Page last updated: 2024-12-05

vesamicol

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Description

vesamicol: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID212231
CHEMBL ID1256846
MeSH IDM0048443
PubMed CID659840
CHEMBL ID20730
CHEBI ID92261
SCHEMBL ID4499985
MeSH IDM0048443
PubMed CID5662
CHEMBL ID20943
CHEBI ID103974
SCHEMBL ID571598
MeSH IDM0048443

Synonyms (150)

Synonym
EU-0101228
(+/-)-vesamicol hydrochloride, >98%, solid
2-(4-phenylpiperidino)cyclohexanol hydrochloride
cyclohexanol, 2-(4-phenylpiperidino)-, hydrochloride
ah 5183 hydrochloride
vesamicol hydrochloride
NCGC00094470-03
NCGC00094470-02
SPECTRUM2300309
(?)-vesamicol hydrochloride
NCGC00094470-04
NCGC00094470-01
( inverted question mark)-vesamicol hydrochloride
120447-62-3
23965-53-9
HMS1570H22
HMS1922L20
l(-)-vesamicol hydrochloride
2-(4-phenylpiperidin-1-yl)cyclohexan-1-ol hydrochloride
CHEMBL1256846
(+/-)-vesamicol hcl
nsc759580
nsc-759580
pharmakon1600-02300309
(+/-)-vesamicol hcl (ah-5183)
LP01228
CCG-222532
tox21_501228
NCGC00261913-01
(y)-vesamicol hydrochloride
(+/-)-vesamicol (hydrochloride)
(+/-)-vesamicol.hcl (ah-5183)
J-004345
SR-01000075352-1
sr-01000075352
DTXSID40923401
FT-0772286
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, hydrochloride
(+/-)-vesamicol middot hcl (ah-5183)
AS-0378
()-vesamicol (hydrochloride)
2-(4-phenylpiperidin-1-yl)cyclohexan-1-ol;hydrochloride
cyclohexanol,2-(4-phenyl-1-piperidinyl)-,hydrochloride
AKOS040754351
BRD-K14765469-003-02-3
(-)-vesamicol
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, trans(+-)-
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, 1r-trans-
(+-)vesamicol
NCGC00016080-01
lopac-v-100
BSPBIO_000800
PRESTWICK3_000920
BPBIO1_000880
AB00471079
ah-5183
CHEMBL20730 ,
(+/-)-vesamicol
(1r,2r)-2-(4-phenylpiperidin-1-yl)cyclohexan-1-ol
bdbm50018094
(1r,2r)-2-(4-phenyl-piperidin-1-yl)-cyclohexanol
2-(4-phenyl-piperidin-1-yl)-cyclohexanol(vesamicol)
trans-2-(4-phenylpiperidin-1-yl)cyclohexanol
3d416v0flm ,
115362-28-2
unii-i1a877466v
i1a877466v ,
112709-59-8
unii-3d416v0flm
vesamicol, (+/-)-
AKOS015969758
SCHEMBL4499985
trans-2-(4-phenylpiperidino)cyclohexanol
(1r,2r)-2-(4-phenylpiperidino)-1-cyclohexanol
(1r,2r,(-))-2.alpha.-(4-phenyl-1-piperidinyl)cyclohexan-1.beta.-ol
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, (1r-trans)-
j404.506h ,
l-(-)-vesamicol
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, (1r,2r)-
(r,r)-(-)-vesamicol
(-)-trans-2-(4-phenylpiperidino)cyclohexanol
vesamicol, (-)-
(1r,2r)-2-(4-phenyl-1-piperidinyl)cyclohexanol
CHEBI:92261
(1r,2r)-2-(4-phenyl-1-piperidyl)cyclohexanol
MRF-0000062
DTXSID20920872
rel-(1r,2r)-2-(4-phenyl-1-piperidinyl)cyclohexanol
l-(-)-vesamicolhydrochloride
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, trans-
ah5183
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, trans-(+/-)-
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-, (1r,2r)-rel-
BRD-A76904477-003-02-5
2-(4-phenyl-piperidin-1-yl)-cyclohexanol
MLS000554350 ,
vesamicol
smr000146667
KBIO1_000376
DIVK1C_000376
SPECTRUM_000292
BSPBIO_003302
OPREA1_695768
PRESTWICK2_000920
LOPAC0_001228
v-100 ,
IDI1_000376
KBIO2_000772
KBIO2_005908
KBIO3_002804
KBIO2_003340
KBIOSS_000772
PRESTWICK0_000920
SPECTRUM3_001861
NINDS_000376
PRESTWICK1_000920
SPBIO_002989
OPREA1_778558
cyclohexanol, 2-(4-phenyl-1-piperidinyl)-
2-(4-phenyl-1-piperidinyl)cyclohexanol
MLS001201728
NCGC00162371-01
NCGC00016080-03
CHEMBL20943 ,
AKOS000572998
2-(4-phenylpiperidin-1-yl)cyclohexan-1-ol
CHEBI:103974
bdbm50018078
2-(4-phenyl-piperidin-1-yl)-cyclohexanol([3h]-(-)vesamicol)
STK700544
2-(4-phenylpiperidin-1-yl)cyclohexanol
CCG-205302
HMS2232G09
NCGC00016080-02
22232-64-0
cyclohexanol,2-(4-phenyl-1-piperidinyl)-, hydrochloride (1:1)
gtpl4759
HMS3370J19
SCHEMBL571598
AKOS025245452
2-(4-phenylpiperidino) cyclohexanol
AG-205/04770017
(a+/-)-vesamicol hydrochloride
OPERA_ID_322
SBI-0051195.P003
FT-0773505
DTXSID701009898
Q7923143
BRD-A76904477-003-05-8
SDCCGSBI-0051195.P004

