Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T78709 Target Info
Target Name 5-HT 1A receptor (HTR1A)
Synonyms
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Target Type Successful Target
Gene Name HTR1A
Biochemical Class GPCR rhodopsin
UniProt ID
5HT1A_HUMAN
Co-Targets of This Target  Top
Co-Target Name Dopamine D2 receptor (D2R) Successful Target
UniProt ID DRD2_HUMAN
Gene Name DRD2
Synonyms
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) OPC-34712 Drug Info Ki = 0.3 nM Click to Show More [1]
2 Sarizotan Drug Info IC50 < 6 nM [4]
3 Buspirone Drug Info Ki = 13 nM [5]
4 Vilazodone Drug Info Ki = 666 nM [9]
Co-Target Name 5-HT 2B receptor (HTR2B) Successful Target
UniProt ID 5HT2B_HUMAN
Gene Name HTR2B
Synonyms
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) OPC-34712 Drug Info Ki = 0.3981 nM [1]
Co-Target Name Serotonin transporter (SERT) Successful Target
UniProt ID SC6A4_HUMAN
Gene Name SLC6A4
Synonyms
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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Representative Drug(s) Vilazodone Drug Info IC50 = 0.4 nM Click to Show More [2]
2 DSP-1053 Drug Info Ki = 1.02 nM [3]
Co-Target Name 5-HT 2A receptor (HTR2A) Successful Target
UniProt ID 5HT2A_HUMAN
Gene Name HTR2A
Synonyms
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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Representative Drug(s) OPC-34712 Drug Info Ki = 0.47 nM Click to Show More [1]
2 Buspirone Drug Info Ki = 851 nM [10]
Co-Target Name Dopamine D3 receptor (D3R) Successful Target
UniProt ID DRD3_HUMAN
Gene Name DRD3
Synonyms
D(3) dopamine receptor
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Representative Drug(s) Sarizotan Drug Info IC50 < 6 nM Click to Show More [4]
2 Buspirone Drug Info Ki = 660 nM [8]
Co-Target Name Dopamine D4 receptor (D4R) Successful Target
UniProt ID DRD4_HUMAN
Gene Name DRD4
Synonyms
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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Representative Drug(s) Sarizotan Drug Info IC50 < 6 nM [4]
Co-Target Name 5-HT 3A receptor (HTR3A) Successful Target
UniProt ID 5HT3A_HUMAN
Gene Name HTR3A
Synonyms
Serotonin-gated ion channel receptor; Serotonin receptor 3A; HTR3; 5HT3R; 5-hydroxytryptamine receptor 3A; 5-HT3RA; 5-HT3A; 5-HT3-A; 5-HT 3A
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Representative Drug(s) Sarizotan Drug Info IC50 < 6 nM [4]
Co-Target Name Opioid receptor sigma 1 (OPRS1) Successful Target
UniProt ID SGMR1_HUMAN
Gene Name SIGMAR1
Synonyms
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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Representative Drug(s) Buspirone Drug Info IC50 = 36.31 nM Click to Show More [6]
2 OPC-14523 Drug Info IC50 = 47 nM [7]
Co-Target Name 5-HT 7 receptor (HTR7) Clinical trial Target
UniProt ID 5HT7R_HUMAN
Gene Name HTR7
Synonyms
Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
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Representative Drug(s) OPC-34712 Drug Info Ki = 3.7 nM [1]
References  Top
REF 1 Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect. Eur J Med Chem. 2019 Dec 1;183:111736.
REF 2 Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. Bioorg Med Chem. 2018 Jul 23;26(12):3117-25.
REF 3 Discovery of DSP-1053, a novel benzylpiperidine derivative with potent serotonin transporter inhibitory activity and partial 5-HT. Bioorg Med Chem. 2018 May 1;26(8):1614-27.
REF 4 Multi-target-directed ligands to combat neurodegenerative diseases. J Med Chem. 2008 Feb 14;51(3):347-72.
REF 5 Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants. J Med Chem. 1993 Jul 23;36(15):2066-74.
REF 6 Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor. J Med Chem. 1994 Nov 25;37(24):4109-17.
REF 7 Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic. Eur J Med Chem. 2014 May 22;79:216-30.
REF 8 New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. J Med Chem. 1997 Mar 14;40(6):952-60.
REF 9 Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants. Eur J Med Chem. 2012 Jul;53:124-32.
REF 10 Synthesis and serotonin receptor activity of the arylpiperazine alkyl/propoxy derivatives of new azatricycloundecanes. Eur J Med Chem. 2009 Jan;44(1):152-64.

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