Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T75984 Target Info
Target Name 5-HT 2 receptor (5HT2R)
Synonyms
Serotonin receptor 2; 5-hydroxytryptamine receptor 2; 5-HT2 receptor
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class GPCR rhodopsin
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
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) Ketanserin Drug Info IC50 = 1 nM [1]
Co-Target Name Histamine H1 receptor (H1R) Successful Target
UniProt ID HRH1_HUMAN
Gene Name HRH1
Synonyms
HH1R; H1R
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Representative Drug(s) Mianserin Drug Info Ki = 1.7 nM Click to Show More [2]
2 Ketanserin Drug Info Ki = 2 nM [3]
3 Quetiapine Drug Info Ki = 8.7 nM [5]
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) Ketanserin Drug Info Ki = 3.5 nM Click to Show More [4]
2 Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name Adrenergic receptor alpha-2C (ADRA2C) Successful Target
UniProt ID ADA2C_HUMAN
Gene Name ADRA2C
Synonyms
Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
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Representative Drug(s) Mianserin Drug Info Ki = 3.8 nM Click to Show More [2]
2 Quetiapine Drug Info Ki = 100 nM [10]
Co-Target Name Adrenergic receptor alpha-2A (ADRA2A) Successful Target
UniProt ID ADA2A_HUMAN
Gene Name ADRA2A
Synonyms
Alpha-2AAR; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; ADRAR; ADRA2R
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Representative Drug(s) Mianserin Drug Info Ki = 4.8 nM Click to Show More [2]
2 Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name Muscarinic acetylcholine receptor M1 (CHRM1) Successful Target
UniProt ID ACM1_HUMAN
Gene Name CHRM1
Synonyms
M1 receptor
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Representative Drug(s) Quetiapine Drug Info Ki = 56 nM [4]
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) Quetiapine Drug Info Ki = 63.1 nM Click to Show More [6]
2 Ketanserin Drug Info Ki = 240 nM [11]
Co-Target Name Synaptic vesicle amine transporter (SLC18A2) Successful Target
UniProt ID VMAT2_HUMAN
Gene Name SLC18A2
Synonyms
Vesicular amine transporter; Vesicular Monoamine Transporter; VMAT; VAT; Solute carrier family 18 member 2; SLC18A2; Monoamine transporter
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Representative Drug(s) Ketanserin Drug Info Ki = 77 nM [7]
Co-Target Name 5-HT 1A receptor (HTR1A) Successful Target
UniProt ID 5HT1A_HUMAN
Gene Name 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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Representative Drug(s) Quetiapine Drug Info Ki = 79.43 nM Click to Show More [8]
2 Mianserin Drug Info IC50 = 398.11 nM [13]
Co-Target Name Adrenergic receptor Alpha-2 (ADRA2) Successful Target
UniProt ID ADA2A_HUMAN; ADA2B_HUMAN; ADA2C_HUMAN
Gene Name NO-GeName
Synonyms
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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Representative Drug(s) Quetiapine Drug Info Ki = 87 nM Click to Show More [9]
2 Quetiapine Drug Info Ki = 87 nM [9]
Co-Target Name Adrenergic receptor alpha-1B (ADRA1B) Successful Target
UniProt ID ADA1B_HUMAN
Gene Name ADRA1B
Synonyms
Alpha-1B adrenoreceptor; Alpha-1B adrenoceptor; Alpha-1B adrenergic receptor; Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
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Representative Drug(s) Quetiapine Drug Info Ki = 100 nM [10]
Co-Target Name Adrenergic receptor alpha-1A (ADRA1A) Successful Target
UniProt ID ADA1A_HUMAN
Gene Name ADRA1A
Synonyms
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
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Representative Drug(s) Quetiapine Drug Info Ki = 100 nM Click to Show More [10]
2 Mianserin Drug Info IC50 = 407.38 nM [13]
Co-Target Name Muscarinic acetylcholine receptor M4 (CHRM4) Successful Target
UniProt ID ACM4_HUMAN
Gene Name CHRM4
Synonyms
M4 receptor; CHRM4
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Representative Drug(s) Quetiapine Drug Info Ki = 125.89 nM [8]
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) Quetiapine Drug Info Ki = 251.19 nM [8]
Co-Target Name 5-HT 1D receptor (HTR1D) Successful Target
UniProt ID 5HT1D_HUMAN
Gene Name HTR1D
Synonyms
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
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Representative Drug(s) Ketanserin Drug Info IC50 = 260 nM Click to Show More [12]
