Compounds > cilansetron

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 Source	ID
PubMed CID	6918107
CHEMBL ID	2103778
SCHEMBL ID	15950
MeSH ID	M0224401

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)

Excerpt	Reference	Relevance
"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

Excerpt	Relevance	Reference
" 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

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
Integrin beta-3	Homo sapiens (human)	Ki	10.0000	0.0010	0.9845	9.1400	AID221935
Muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Ki	0.9100	0.0001	0.5797	10.0000	AID104027
Muscarinic acetylcholine receptor M3	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	1.4833	9.1400	AID225226
Integrin alpha-IIb	Homo sapiens (human)	Ki	10.0000	0.0020	2.3352	9.1400	AID221935
5-hydroxytryptamine receptor 2C	Rattus norvegicus (Norway rat)	Ki	7.5667	0.0002	0.6677	10.0000	AID4767; AID5304; AID6424
Beta-2 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0005	0.3546	1.6000	AID218722
Muscarinic acetylcholine receptor M2	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.5890	8.2600	AID101705
5-hydroxytryptamine receptor 2A	Rattus norvegicus (Norway rat)	Ki	8.9000	0.0001	0.6017	10.0000	AID5304; AID6424
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
Alpha-1B adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.9490	10.0000	AID218722
Beta-1 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.6673	10.0000	AID218722
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.5614	10.0000	AID40505; AID72139
D	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.6100	10.0000	AID218722; AID61649
D(3) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.2567	5.8000	AID218722; AID65752
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.7396	10.0000	AID4352; AID6424
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6352	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6217	10.0000	AID40505; AID72139
Voltage-dependent L-type calcium channel subunit alpha-1C	Rattus norvegicus (Norway rat)	Ki	7.7000	0.0008	0.5796	5.4000	AID47563; AID47564
Alpha-2A adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.9375	10.0000	AID219805
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6758	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6469	10.0000	AID40505; AID72139
Alpha-1D adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.5751	10.0000	AID218722
D(1B) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.2462	2.0000	AID218722
Beta-3 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0005	0.3367	1.6000	AID218722
Voltage-dependent L-type calcium channel subunit alpha-1D	Rattus norvegicus (Norway rat)	Ki	8.4667	0.0008	0.7410	5.4000	AID47563; AID47564
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
5-hydroxytryptamine receptor 1B	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0003	1.2967	9.2440	AID4703; AID6424
5-hydroxytryptamine receptor 1D	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0010	1.6747	9.2000	AID4876; AID6424
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6712	10.0000	AID40505; AID72139
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.2789	2.8900	AID50508
Gastrin/cholecystokinin type B receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0006	0.1196	0.6800	AID51469
D(4) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.1887	2.0000	AID218722
5-hydroxytryptamine receptor 1F	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0010	1.6747	9.2000	AID6424
5-hydroxytryptamine receptor 2B	Rattus norvegicus (Norway rat)	Ki	8.9000	0.0002	0.5909	10.0000	AID5304; AID6424
5-hydroxytryptamine receptor 6	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.4254	2.1000	AID6424
Histamine H1 receptor	Rattus norvegicus (Norway rat)	Ki	6.5000	0.0007	1.5440	6.5000	AID87533
5-hydroxytryptamine receptor 7	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.1480	3.1800	AID6424
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.6068	9.2330	AID220521
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	8.5000	0.0000	0.3845	8.6000	AID224719
Kappa-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.1868	3.9500	AID223592
5-hydroxytryptamine receptor 5A	Rattus norvegicus (Norway rat)	Ki	10.0000	0.3010	1.3003	2.1000	AID6424
5-hydroxytryptamine receptor 5B	Rattus norvegicus (Norway rat)	Ki	10.0000	0.3010	1.3003	2.1000	AID228446; AID6424
5-hydroxytryptamine receptor 3A	Rattus norvegicus (Norway rat)	Ki	5.0001	0.0002	0.4841	10.0000	AID5908; AID6424
Alpha-1A adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.9650	10.0000	AID218722
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.4375	10.0000	AID218722; AID6424; AID65903
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.5577	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6403	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.5708	10.0000	AID40505; AID72139
Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0003	0.8196	6.6900	AID143098
Thyrotropin-releasing hormone receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0200	0.0312	0.0423	AID210172
Voltage-dependent L-type calcium channel subunit alpha-1S	Rattus norvegicus (Norway rat)	Ki	7.7000	0.0008	0.6673	5.4000	AID47563; AID47564
5-hydroxytryptamine receptor 4	Rattus norvegicus (Norway rat)	Ki	5.4800	0.0016	1.0253	5.0119	AID3202; AID6424
GABA theta subunit	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0002	0.6561	10.0000	AID40505; AID72139
5-hydroxytryptamine receptor 3B	Rattus norvegicus (Norway rat)	Ki	5.0001	0.0002	0.5023	10.0000	AID5908; AID6424
Histamine H3 receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.2963	8.5110	AID89720
Sigma non-opioid intracellular receptor 1	Rattus norvegicus (Norway rat)	Ki	0.3400	0.0003	0.2671	5.0700	AID229206
Nischarin	Homo sapiens (human)	Ki	10.0000	0.0042	0.2192	3.8019	AID91719