Research Excerpts

Overview

Vesamicol (AH5183) is an inhibitor (IC50, 50 nM) of acetylcholine (ACh) vesicle packaging. Vesamicol is a leading compound for positron emission tomography (PET) and single photon emission computed tomographer (SPECT) tracers for mapping the vesicular acetyl choline transporter (VAChT)

ExcerptReferenceRelevance
"Vesamicol is a leading compound for positron emission tomography (PET) and single photon emission computed tomography (SPECT) tracers for mapping the vesicular acetylcholine transporter (VAChT). "( Evaluation of (+)-p-[11C]methylvesamicol for mapping sigma1 receptors: a comparison with [11C]SA4503.
Ishiwata, K; Kawamura, K; Mori, H; Shiba, K; Yajima, K, 2006
)
2.06
"Vesamicol (AH5183) is an inhibitor (IC50, 50 nM) of acetylcholine (ACh) vesicle packaging. "( Vesamicol, an inhibitor of acetylcholine vesicle packaging, increases synaptophysin phosphorylation in rat cortical synaptosomes.
Asermely, KE; O'Neill, JJ, 1996
)
3.18
"Vesamicol is a highly potent inhibitor of active acetylcholine transport into isolated cholinergic vesicles from Torpedo. "( Effect of N,N'-dicyclohexylcarbodiimide on the binding of vesamicol, an inhibitor of acetylcholine transport into synaptic vesicles.
Diebler, MF, 1992
)
1.97
"7. Vesamicol is an inhibitor of active ACh uptake into isolated synaptic vesicles."( Increasing quantal size at the mouse neuromuscular junction and the role of choline.
Van der Kloot, W; Yu, SP, 1991
)
0.8

Actions

Vesamicol is known to inhibit the transport of acetylcholine (ACh) into synaptic vesicles in vitro, but much less is known about its effects in the brain in vivo. Vesamicol, in lower concentration (20 microM) when neither of the above parameters was changed, completely prevented veratridine-evoked increase of [14C]acetyl choline release.

