Target Information

Target General Information

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Target ID

T84160 (Former ID: TTDS00106)

Target Name

5-HT 3 receptor (5HT3R)

Synonyms

5-hydroxytryptamine receptor type 3; 5-hydroxytryptamine receptor 3; 5-HT3R; 5-HT3 receptor; 5-HT-3

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Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 1 Target-related Diseases

Nausea/vomiting [ICD-11: MD90]

Function

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel.

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BioChemical Class

GPCR rhodopsin

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 4 Approved Drugs

Granisetron

Drug Info

Approved

Nausea and vomiting

[2]

Ondansetron

Drug Info

Approved

Chemotherapy-induced nausea

[3], [4]

Ramosetron

Drug Info

Approved

Nausea and vomiting

[2], [5]

Y-25130

Drug Info

Approved

Nausea and vomiting

[2], [6], [7]

Clinical Trial Drug(s)

[+] 16 Clinical Trial Drugs

Lerisetron

Drug Info

Phase 3

Vomiting

[8]

LITOXETINE

Drug Info

Phase 3

Mood disorder

[9]

Pancopride

Drug Info

Phase 3

Nausea

[10]

Renzapride

Drug Info

Phase 3

Irritable bowel syndrome

[11], [12]

Zatosetron maleate

Drug Info

Phase 3

Anxiety disorder

[13]

AD04

Drug Info

Phase 2

Alcohol dependence

[14]

DDP-225

Drug Info

Phase 2

Irritable bowel syndrome

[12]

KB-6806

Drug Info

Phase 2

Chemotherapy-induced nausea

[8]

Lintopride

Drug Info

Phase 2

Nausea

[15]

Pumosetrag

Drug Info

Phase 2

Irritable bowel syndrome

[12]

ADR-851

Drug Info

Phase 1

Nausea and vomiting

[16]

BIMU-1

Drug Info

Phase 1

Cognitive impairment

[17], [18]

CVN058

Drug Info

Phase 1

Schizophrenia

[19]

ITASETRON

Drug Info

Phase 1

Nausea

[20]

TAK-058

Drug Info

Phase 1

Schizophrenia

[21]

Tedatioxetine

Drug Info

Phase 1

Major depressive disorder

[22]

Discontinued Drug(s)

[+] 17 Discontinued Drugs

RG-12915

Drug Info

Discontinued in Phase 3

Nausea

[23]

BRL-46470

Drug Info

Discontinued in Phase 2

Anxiety disorder

[24], [25]

DAT-582

Drug Info

Discontinued in Phase 2

Nausea

[26]

E-3620

Drug Info

Discontinued in Phase 2

Gastric motility disorder

[27]

Fabesetron

Drug Info

Discontinued in Phase 2

Irritable bowel syndrome

[28]

Lurosetron

Drug Info

Discontinued in Phase 2

Vomiting

[29]

SR-57227

Drug Info

Discontinued in Phase 2

Major depressive disorder

[30], [31]

Mirisetron maleate

Drug Info

Discontinued in Phase 1

Anxiety disorder

[32]

SEP-226332

Drug Info

Discontinued in Phase 1

Obstructive sleep apnea

[33]

WAY-100289

Drug Info

Discontinued in Phase 1

Anxiety disorder

[34]

BP4.879a

Drug Info

Terminated

Schizophrenia

[35]

CR-3124

Drug Info

Terminated

Substance use disorder

[36]

GK-128

Drug Info

Terminated

Vomiting

[37]

GR-65630

Drug Info

Terminated

Vomiting

[38]

SC-52150

Drug Info

Terminated

Vomiting

[39]

SDZ-ICM-567

Drug Info

Terminated

Anxiety disorder

[40]

SRSS-021

Drug Info

Terminated

Vomiting

[41]

Mode of Action

[+] 4 Modes of Action

Antagonist

[+] 15 Antagonist drugs

Granisetron

Drug Info

[1], [42]

