Page last updated: 2024-12-11

cilansetron

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Description

cilansetron: structure given in first source; binds to 5-HT(3) receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918107
CHEMBL ID2103778
SCHEMBL ID15950
MeSH IDM0224401

Synonyms (26)

Synonym
gtpl2297
kc-9946
cilansetron
D03495
120635-74-7
cilansetron (usan/inn)
(-)-(r)-5,6,9,10-tetrahydro-10-((2-methylimidazol-1-yl)methyl)-4h-pyrido(3,2,1-jk)carbazol-11(8h)-one
4h-pyrido(3,2,1-jk)carbazol-11(8h)-one, 5,6,9,10-tetrahydro-10-((2-methyl-1h-imidazol-1-yl)methyl)-, (r)-
cilansetron [usan:inn]
2j6dq1u5b5 ,
unii-2j6dq1u5b5
CHEMBL2103778
DB04885
SCHEMBL15950
cilansetron [usan]
cilansetron [inn]
4h-pyrido(3,2,1-jk)carbazol-11(8h)-one, 5,6,9,10-tetrahydro-10-((2-mrthyl-1h-inidazol-1-yl)methyl)-, (10r)-
cilansetron [mart.]
cilansetron [who-dd]
cilansetron [mi]
(10r)-5,6,9,10-tetrahydro-10((2-methylimidazol-1-yl)methyl)-4h-pyridol(3,2,1-jk)carbazol-11(8h)-one
DTXSID40152951
Q5119931
bdbm50231569
(12r)-12-[(2-methylimidazol-1-yl)methyl]-1-azatetracyclo[7.6.1.05,16.010,15]hexadeca-5(16),6,8,10(15)-tetraen-11-one
AKOS040748135

Research Excerpts

Overview

Cilansetron [KC 9946] is a serotonin-3 receptor (5-HT(3) antagonist under development with Solvay Pharmaceuticals. It is being evaluated for the treatment of female and male patients with irritable bowel syndrome with diarrhoea predominance (IBS-D)

ExcerptReferenceRelevance
"Cilansetron is a novel serotonin type-3 (5-hydroxytryptamine; 5-HT) receptor subtype 3 (5-HT(3)) receptor antagonist currently being evaluated for the treatment of female and male patients with irritable bowel syndrome with diarrhoea predominance (IBS-D). "( Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.
Cash, BD; Chey, WD, 2005
)
3.21
"Cilansetron [KC 9946] is a serotonin-3 receptor (5-HT(3)) antagonist under development with Solvay Pharmaceuticals for the treatment of irritable bowel syndrome with diarrhoea predominance (IBS-D), in both men and women.5-HT(3) antagonists inhibit the 5-HT(3) receptors, resulting in decreased GI motility, secretion and sensation, thereby improving symptoms of IBS-D. "( Cilansetron: KC 9946.
, 2005
)
3.21
"Cilansetron is a 5-HT3 antagonist tinder development by Solvay Pharmaceuticals as a potential treatment for irritable bowel syndrome (IBS). "( Cilansetron. Solvay.
Stacher, G, 2001
)
3.2