ExcerptReferenceRelevance
"Vesamicol is known to inhibit the transport of acetylcholine (ACh) into synaptic vesicles in vitro, but much less is known about its effects in the brain in vivo. "( Effects of systemic administration of 2-(4-phenyl-piperidino)-cyclohexanol (vesamicol) and an organophosphate DDVP on the cholinergic system in brain regions of rats.
Kobayashi, H; Saitoh, S; Suzuki, T; Takeno, K; Watanabe, T; Yasufuku, T, 1997
)
1.97
"Vesamicol, in lower concentration (20 microM) when neither of the above parameters was changed, completely prevented veratridine-evoked increase of [14C]acetylcholine release."( Parameters not influenced by vesamicol: membrane potential, calcium uptake, and internal calcium concentration of synaptosomes.
Adam-Vizi, V; Deri, Z, 1992
)
1.3

Treatment

At vesamicol-treated endplates, miniature endplate current (MEPC) frequency increased initially from 0.4 to >300 s-1 in 35 KP. The effect on nAChRs was independent from the activity of methamidophos as a cholinesterase inhibitor.

ExcerptReferenceRelevance
"At vesamicol-treated endplates, miniature endplate current (MEPC) frequency increased initially from 0.4 to >300 s-1 in 35 KP but then declined to <1 s-1 by 90 min."( Empty synaptic vesicles recycle and undergo exocytosis at vesamicol-treated motor nerve terminals.
Calupca, MA; Merriam, LA; Parsons, RL; Prior, C, 1999
)
1.06
"Pre-treatment with vesamicol did not prevent the reduction of nicotine-induced currents, indicating that the effect on nAChRs was independent from the activity of methamidophos as a cholinesterase inhibitor."( Methamidophos transiently inhibits neuronal nicotinic receptors of rat substantia nigra dopaminergic neurons via open channel block.
Bernardi, G; Di Angelantonio, S; Mercuri, NB, 2004
)
0.64
"Pretreatment with vesamicol blocked the cerebral uptake, indicating a specific interaction with the vesamicol binding site."( 18F-labelled vesamicol derivatives: syntheses and preliminary in vivo small animal positron emission tomography evaluation.
Eriksson, L; Ingvar, M; Parsons, SM; Rogers, GA; Stone-Elander, S; Widén, L, 1994
)
0.98

Dosage Studied

ExcerptRelevanceReference
" In experiment 1, a dose-response curve was performed."( Vesamicol, an acetylcholine uptake blocker in presynaptic vesicles, suppresses rapid eye movement (REM) sleep in the rat.
Jimenez-Anguiano, A; Salin-Pascual, RJ, 1995
)
1.73
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperidines
piperidines
[compound class information is derived from 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]