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Process	via Protein(s)	Taxonomy
negative regulation of low-density lipoprotein receptor activity	Integrin beta-3	Homo sapiens (human)
positive regulation of protein phosphorylation	Integrin beta-3	Homo sapiens (human)
positive regulation of endothelial cell proliferation	Integrin beta-3	Homo sapiens (human)
positive regulation of cell-matrix adhesion	Integrin beta-3	Homo sapiens (human)
cell-substrate junction assembly	Integrin beta-3	Homo sapiens (human)
cell adhesion	Integrin beta-3	Homo sapiens (human)
cell-matrix adhesion	Integrin beta-3	Homo sapiens (human)
integrin-mediated signaling pathway	Integrin beta-3	Homo sapiens (human)
embryo implantation	Integrin beta-3	Homo sapiens (human)
blood coagulation	Integrin beta-3	Homo sapiens (human)
positive regulation of endothelial cell migration	Integrin beta-3	Homo sapiens (human)
positive regulation of gene expression	Integrin beta-3	Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiation	Integrin beta-3	Homo sapiens (human)
positive regulation of fibroblast migration	Integrin beta-3	Homo sapiens (human)
negative regulation of lipid storage	Integrin beta-3	Homo sapiens (human)
response to activity	Integrin beta-3	Homo sapiens (human)
smooth muscle cell migration	Integrin beta-3	Homo sapiens (human)
positive regulation of smooth muscle cell migration	Integrin beta-3	Homo sapiens (human)
platelet activation	Integrin beta-3	Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathway	Integrin beta-3	Homo sapiens (human)
cell-substrate adhesion	Integrin beta-3	Homo sapiens (human)
activation of protein kinase activity	Integrin beta-3	Homo sapiens (human)
negative regulation of lipid transport	Integrin beta-3	Homo sapiens (human)
regulation of protein localization	Integrin beta-3	Homo sapiens (human)
regulation of actin cytoskeleton organization	Integrin beta-3	Homo sapiens (human)
cell adhesion mediated by integrin	Integrin beta-3	Homo sapiens (human)
positive regulation of cell adhesion mediated by integrin	Integrin beta-3	Homo sapiens (human)
positive regulation of osteoblast proliferation	Integrin beta-3	Homo sapiens (human)
heterotypic cell-cell adhesion	Integrin beta-3	Homo sapiens (human)
substrate adhesion-dependent cell spreading	Integrin beta-3	Homo sapiens (human)
tube development	Integrin beta-3	Homo sapiens (human)
wound healing, spreading of epidermal cells	Integrin beta-3	Homo sapiens (human)
cellular response to platelet-derived growth factor stimulus	Integrin beta-3	Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathway	Integrin beta-3	Homo sapiens (human)
wound healing	Integrin beta-3	Homo sapiens (human)
apoptotic cell clearance	Integrin beta-3	Homo sapiens (human)
regulation of bone resorption	Integrin beta-3	Homo sapiens (human)
positive regulation of angiogenesis	Integrin beta-3	Homo sapiens (human)
positive regulation of bone resorption	Integrin beta-3	Homo sapiens (human)
symbiont entry into host cell	Integrin beta-3	Homo sapiens (human)
platelet-derived growth factor receptor signaling pathway	Integrin beta-3	Homo sapiens (human)
positive regulation of fibroblast proliferation	Integrin beta-3	Homo sapiens (human)
mesodermal cell differentiation	Integrin beta-3	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Integrin beta-3	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Integrin beta-3	Homo sapiens (human)
negative regulation of lipoprotein metabolic process	Integrin beta-3	Homo sapiens (human)
negative chemotaxis	Integrin beta-3	Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosol	Integrin beta-3	Homo sapiens (human)
regulation of serotonin uptake	Integrin beta-3	Homo sapiens (human)
angiogenesis involved in wound healing	Integrin beta-3	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Integrin beta-3	Homo sapiens (human)
platelet aggregation	Integrin beta-3	Homo sapiens (human)
cellular response to mechanical stimulus	Integrin beta-3	Homo sapiens (human)
cellular response to xenobiotic stimulus	Integrin beta-3	Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferation	Integrin beta-3	Homo sapiens (human)
blood coagulation, fibrin clot formation	Integrin beta-3	Homo sapiens (human)
maintenance of postsynaptic specialization structure	Integrin beta-3	Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalization	Integrin beta-3	Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trapping	Integrin beta-3	Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreading	Integrin beta-3	Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathway	Integrin beta-3	Homo sapiens (human)
regulation of trophoblast cell migration	Integrin beta-3	Homo sapiens (human)
regulation of extracellular matrix organization	Integrin beta-3	Homo sapiens (human)
cellular response to insulin-like growth factor stimulus	Integrin beta-3	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	Integrin beta-3	Homo sapiens (human)
positive regulation of T cell migration	Integrin beta-3	Homo sapiens (human)
cell migration	Integrin beta-3	Homo sapiens (human)
positive regulation of leukocyte migration	Integrin alpha-IIb	Homo sapiens (human)
cell-matrix adhesion	Integrin alpha-IIb	Homo sapiens (human)
integrin-mediated signaling pathway	Integrin alpha-IIb	Homo sapiens (human)
angiogenesis	Integrin alpha-IIb	Homo sapiens (human)
cell-cell adhesion	Integrin alpha-IIb	Homo sapiens (human)
cell adhesion mediated by integrin	Integrin alpha-IIb	Homo sapiens (human)
apoptotic process	Nischarin	Homo sapiens (human)
Rac protein signal transduction	Nischarin	Homo sapiens (human)
actin cytoskeleton organization	Nischarin	Homo sapiens (human)
negative regulation of cell migration	Nischarin	Homo sapiens (human)
outer dynein arm assembly	Nischarin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