Y-25130

Drug Info

[45]

Lerisetron

Drug Info

[8]

AD04

Drug Info

[14]

KB-6806

Drug Info

[8]

CVN058

Drug Info

[53]

TAK-058

Drug Info

[2], [54]

RG-12915

Drug Info

[55]

DAT-582

Drug Info

[57]

SEP-226332

Drug Info

[62]

BP4.879a

Drug Info

[64]

SDZ-ICM-567

Drug Info

[69]

SRSS-021

Drug Info

[70]

BRL 43694A

Drug Info

[72]

Ciproxifan

Drug Info

[73]

Agonist

[+] 1 Agonist drugs

Ondansetron

Drug Info

[43]

Modulator

[+] 26 Modulator drugs

Ramosetron

Drug Info

[44]

LITOXETINE

Drug Info

[46]

Renzapride

Drug Info

[48]

Zatosetron maleate

Drug Info

[49]

DDP-225

Drug Info

[50]

Lintopride

Drug Info

[15]

Pumosetrag

Drug Info

[51]

ADR-851

Drug Info

[52]

BIMU-1

Drug Info

[18]

ITASETRON

Drug Info

[50]

Tedatioxetine

Drug Info

[50]

BRL-46470

Drug Info

[56]

E-3620

Drug Info

[50]

Fabesetron

Drug Info

[58]

Lurosetron

Drug Info

[59]

SR-57227

Drug Info

[60]

Mirisetron maleate

Drug Info

[61]

WAY-100289

Drug Info

[63]

CR-3124

Drug Info

[65]

GK-128

Drug Info

[66]

GR-65630

Drug Info

[67]

SC-52150

Drug Info

[68]

(R)-zacopride

Drug Info

[71]

S-21007

Drug Info

[74]

SC-52491

Drug Info

[75]

SC-54750

Drug Info

[75]

Inhibitor

[+] 1 Inhibitor drugs

Pancopride

Drug Info

[47]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target-Related Models and Studies

Top

Target QSAR Model

References

Top

REF 1

New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7.

REF 2

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 3

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2290).

REF 4

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 5

REF 6

REF 7

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000557)

REF 8

Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.

REF 9

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001264)

REF 10

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001751)

REF 11

REF 12

Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.

REF 13

Concise Dictionary of Pharmacological Agents: Properties and Synonyms, Dr. Ian Morton,I.K. Morton,Judith M. Hall. Page(298).

REF 14

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 15

The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001323)

REF 17

REF 18

Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1994 Apr;349(4):338-45.

REF 19

ClinicalTrials.gov (NCT03669250) CVN058 Effect on Mismatch Negativity in Schizophrenics. U.S. National Institutes of Health.

REF 20

ClinicalTrials.gov (NCT02259985) Effects of Food on the Bioavailability and Pharmacokinetic Profile of Itasetron After a Single Oral Dose in Healthy Male Subjects. U.S. National Institutes of Health.

REF 21

ClinicalTrials.gov (NCT02389881) Safety, Tolerability, and Pharmacokinetics of Multiple-Dose TAK-058 in Healthy Participants. U.S. National Institutes of Health.

REF 22

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023694)

REF 23

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001786)

REF 24

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001328)

REF 26

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001226)

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004004)

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001434)

REF 29

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002948)

REF 30

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001602)

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003649)

REF 33

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129)

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001552)

REF 35

The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.

REF 36

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024202)

REF 37

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002051)

REF 38

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003534)

REF 39

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830)

REF 40

Determination of SDZ ICM 567 in blood and muscle microdialysis samples by microbore liquid chromatography with ultraviolet and fluorescence detection. J Chromatogr B Biomed Sci Appl. 1997 Oct 24;700(1-2):191-200.

REF 41

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090)

REF 42

Reduction of rectal sensitivity and post-prandial motility by granisetron, a 5 HT3-receptor antagonist, in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1993 Apr;7(2):175-80.