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency14.12540.003245.467312,589.2998AID1705
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00280.540617.639296.1227AID2364; AID2528
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency0.07080.050127.073689.1251AID588590
survival motor neuron protein isoform dHomo sapiens (human)Potency14.12540.125912.234435.4813AID1458
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.50120.00207.533739.8107AID891
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency14.12540.00106.000935.4813AID943
Chain A, Beta-lactamaseEscherichia coli K-12Potency89.12510.044717.8581100.0000AID485294
thioredoxin reductaseRattus norvegicus (Norway rat)Potency3.04880.100020.879379.4328AID588453; AID588456
GLS proteinHomo sapiens (human)Potency0.63100.35487.935539.8107AID624146
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.75190.035520.977089.1251AID504332
gemininHomo sapiens (human)Potency0.05800.004611.374133.4983AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency35.48130.125912.234435.4813AID1458
TAR DNA-binding protein 43Homo sapiens (human)Potency31.62281.778316.208135.4813AID652104
[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)
Cytochrome P450 2D6Homo sapiens (human)Ki0.00440.00011.19868.0000AID615930
Delta-type opioid receptorMus musculus (house mouse)Ki0.00200.00000.53939.4000AID476627
Vesicular acetylcholine transporterTetronarce californica (Pacific electric ray)IC50 (µMol)0.03400.03401.12202.6200AID30530
Vesicular acetylcholine transporterTetronarce californica (Pacific electric ray)Ki0.00150.00010.00060.0020AID216228; AID476627
Vesicular acetylcholine transporterHomo sapiens (human)IC50 (µMol)0.02000.01200.76803.0000AID30531
Vesicular acetylcholine transporterHomo sapiens (human)Ki0.00680.00010.00460.0152AID1237778; AID216232; AID216233; AID346599; AID615930; AID671079
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.07380.00000.338510.0000AID671080
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki0.04680.00130.56224.5230AID1233648; AID649865
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.02600.00000.490110.0000AID204794
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.02040.00030.26715.0700AID1233650
Vesicular acetylcholine transporterTetronarce californica (Pacific electric ray)IC50 (µMol)0.03400.03401.12202.6200AID216226
Vesicular acetylcholine transporterHomo sapiens (human)IC50 (µMol)1.52000.01200.76803.0000AID30531
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki0.03850.00130.56224.5230AID1506088; AID674894; AID674902
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.02210.00030.26715.0700AID674895
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
neurotransmitter transportVesicular acetylcholine transporterHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionVesicular acetylcholine transporterHomo sapiens (human)
serotonin uptakeVesicular acetylcholine transporterHomo sapiens (human)
acetylcholine uptakeVesicular acetylcholine transporterHomo sapiens (human)
positive regulation of long-term synaptic potentiationVesicular acetylcholine transporterHomo sapiens (human)
proton transmembrane transportVesicular acetylcholine transporterHomo sapiens (human)
positive regulation of neuromuscular junction developmentVesicular acetylcholine transporterHomo sapiens (human)
chemical synaptic transmissionVesicular acetylcholine transporterHomo 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)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
neurotransmitter transportVesicular acetylcholine transporterHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionVesicular acetylcholine transporterHomo sapiens (human)
serotonin uptakeVesicular acetylcholine transporterHomo sapiens (human)
acetylcholine uptakeVesicular acetylcholine transporterHomo sapiens (human)
positive regulation of long-term synaptic potentiationVesicular acetylcholine transporterHomo sapiens (human)
proton transmembrane transportVesicular acetylcholine transporterHomo sapiens (human)
positive regulation of neuromuscular junction developmentVesicular acetylcholine transporterHomo sapiens (human)
chemical synaptic transmissionVesicular acetylcholine transporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
acetylcholine transmembrane transporter activityVesicular acetylcholine transporterHomo sapiens (human)
acetylcholine:proton antiporter activityVesicular acetylcholine transporterHomo sapiens (human)
protein bindingVesicular acetylcholine transporterHomo sapiens (human)
monoamine:proton antiporter activityVesicular acetylcholine transporterHomo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
acetylcholine transmembrane transporter activityVesicular acetylcholine transporterHomo sapiens (human)
acetylcholine:proton antiporter activityVesicular acetylcholine transporterHomo sapiens (human)
protein bindingVesicular acetylcholine transporterHomo sapiens (human)
monoamine:proton antiporter activityVesicular acetylcholine transporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
plasma membraneVesicular acetylcholine transporterHomo sapiens (human)
clathrin-coated endocytic vesicle membraneVesicular acetylcholine transporterHomo sapiens (human)
synaptic vesicle membraneVesicular acetylcholine transporterHomo sapiens (human)
clathrin-sculpted acetylcholine transport vesicle membraneVesicular acetylcholine transporterHomo sapiens (human)
AP-1 adaptor complexVesicular acetylcholine transporterHomo sapiens (human)
AP-2 adaptor complexVesicular acetylcholine transporterHomo sapiens (human)
terminal boutonVesicular acetylcholine transporterHomo 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)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
plasma membraneVesicular acetylcholine transporterHomo sapiens (human)
clathrin-coated endocytic vesicle membraneVesicular acetylcholine transporterHomo sapiens (human)
synaptic vesicle membraneVesicular acetylcholine transporterHomo sapiens (human)
clathrin-sculpted acetylcholine transport vesicle membraneVesicular acetylcholine transporterHomo sapiens (human)
AP-1 adaptor complexVesicular acetylcholine transporterHomo sapiens (human)
AP-2 adaptor complexVesicular acetylcholine transporterHomo sapiens (human)
terminal boutonVesicular acetylcholine transporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (103)