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

Ceullar Components (39)

Process	via Protein(s)	Taxonomy
glutamatergic synapse	Integrin beta-3	Homo sapiens (human)
nucleus	Integrin beta-3	Homo sapiens (human)
nucleoplasm	Integrin beta-3	Homo sapiens (human)
plasma membrane	Integrin beta-3	Homo sapiens (human)
cell-cell junction	Integrin beta-3	Homo sapiens (human)
focal adhesion	Integrin beta-3	Homo sapiens (human)
external side of plasma membrane	Integrin beta-3	Homo sapiens (human)
cell surface	Integrin beta-3	Homo sapiens (human)
apical plasma membrane	Integrin beta-3	Homo sapiens (human)
platelet alpha granule membrane	Integrin beta-3	Homo sapiens (human)
lamellipodium membrane	Integrin beta-3	Homo sapiens (human)
filopodium membrane	Integrin beta-3	Homo sapiens (human)
microvillus membrane	Integrin beta-3	Homo sapiens (human)
ruffle membrane	Integrin beta-3	Homo sapiens (human)
integrin alphav-beta3 complex	Integrin beta-3	Homo sapiens (human)
melanosome	Integrin beta-3	Homo sapiens (human)
synapse	Integrin beta-3	Homo sapiens (human)
postsynaptic membrane	Integrin beta-3	Homo sapiens (human)
extracellular exosome	Integrin beta-3	Homo sapiens (human)
integrin alphaIIb-beta3 complex	Integrin beta-3	Homo sapiens (human)
glycinergic synapse	Integrin beta-3	Homo sapiens (human)
integrin complex	Integrin beta-3	Homo sapiens (human)
protein-containing complex	Integrin beta-3	Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complex	Integrin beta-3	Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complex	Integrin beta-3	Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complex	Integrin beta-3	Homo sapiens (human)
receptor complex	Integrin beta-3	Homo sapiens (human)
alphav-beta3 integrin-vitronectin complex	Integrin beta-3	Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complex	Integrin beta-3	Homo sapiens (human)
focal adhesion	Integrin beta-3	Homo sapiens (human)
cell surface	Integrin beta-3	Homo sapiens (human)
synapse	Integrin beta-3	Homo sapiens (human)
plasma membrane	Integrin alpha-IIb	Homo sapiens (human)
focal adhesion	Integrin alpha-IIb	Homo sapiens (human)
cell surface	Integrin alpha-IIb	Homo sapiens (human)
platelet alpha granule membrane	Integrin alpha-IIb	Homo sapiens (human)
extracellular exosome	Integrin alpha-IIb	Homo sapiens (human)
integrin alphaIIb-beta3 complex	Integrin alpha-IIb	Homo sapiens (human)
blood microparticle	Integrin alpha-IIb	Homo sapiens (human)
integrin complex	Integrin alpha-IIb	Homo sapiens (human)
external side of plasma membrane	Integrin alpha-IIb	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)
plasma membrane	Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)
plasma membrane	Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
nucleoplasm	Nischarin	Homo sapiens (human)
early endosome	Nischarin	Homo sapiens (human)
cytosol	Nischarin	Homo sapiens (human)
plasma membrane	Nischarin	Homo sapiens (human)
microtubule cytoskeleton	Nischarin	Homo sapiens (human)
membrane	Nischarin	Homo sapiens (human)
intracellular membrane-bounded organelle	Nischarin	Homo sapiens (human)
intercellular bridge	Nischarin	Homo sapiens (human)
recycling endosome	Nischarin	Homo sapiens (human)
cytoplasm	Nischarin	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay ID	Title	Year	Journal	Article
AID4876	The binding affinity was measured on 5-hydroxytryptamine 1D receptor using [3H]- serotonin as radioligand.	1993	Journal 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.
AID4767	The binding affinity was measured on 5-hydroxytryptamine 1C receptor using [3H]- serotonin as radioligand.	1993	Journal 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.
AID221935	The binding affinity was measured on glycine receptor using [3H]- strychnine as radioligand.	1993	Journal 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.
AID219805	The binding affinity was measured on alpha-2-adrenergic receptor using [3H]- clonidine as radioligand.	1993	Journal 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.
AID50508	The binding affinity was measured on cholecystokinin type A receptor using [3H]- CCK-8 as radioligand.	1993	Journal 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.
AID61649	The binding affinity was measured on dopamine receptor D1 using [3H]- dopamine as radioligand.	1993	Journal 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.
AID221936	The binding affinity was measured on glycine strych. ins receptor using [3H]- 5,7-diClkyn.acid as radioligand.	1993	Journal 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.
AID146872	The binding affinity was measured on Na+2(BTX)brain receptor using [3H]- batrachotox as radioligand.	1993	Journal 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.
AID6424	The binding affinity was measured on 5-hydroxytryptamine receptor uptake receptor using [3H]- paroxetine as radioligand.	1993	Journal 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.
AID5304	The binding affinity was measured on 5-hydroxytryptamine 2 receptor using [3H]- spiperone as radioligand.	1993	Journal 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.
AID47563	Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of rat brain	1993	Journal 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.
AID143098	The binding affinity was measured on NMDA receptor using [3H]- CGS-19755 as radioligand.	1993	Journal 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.
