Target Information

Target General Information

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Target ID

T67054 (Former ID: TTDR00155)

Target Name

5-HT 1 receptor (5HT1R)

Synonyms

Serotonin receptor 1; 5-hydroxytryptamine receptor 1; 5-HT1 receptor

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Gene Name

NO-GeName

Target Type

Patented-recorded target

[1]

Disease

[+] 3 Target-related Diseases

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

Depression [ICD-11: 6A70-6A7Z]

Migraine [ICD-11: 8A80]

BioChemical Class

GPCR rhodopsin

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Discontinued Drug(s)

[+] 3 Discontinued Drugs

Befiperide

Drug Info

Terminated

Anxiety disorder

[2]

FCE-25876

Drug Info

Terminated

Major depressive disorder

[3]

SRSS-023

Drug Info

Terminated

Migraine

[4]

Mode of Action

[+] 3 Modes of Action

Agonist

[+] 5 Agonist drugs

Aryl piperazine derivative 14

Drug Info

[1]

Aryl piperazine derivative 15

Drug Info

[1]

Aryl piperazine derivative 16

Drug Info

[1]

RU 24969

Drug Info

[7]

SRSS-023

Drug Info

[8]

Modulator

[+] 2 Modulator drugs

Befiperide

Drug Info

[5]

FCE-25876

Drug Info

[6]

Antagonist

[+] 1 Antagonist drugs

Cyanopindolol

Drug Info

[9]

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

References

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REF 1

5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.

REF 2

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000673)

REF 3

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001389)

REF 4

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019089)

REF 5

Behavioral Pharmacology of 5-ht. Paul Bevan, Paul Bevan Duphar, Alexander R. Cools. 2013. Figure(15.2).

REF 6

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001389)

REF 7

Effect of chronic treatment with 5-HT1 agonist (8-OH-DPAT and RU 24969) and antagonist (isapirone) drugs on the behavioural responses of mice to 5-HT1 and 5-HT2 agonists. Br J Pharmacol. 1986 Oct;89(2):377-84.

REF 8

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019089)

REF 9

The inhibitory effect of serotonin on the spontaneous discharge of suprachiasmatic neurons in hypothalamic slice is mediated by 5-HT(7) receptor. Brain Res Bull. 2001 Mar 1;54(4):395-8.

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