Assay IDTitleYearJournalArticle
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1237782Selectivity ratio of Ki for human VAChT to Ki for sigma2 receptor in rat liver membrane homogenates2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
AID1233652Selectivity index, ratio of Ki for sigma1 receptor in Sprague-Dawley rat cortical membranes to Ki for rat VAChT expressed in PC12 cell membranes2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID671079Displacement of [3H]vesamicol from human VAChT expressed in rat PC12 cells after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
AID649865Displacement of (-)-[3H]vesamicol from rat VAchT transfected in rat PC12 cells after 2 hrs by scintillation counting2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Pyrrolovesamicols--synthesis, structure and VAChT binding of two 4-fluorobenzoyl regioisomers.
AID1237779Displacement of (+)-[3H]pentazocine from sigma1 receptor in guinea pig brain membrane homogenates2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
AID476631Selectivity ratio of for sigma 2 receptor in rat liver membrane homogenates to Ki for VAChT in Torpedo californica cholinergic synaptic vesicles2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
AID30531Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).
AID476628Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane homogenates after 90 mins by liquid scintillation counting2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
AID671081Displacement of [3H]DTG from sigma2 receptor in rat liver homogenate after 120 mins by liquid scintillation counting in presence of (+)-pentazocine2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
AID346818Selectivity ratio of Ki for human vesicular acetylcholine transporter to Ki for sigma2 receptor in rat liver membrane2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
AID117216Lethal dose of the compound, when administered intraperitoneally in mice1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).
AID1233647Displacement of (-)-[3H]vesamicol from VAChT in Sprague-Dawley rat brain membranes incubated for 2 hrs by liquid scintillation counting based competitive radioligand binding assay2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID216233Displacement of [3H]vesamicol from Vesicular Acetylcholine Transporter (VAChT)1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
AID346600Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane by liquid scintillation counting2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
AID671083Selectivity ratio of Ki for sigma2 receptor in rat liver homogenate to Ki for human VACht2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
AID1233651Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membranes incubated for 2 hrs in presence of dextrallorphan by liquid scintillation counting based competitive radioligand binding assay2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID1233646Binding affinity to VAChT Torpedo californica electric organ synaptic vesicles2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID1237781Selectivity ratio of Ki for human VAChT to Ki for sigma1 receptor in guinea pig brain membrane homogenates2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
AID1237780Displacement of [3H]DTG from sigma2 receptor in rat liver membrane homogenates2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
AID204941Sigma 2 binding assay was done rat liver membrane, by labeling the binding site with [3H]DTG (DuPont-NEN) in the presence of [3H](+)-pentazocine (100 nM)1997Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.
AID346601Displacement of [3H]DTG from sigma2 receptor in rat liver membrane2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
AID615929Displacement of [3H]-DTG from sigma 2 receptor in rat liver membrane homogenates after 2 hrs by liquid scintillation counting2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors.
AID204794Sigma-1 binding assay was done in guinea pig membranes by labeling the binding site with [3H](+)-pentazocine1997Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.
AID615933Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membrane homogenates to Ki for human VAChT2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors.
AID216228In vitro binding affinity to vesamicol receptor using [3H]vesamicol.1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
Spirovesamicols: conformationally restricted analogs of 2-(4-phenylpiperidino)cyclohexanol (vesamicol, AH5183) as potential modulators of presynaptic cholinergic function.
AID476627Displacement of [3H]vesamicol from VAChT in Torpedo californica cholinergic synaptic vesicles2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
AID615930Displacement of (-)-[3H]vesamicol from human VAChT expressed in rat PC12 A123.7 cells after 20 hrs2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors.
AID615932Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membrane homogenates to Ki for sigma 2 receptor in rat liver membrane homogenates2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors.
AID346599Displacement of [3H]vesamicol from human vesicular acetylcholine transporter expressed in rat PC12 cells by liquid scintillation spectrometry2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
AID331149Displacement of [3H]vesamicol from VAChT receptor in torpedo electrical organ synaptic vesicle2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
