by scintillation counting2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1076173Inhibition of human recombinant MAO-A using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1076176Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID1195743Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
AID1545345Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID635871Inhibition of equine serum BuchE using butyrylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di
AID1656488Inhibition of human MAO A2020Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (88.89)24.3611
2020's1 (11.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.50

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index21.50 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (55.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (44.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]