AID197156	The 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.	1993	Journal 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.
AID3202	The binding affinity was measured on 5-hydroxytryptamine 4 receptor using [3H]- GR-113808 as radioligand.	1993	Journal 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.
AID222169	The binding affinity was measured on melatonin receptor using [3H]- 2-iodo-melat as radioligand.	1993	Journal 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.
AID51469	The binding affinity was measured on cholecystokinin type B receptor using [3H]- CCK-8 as radioligand.	1993	Journal 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.
AID210172	The binding affinity was measured on TRH receptor using [3H]- MeTRH as radioligand.	1993	Journal 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.
AID221171	The binding affinity was measured on leukotriene-D4 receptor using [3H]- LTD4 as radioligand.	1993	Journal 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.
AID5902	Displacement of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranes	1993	Journal 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.
AID225226	The binding affinity was measured on muscarine M3 receptor using [3H]- N-Me-SCOPOL as radioligand.	1993	Journal 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.
AID228446	The binding affinity was measured on tryptamine receptor using [3H]- tryptamine as radioligand.	1993	Journal 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.
AID87533	The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand.	1993	Journal 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.
AID221170	The binding affinity was measured on leukotriene-6 receptor using [3H]- IL-6 as radioligand.	1993	Journal 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.
AID104027	The binding affinity was measured on muscarine M1 receptor using [3H]- pirenzepine as radioligand.	1993	Journal 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.
AID218722	The binding affinity was measured on beta-1,2-adrenergic receptor using [3H]- DHA as radioligand.	1993	Journal 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.
AID152095	The binding affinity was measured on substance P as radioligand.	1993	Journal 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.
AID229206	The binding affinity was measured on sigma receptor using [3H]- (+)-3-PPP as radioligand.	1993	Journal 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.
AID173594	Dose of antagonist which inhibits the by the 2-Me-5-HT induced slowing of the heart rate by 10 beats/5 s.	1993	Journal 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.
AID5908	The binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand.	1993	Journal 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.
AID65752	The binding affinity was measured on dopamine receptor D3 using [3H]- dopamine as radioligand.	1993	Journal 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.
AID223592	The binding affinity was measured on kappa-opiate receptor using [3H]- EKC as radioligand.	1993	Journal 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.
AID224719	The binding affinity was measured on mu-opiate receptor using [3H]- naloxone as radioligand.	1993	Journal 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.
AID101705	The binding affinity was measured on muscarine M2 receptor using [3H]- N-Me-SCOPOL as radioligand.	1993	Journal 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.
AID65903	The binding affinity was measured on dopamine receptor D2 using [3H]- spiperone as radioligand.	1993	Journal 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.
AID72139	Displacement of [3H]DH-muscimol from rat GABA-A receptor	1993	Journal 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.
AID220521	The binding affinity was measured on delta-opiate receptor using [3H]- dadle as radioligand.	1993	Journal 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.
AID197155	The 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.	1993	Journal 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.
AID47564	Inhibition of [3H]D-888 binding to L-type calcium channel verapamil site of rat brain	1993	Journal 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.
AID4352	The binding affinity was measured on 5-hydroxytryptamine 1A receptor using [3H]- 8-OH-DPAT as radioligand.	1993	Journal 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.
AID91719	The binding affinity was measured on imidazoline I2 receptor using [3H]- indazoxan as radioligand.	1993	Journal 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.
AID184810	Lowest effective dose affecting behavioral parameter in at least half of the animals.	1993	Journal 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.
AID40505	Displacement of [3H]- Diazepam from rat GABA-A benzodiazepine receptor	1993	Journal 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.
AID4703	The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.	1993	Journal 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.
AID89720	The binding affinity was measured on histamine H3 receptor using [3H]- N-Me-histam as radioligand.	1993	Journal 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)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	3 (16.67)	18.2507
2000's	15 (83.33)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (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.