First CoMFA characterization of vesamicol analogs as ligands for the vesicular acetylcholine transporter.
AID216232Binding to vesicular acetylcholine transporter of torpedo synaptic vesicles1997Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.
AID30530Inhibition of [3H]- vesamicol binding to synaptic vesicles preparation from the electric organ of Torpedo californica1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Nonsymmetrical bipiperidyls as inhibitors of vesicular acetylcholine storage.
AID671080Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig membrane after 90 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
AID204305Binding affinity against Sigma opioid receptor type 2 in rat liver membranes using [3H]DTG (DuPont-NEN) as radioligand in the presence of (+)-pentazocine (100 nM)1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
AID1233653Selectivity index, ratio of Ki for sigma2 receptor in Sprague-Dawley rat liver membranes to Ki for rat VAChT expressed in PC12 cell membranes2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID615928Displacement of (+)-[3H]pentazocine from sigma 1 receptor in guinea pig brain membrane homogenates after 90 mins by liquid scintillation counting2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors.
AID476629Displacement of [3H]DTG from sigma 2 receptor in rat liver membrane homogenates after 2 hrs by liquid scintillation counting2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
AID1233650Displacement of (-)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cortical membranes incubated for 2 hrs by liquid scintillation counting based competitive radioligand binding assay2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID1237778Displacement of [3H]-vesamicol from human VAChT after 24 hrs by by liquid scintillation spectrometry analysis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
AID671082Selectivity ratio of Ki for sigma1 receptor in guinea pig membrane to Ki for human VACht2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
AID346817Selectivity ratio of Ki for human vesicular acetylcholine transporter to Ki for sigma1 receptor in guinea pig brain membrane2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
AID476630Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membrane homogenates to Ki for VAChT in Torpedo californica cholinergic synaptic vesicles2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
AID204161Binding affinity against Sigma opioid receptor type 1 in guinea pig brain membranes using [3H](+)-pentazocine as radioligand1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
AID1233648Displacement of (-)-[3H]vesamicol from rat VAChT expressed in PC12 cell membranes incubated for 2 hrs by liquid scintillation counting based competitive radioligand binding assay2015European journal of medicinal chemistry, Jul-15, Volume: 100New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID216226Displacement of [3H]vesamicol from Vesamicol receptor of Torpedo californica1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Acyclic analogues of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport.
AID1506086Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain 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.
AID674895Displacement of (+)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cerebral membrane after 90 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
AID117216Lethal dose of the compound, when administered intraperitoneally in mice1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).
AID30531Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).
AID674894Displacement of (-)-[3H]vesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 60 mins by liquid scintillation counting in presence of DTG2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
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.
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.
AID674902Displacement of [125I]O-iodo-trans-decalinvesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 1 hr by gamma counting2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
AID674896Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membrane after 90 mins by liquid scintillation counting in presence of pentazocine2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
AID409949Inhibition of human liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID409951Inhibition of human liver MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
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.
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.
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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (258)

TimeframeStudies, This Drug (%)All Drugs %
pre-199041 (15.89)18.7374
1990's115 (44.57)18.2507
2000's58 (22.48)29.6817
2010's39 (15.12)24.3611
2020's5 (1.94)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 43.69

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

MetricThis Compound (vs All)
Research Demand Index43.69 (24.57)
Research Supply Index5.52 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index69.20 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (43.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Reviews0 (0.00%)6.00%
Reviews5 (2.02%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Case Studies1 (0.40%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
Other14 (100.00%)84.16%
Other242 (97.58%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]