Dosage Studied

ExcerptRelevanceReference
" Dose-ranging studies showed no dose-response relationship."( Cilansetron in the treatment of diarrhea-predominant irritable bowel syndrome?
Stacher, G, 2007
)
1.78
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (64)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
Integrin beta-3Homo sapiens (human)Ki10.00000.00100.98459.1400AID221935
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.91000.00010.579710.0000AID104027
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki10.00000.00011.48339.1400AID225226
Integrin alpha-IIbHomo sapiens (human)Ki10.00000.00202.33529.1400AID221935
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki7.56670.00020.667710.0000AID4767; AID5304; AID6424
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00050.35461.6000AID218722
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki10.00000.00010.58908.2600AID101705
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki8.90000.00010.601710.0000AID5304; AID6424
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00010.949010.0000AID218722
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00000.667310.0000AID218722
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki10.00000.00020.561410.0000AID40505; AID72139
DRattus norvegicus (Norway rat)Ki10.00000.00010.610010.0000AID218722; AID61649
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki10.00000.00010.25675.8000AID218722; AID65752
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki10.00000.00010.739610.0000AID4352; AID6424
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki10.00000.00020.635210.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki10.00000.00020.621710.0000AID40505; AID72139
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)Ki7.70000.00080.57965.4000AID47563; AID47564
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00000.937510.0000AID219805
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki10.00000.00020.675810.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki10.00000.00020.646910.0000AID40505; AID72139
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00000.575110.0000AID218722
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki10.00000.00020.24622.0000AID218722
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00050.33671.6000AID218722
Voltage-dependent L-type calcium channel subunit alpha-1DRattus norvegicus (Norway rat)Ki8.46670.00080.74105.4000AID47563; AID47564
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki10.00000.00031.29679.2440AID4703; AID6424
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki10.00000.00101.67479.2000AID4876; AID6424
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki10.00000.00020.671210.0000AID40505; AID72139
Cholecystokinin receptor type ARattus norvegicus (Norway rat)Ki10.00000.00010.27892.8900AID50508
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)Ki10.00000.00060.11960.6800AID51469
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki10.00000.00020.18872.0000AID218722
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki10.00000.00101.67479.2000AID6424
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki8.90000.00020.590910.0000AID5304; AID6424
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki10.00000.00020.42542.1000AID6424
Histamine H1 receptorRattus norvegicus (Norway rat)Ki6.50000.00071.54406.5000AID87533
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki10.00000.00000.14803.1800AID6424
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki10.00000.00000.60689.2330AID220521
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki8.50000.00000.38458.6000AID224719
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki10.00000.00000.18683.9500AID223592
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Ki10.00000.30101.30032.1000AID6424
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Ki10.00000.30101.30032.1000AID228446; AID6424
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki5.00010.00020.484110.0000AID5908; AID6424
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki10.00000.00000.965010.0000AID218722
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki10.00000.00000.437510.0000AID218722; AID6424; AID65903
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki10.00000.00020.557710.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki10.00000.00020.640310.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki10.00000.00020.570810.0000AID40505; AID72139
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.00000.00030.81966.6900AID143098
Thyrotropin-releasing hormone receptorRattus norvegicus (Norway rat)Ki10.00000.02000.03120.0423AID210172
Voltage-dependent L-type calcium channel subunit alpha-1SRattus norvegicus (Norway rat)Ki7.70000.00080.66735.4000AID47563; AID47564
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki5.48000.00161.02535.0119AID3202; AID6424
GABA theta subunitRattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki10.00000.00020.656110.0000AID40505; AID72139
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki5.00010.00020.502310.0000AID5908; AID6424
Histamine H3 receptorRattus norvegicus (Norway rat)Ki10.00000.00010.29638.5110AID89720
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.34000.00030.26715.0700AID229206
NischarinHomo sapiens (human)Ki10.00000.00420.21923.8019AID91719
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID4876The binding affinity was measured on 5-hydroxytryptamine 1D receptor using [3H]- serotonin as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID4767The binding affinity was measured on 5-hydroxytryptamine 1C receptor using [3H]- serotonin as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID221935The binding affinity was measured on glycine receptor using [3H]- strychnine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID219805The binding affinity was measured on alpha-2-adrenergic receptor using [3H]- clonidine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID50508The binding affinity was measured on cholecystokinin type A receptor using [3H]- CCK-8 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID61649The binding affinity was measured on dopamine receptor D1 using [3H]- dopamine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID221936The binding affinity was measured on glycine strych. ins receptor using [3H]- 5,7-diClkyn.acid as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID146872The binding affinity was measured on Na+2(BTX)brain receptor using [3H]- batrachotox as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID6424The binding affinity was measured on 5-hydroxytryptamine receptor uptake receptor using [3H]- paroxetine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID5304The binding affinity was measured on 5-hydroxytryptamine 2 receptor using [3H]- spiperone as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID47563Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of rat brain1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID143098The binding affinity was measured on NMDA receptor using [3H]- CGS-19755 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID197156The pA2 is the negative logarithm of the molar concentration of an antagonist which necessitates the doubling of the agonist dose to couteract the effect of that antagonist and restore the original response was measured in rat isolated vagus nerve test.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID3202The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID222169The binding affinity was measured on melatonin receptor using [3H]- 2-iodo-melat as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID51469The binding affinity was measured on cholecystokinin type B receptor using [3H]- CCK-8 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID210172The binding affinity was measured on TRH receptor using [3H]- MeTRH as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID221171The binding affinity was measured on leukotriene-D4 receptor using [3H]- LTD4 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID5902Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID225226The binding affinity was measured on muscarine M3 receptor using [3H]- N-Me-SCOPOL as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID228446The binding affinity was measured on tryptamine receptor using [3H]- tryptamine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID87533The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID221170The binding affinity was measured on leukotriene-6 receptor using [3H]- IL-6 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID104027The binding affinity was measured on muscarine M1 receptor using [3H]- pirenzepine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID218722The binding affinity was measured on beta-1,2-adrenergic receptor using [3H]- DHA as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID152095The binding affinity was measured on substance P as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID229206The binding affinity was measured on sigma receptor using [3H]- (+)-3-PPP as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID173594Dose of antagonist which inhibits the by the 2-Me-5-HT induced slowing of the heart rate by 10 beats/5 s.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID5908The binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID65752The binding affinity was measured on dopamine receptor D3 using [3H]- dopamine as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID223592The binding affinity was measured on kappa-opiate receptor using [3H]- EKC as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID224719The binding affinity was measured on mu-opiate receptor using [3H]- naloxone as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID101705The binding affinity was measured on muscarine M2 receptor using [3H]- N-Me-SCOPOL as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID65903The binding affinity was measured on dopamine receptor D2 using [3H]- spiperone as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID72139Displacement of [3H]DH-muscimol from rat GABA-A receptor1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID220521The binding affinity was measured on delta-opiate receptor using [3H]- dadle as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID197155The pA2 is the negative logarithm of the molar concentration of an antagonist which necessitates the doubling of the agonist dose to couteract the effect of that antagonist and restore the original response was measured in guinea pig isolated ileu m test.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID47564Inhibition of [3H]D-888 binding to L-type calcium channel verapamil site of rat brain1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID4352The binding affinity was measured on 5-hydroxytryptamine 1A receptor using [3H]- 8-OH-DPAT as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID91719The binding affinity was measured on imidazoline I2 receptor using [3H]- indazoxan as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID184810Lowest effective dose affecting behavioral parameter in at least half of the animals.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID40505Displacement of [3H]- Diazepam from rat GABA-A benzodiazepine receptor1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID4703The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
AID89720The binding affinity was measured on histamine H3 receptor using [3H]- N-Me-histam as radioligand.1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (16.67)18.2507
2000's15 (83.33)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.31

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index26.31 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (5.56%)5.53%
Reviews9 (50.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (44.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]