Metric	This Compound (vs All)
Research Demand Index	26.31 (24.57)
Research Supply Index	3.00 (2.92)
Research Growth Index	4.63 (4.65)
Search Engine Demand Index	29.35 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (26.31)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (5.56%)	5.53%
Reviews	9 (50.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	8 (44.44%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
glycerol Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.	1.99	1	alditol; triol	algal metabolite; detergent; Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; solvent
alosetron alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.	10.73	8	imidazoles; pyridoindole	antiemetic; gastrointestinal drug; serotonergic antagonist
clonidine Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.	2.05	1	clonidine; imidazoline
granisetron [no description available]	1.98	1	aromatic amide; indazoles
loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.	2.73	3	monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol	anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist
mebeverine mebeverine: RN given refers to parent cpd; structure	3.14	1	methoxybenzoic acid
ondansetron Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.	2.39	2	carbazoles
ng-nitroarginine methyl ester NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.	2.05	1	alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor
ramosetron [no description available]	2.73	3	indoles
gr 65630 GR 65630: serotonin receptor ligand. GR 65630 : A member of the class of methylindoles that is 1-methylindole substituted at position 3 by a 3-(4-methylimidazol-5-yl)propanoyl group.	1.98	1
piboserod Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.	2.05	1
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	3.11	1
prucalopride prucalopride: a 5-HT4 agonist enterokinetic compound	3.11	1	benzamides
tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source	9.34	3	carboxamidine; guanidines; hydrazines; indoles	gastrointestinal drug; serotonergic agonist

Condition	Relationship Strength	Studies	Trials
Colitis, Mucous [description not available]	6.08	9	0
Diarrhea An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.	9.89	4	0
Irritable Bowel Syndrome A disorder with chronic or recurrent colonic symptoms without a clearcut etiology. This condition is characterized by chronic or recurrent ABDOMINAL PAIN, bloating, MUCUS in FECES, and an erratic disturbance of DEFECATION.	6.08	9	0
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	2.41	2	0
Colonic Diseases, Functional Chronic or recurrent colonic disorders without an identifiable structural or biochemical explanation. The widely recognized IRRITABLE BOWEL SYNDROME falls into this category.	4.09	3	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.03	1	0
Colonic Inertia Symptom characterized by the passage of stool once a week or less.	2.96	1	0
Constipation Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections.	2.96	1	0
Colicky Pain [description not available]	1.98	1	0
Abdominal Pain Sensation of discomfort, distress, or agony in the abdominal region.	1.98	1	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	3.79	2	1

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