Target Information

Target General Information

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Target ID

T85605 (Former ID: TTDS00097)

Target Name

5-HT receptor (5HTR)

Synonyms

5-Hydroxytryptamine receptor

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Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 6 Target-related Diseases

Anxiety disorder [ICD-11: 6B00-6B0Z]

Cerebral ischaemia [ICD-11: 8B1Z]

Headache [ICD-11: 8A80-8A84]

Nausea/vomiting [ICD-11: MD90]

Pituitary gland disorder [ICD-11: 5A60-5A61]

Schizophrenia [ICD-11: 6A20]

BioChemical Class

GPCR rhodopsin

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 6 Approved Drugs

Metergolin

Drug Info

Approved

Hyperprolactinaemia

[1]

Nafronyl

Drug Info

Approved

Cerebrovascular ischaemia

[1]

Paliperidone

Drug Info

Approved

Schizophrenia

[1], [2], [3]

Pizotyline

Drug Info

Approved

Headache

[4], [1]

Ramosetron

Drug Info

Approved

Nausea and vomiting

[5], [1]

Tandospirone

Drug Info

Approved

Anxiety disorder

[6], [1]

Clinical Trial Drug(s)

[+] 9 Clinical Trial Drugs

Fenfluramine

Drug Info

Phase 3

Dravet syndrome

[7], [8]

ITI-007

Drug Info

Phase 3

Insomnia

[9], [10]

EPX-200

Drug Info

Phase 2

Dravet syndrome

[7]

Lu-AA34893

Drug Info

Phase 2

Anxiety disorder

[11]

MIN-117

Drug Info

Phase 2

Major depressive disorder

[12]

SEP--4199

Drug Info

Phase 2

Bipolar disorder

[13]

BF-1

Drug Info

Phase 1

Cluster headache

[14]

DSP-6745

Drug Info

Phase 1

Parkinson disease

[7], [15]

EPX-100

Drug Info

Phase 1

Dravet syndrome

[7]

Discontinued Drug(s)

[+] 3 Discontinued Drugs

Ritanserin

Drug Info

Discontinued in Phase 3

Anxiety disorder

[16], [17]

REV-598

Drug Info

Terminated

Carcinoid syndrome

[18]

RGH-2721

Drug Info

Terminated

Psychotic disorder

[19]

Mode of Action

[+] 3 Modes of Action

Modulator

[+] 11 Modulator drugs

Metergolin

Drug Info

[20], [21]

Nafronyl

Drug Info

[1]

Pizotyline

Drug Info

[1]

Ramosetron

Drug Info

[20]

Tandospirone

Drug Info

[20]

EPX-200

Drug Info

[7]

EPX-300

Drug Info

[7]

Lu-AA34893

Drug Info

[23]

BF-1

Drug Info

[24]

EPX-100

Drug Info

[7]

RGH-2721

Drug Info

[27]

Antagonist

[+] 10 Antagonist drugs

Paliperidone

Drug Info

[1]

Fenfluramine

Drug Info

[22]

ITI-007

Drug Info

[15]

MIN-117

Drug Info

[15]

SEP--4199

Drug Info

[13]

DSP-6745

Drug Info

[7]

Ritanserin

Drug Info

[25]

EpiCept

Drug Info

[28]

MCI

Drug Info

[29]

SB 203106

Drug Info

[30]

Inhibitor

[+] 1 Inhibitor drugs

REV-598

Drug Info

[26]

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

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

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

REF 2

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: 7258).

REF 3

ClinicalTrials.gov (NCT02146547) European Long-acting Antipsychotics in Schizophrenia Trial. U.S. National Institutes of Health.

REF 4

REF 5

REF 6

REF 7

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

REF 8

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

REF 9

ClinicalTrials.gov (NCT02469155) A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment.

REF 10

Clinical pipeline report, company report or official report of Intra-Cellular Therapies.

REF 11

ClinicalTrials.gov (NCT00622245) Efficacy and Safety of Lu AA34893 in Patients With Bipolar Depression. U.S. National Institutes of Health.

REF 12

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037483)

REF 13

ClinicalTrials.gov (NCT03543410) A Clinical Study to Test the Effectiveness of an Investigational Drug to Treat People That Have Major Depressive Episodes When They Have Bipolar 1 Depression. U.S. National Institutes of Health.

REF 14

REF 15

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

REF 16

REF 17

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000237)

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)

REF 19

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004008)

REF 20

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

REF 21

Endocrine profile and therapeutic employment of a new prolactin-lowering drug, metergoline. Gynecol Obstet Invest. 1980;11(1):1-16.

REF 22

Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.

REF 23

Encyclopedia of Psychopharmacology. Ian Stolerman. 2010. Page(105).

REF 24

Serotonin (5-HT2B) receptor. SciBX 4(19); doi:10.1038/scibx.2011.534. May 12 2011

REF 25

Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82.

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 800016819)

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 800004008)

REF 28

Emerging therapies for neuropathic pain. Expert Opin Emerg Drugs. 2005 Feb;10(1):95-108.

REF 29

Effect of a serotonin receptor antagonist on interleukin-6-induced pulmonary hypertension in rats. Chest. 2001 Feb;119(2):554-61.

REF 30

5-Hydroxytryptamine mediated contractions in isolated preparations of equine ileum and pelvic flexure: pharmacological characterization of a new 5-HT(4) agonist. J Vet Pharmacol Ther. 2002 Feb;25(1):49-58.

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