REF 43

Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron: a randomized, placebo-controlled, double-blind cross-over trial. Eur J Gastroenterol Hepatol. 1998 Oct;10(10):865-70.

REF 44

Inhibitory effect of YM060 on 5-HT3 receptor-mediated depolarization in colonic myenteric neurons of the guinea pig. Eur J Pharmacol. 1995 Sep 5;283(1-3):107-12.

REF 45

The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist. Eur J Pharmacol. 1991 Apr 24;196(3):299-305.

REF 46

Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45.

REF 47

Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol. 1992 Nov 10;222(2-3):257-64.

REF 48

Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63.

REF 49

Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety. J Clin Psychopharmacol. 1999 Apr;19(2):125-31.

REF 50

Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

REF 51

Novel partial 5HT3 agonist pumosetrag reduces acid reflux events in uninvestigated GERD patients after a standard refluxogenic meal: a randomized, double-blind, placebo-controlled pharmacodynamic study.Neurogastroenterol Motil.2014 Jan;26(1):13-20.

REF 52

Analgesic effects of S and R isomers of the novel 5-HT3 receptor antagonists ADR-851 and ADR-882 in rats. Eur J Pharmacol. 1991 Oct 29;204(1):117-9.

REF 53

Clinical pipeline report, company report or official report of Cerevance.

REF 54

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040805)

REF 55

Cataractogenesis in rats induced by in utero exposure to RG 12915, a 5-HT3 antagonist. Fundam Appl Toxicol. 1995 Sep;27(2):270-6.

REF 56

Evidence that the atypical 5-HT3 receptor ligand, [3H]-BRL46470, labels additional 5-HT3 binding sites compared to [3H]-granisetron. Br J Pharmacol. 1995 Sep;116(2):1781-8.

REF 57

5-HT3 receptor antagonist effects of DAT-582, (R) enantiomer of AS-5370. Eur J Pharmacol. 1992 Jun 17;216(3):435-40.

REF 58

Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. J Pharmacol Exp Ther. 1993 May;265(2):752-8.

REF 59

US patent application no. 7,932,267, Use of α-glucosidase inhibitors to treat alphavirus infections.

REF 60

Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83-90.

REF 61

The effects of 5-HT3 receptor antagonists on cognitive performance in aged monkeys. Neurobiol Aging. 1997 Jan-Feb;18(1):21-8.

REF 62

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129)

REF 63

The selective 5-HT3 receptor antagonist, WAY100289, enhances spatial memory in rats with ibotenate lesions of the forebrain cholinergic projection system. Psychopharmacology (Berl). 1995 Feb;117(3):318-32.

REF 64

5-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking. Neuropsychopharmacology. 2004 Oct;29(10):1807-13.

REF 65

Physicochemical and biopharmaceutical characterization of endo-2-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one (CR312... J Pharm Sci. 2006 Dec;95(12):2706-21.

REF 66

Effect of a novel 5-hydroxytryptamine3 (5-HT3) receptor antagonist, GK-128, on 5-HT3 receptors mediating contractions and relaxations in guinea-pig distal colon. Gen Pharmacol. 1997 Sep;29(3):353-9.

REF 67

Binding of the 5-HT3 ligand, [3H]GR65630, to rat area postrema, vagus nerve and the brains of several species. Eur J Pharmacol. 1989 Jan 10;159(2):157-64.

REF 68

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830)

REF 69

Microdialysis sampling to determine the pharmacokinetics of unbound SDZ ICM 567 in blood and brain in awake, freely-moving rats. Pharm Res. 1995 Feb;12(2):291-4.

REF 70

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090)

REF 71

R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):283-9.

REF 72

BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy. Schweiz Med Wochenschr. 1989 Jun 10;119(23):831-4.

REF 73

The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.

REF 74

Effects of S-21007, a potent 5-HT3 partial agonist, in mouse anxiety. Zhongguo Yao Li Xue Bao. 1999 Sep;20(9):805-12.

REF 75

Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5509-12.

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