2 Mianserin Drug Info IC50 = 380.19 nM [13]
3 Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name Dopamine D1 receptor (D1R) Successful Target
UniProt ID DRD1_HUMAN
Gene Name DRD1
Synonyms
D(1A) dopamine receptor
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Representative Drug(s) Quetiapine Drug Info Ki = 390 nM [4]
Co-Target Name Adrenergic receptor alpha-2B (ADRA2B) Successful Target
UniProt ID ADA2B_HUMAN
Gene Name ADRA2B
Synonyms
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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Representative Drug(s) Quetiapine Drug Info Ki = 1000 nM [10]
Co-Target Name Muscarinic acetylcholine receptor M2 (CHRM2) Successful Target
UniProt ID ACM2_HUMAN
Gene Name CHRM2
Synonyms
M2 receptor; CHRM2
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name Muscarinic acetylcholine receptor M3 (CHRM3) Successful Target
UniProt ID ACM3_HUMAN
Gene Name CHRM3
Synonyms
M3 receptor; CHRM3
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name Muscarinic acetylcholine receptor M5 (CHRM5) Successful Target
UniProt ID ACM5_HUMAN
Gene Name CHRM5
Synonyms
CHRM5
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name Dopamine D5 receptor (D5R) Successful Target
UniProt ID DRD5_HUMAN
Gene Name DRD5
Synonyms
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name 5-HT 1B receptor (HTR1B) Successful Target
UniProt ID 5HT1B_HUMAN
Gene Name HTR1B
Synonyms
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name 5-HT 1E receptor (HTR1E) Successful Target
UniProt ID 5HT1E_HUMAN
Gene Name HTR1E
Synonyms
Serotonin receptor 1E; S31; 5-hydroxytryptamine receptor 1E; 5-HT1E; 5-HT-1E; 5-HT 1E
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
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) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name 5-HT 5A receptor (HTR5A) Successful Target
UniProt ID 5HT5A_HUMAN
Gene Name HTR5A
Synonyms
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
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Representative Drug(s) Quetiapine Drug Info Ki ~ 1000 nM [10]
Co-Target Name 5-HT 6 receptor (HTR6) Clinical trial Target
UniProt ID 5HT6R_HUMAN
Gene Name HTR6
Synonyms
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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Representative Drug(s) Mianserin Drug Info Ki = 55 nM Click to Show More [14]
2 Quetiapine Drug Info Ki ~ 1000 nM [10]
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) Mianserin Drug Info Ki = 56 nM Click to Show More [2]
2 Quetiapine Drug Info Ki = 63.1 nM [8]
Co-Target Name HUAMN alpha-1 adrenergic receptor (ADRA1) Literature-reported Target
UniProt ID ADA1A_HUMAN; ADA1B_HUMAN; ADA1D_HUMAN
Gene Name ADRA1A; ADRA1B; ADRA1D
Synonyms
Alpha-1 adrenoreceptor
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Representative Drug(s) Ketanserin Drug Info Ki = 3.5 nM l-1 hr-1 Click to Show More [15]
2 Quetiapine Drug Info Ki = 4.5 nM [4]
References  Top
REF 1 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 2 Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. J Med Chem. 2005 Mar 24;48(6):1709-12.
REF 3 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. J Med Chem. 2012 Jun 28;55(12):5749-59.
REF 4 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
REF 5 Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. Bioorg Med Chem. 2008 Aug 1;16(15):7291-301.
REF 6 Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?. Bioorg Med Chem Lett. 2001 May 21;11(10):1313-6.
REF 7 Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter. J Med Chem. 2018 Oct 25;61(20):9121-31.
REF 8 Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. J Med Chem. 2007 Oct 18;50(21):5103-8.
REF 9 Selective optimization of side activities: another way for drug discovery. J Med Chem. 2004 Mar 11;47(6):1303-14.
REF 10 The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic. Medchemcomm. 2012;3:580-3.
REF 11 N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. Bioorg Med Chem Lett. 2000 Mar 6;10(5):509-12.
REF 12 3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype. J Med Chem. 1997 Oct 24;40(22):3497-500.
REF 13 Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1. Bioorg Med Chem Lett. 2002 Jan 21;12(2):243-8.
REF 14 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
REF 15 N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2457-61.

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