Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T83813 Target Info
Target Name 5-HT 2C receptor (HTR2C)
Synonyms
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Target Type Successful Target
Gene Name HTR2C
Biochemical Class GPCR rhodopsin
UniProt ID
5HT2C_HUMAN
Co-Targets of This Target  Top
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) M100907 Drug Info Ki = 0.1 nM Click to Show More [1]
2 Lorcaserin Drug Info Ki = 1.3 nM [3]
3 Nefazodone Drug Info Ki = 5.8 nM [6]
4 Mirtazapine Drug Info Ki = 8.2 nM [8]
5 Methysergide Drug Info Ki = 10 nM [9]
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) METHYLENEDIOXYMETHAMPHETAMINE Drug Info Ki = 0.73 nM Click to Show More [2]
2 Nefazodone Drug Info Ki = 290 nM [6]
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) Lorcaserin Drug Info Ki = 1.3 nM Click to Show More [3]
2 Methysergide Drug Info Ki = 7.586 nM [7]
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) Mirtazapine Drug Info Ki = 1.6 nM Click to Show More [4]
2 M100907 Drug Info Ki = 1000 nM [1]
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) Metergolin Drug Info Ki = 2.3 nM Click to Show More [5]
2 Mirtazapine Drug Info Ki = 18 nM [8]
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) Mirtazapine Drug Info Ki = 18 nM [4]
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) Mirtazapine Drug Info Ki = 20 nM [4]
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) Mirtazapine Drug Info Ki ~ 20 nM [10]
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) Mirtazapine Drug Info Ki ~ 25 nM [10]
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) Mirtazapine Drug Info IC50 = 223.87 nM [11]
Co-Target Name Norepinephrine transporter (NET) Successful Target
UniProt ID SC6A2_HUMAN
Gene Name SLC6A2
Synonyms
Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1
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Representative Drug(s) METHYLENEDIOXYMETHAMPHETAMINE Drug Info Ki = 398 nM [12]
Co-Target Name Carbonic anhydrase XII (CA-XII) Successful Target
UniProt ID CAH12_HUMAN
Gene Name CA12
Synonyms
Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII
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Representative Drug(s) Puerarin Drug Info Ki = 515 nM [13]
Co-Target Name Dopamine transporter (DAT) Successful Target
UniProt ID SC6A3_HUMAN
Gene Name SLC6A3
Synonyms
Solute carrier family 6 member 3; Sodium-dependent dopamine transporter; DAT1; DAT; DA transporter
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Representative Drug(s) METHYLENEDIOXYMETHAMPHETAMINE Drug Info Ki = 897 nM [12]
Co-Target Name Opioid receptor mu (MOP) Successful Target
UniProt ID OPRM_HUMAN
Gene Name OPRM1
Synonyms
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Representative Drug(s) Tramadol Drug Info EC50 = 1000 nM [14]
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) Metergolin Drug Info Ki = 6.31 nM Click to Show More [15]
2 Mirtazapine Drug Info Ki = 265 nM [4]
Co-Target Name Albendazole monooxygenase (CYP3A4) Clinical trial Target
UniProt ID CP3A4_HUMAN
Gene Name CYP3A4
Synonyms
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) Nefazodone Drug Info IC50 = 15 nM [16]
Co-Target Name Carbonic anhydrase VII (CA-VII) Patented-recorded Target
UniProt ID CAH7_HUMAN
Gene Name CA7
Synonyms
Carbonic anhydrase 7; Carbonate dehydratase VII
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Representative Drug(s) Puerarin Drug Info Ki = 452.6 nM [13]
References  Top
REF 1 Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders. J Med Chem. 2010 Nov 11;53(21):7778-95.
REF 2 Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter. Bioorg Med Chem. 2008 Jun 15;16(12):6364-70.
REF 3 Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists. Bioorg Med Chem Lett. 2013 Jan 1;23(1):330-5.
REF 4 Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. J Med Chem. 2005 Mar 24;48(6):1709-12.
REF 5 Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1834-8.
REF 6 Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter. J Med Chem. 2011 Sep 22;54(18):6305-18.
REF 7 The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. Bioorg Med Chem Lett. 2014 Jan 15;24(2):576-9.
REF 8 Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system. Bioorg Med Chem Lett. 2019 Nov 1;29(21):126679.
REF 9 Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4.
REF 10 Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine. J Med Chem. 2002 Jul 18;45(15):3280-5.
REF 11 New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants. Bioorg Med Chem Lett. 2000 Jan 3;10(1):71-4.
REF 12 An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3411-5.
REF 13 New natural product carbonic anhydrase inhibitors incorporating phenol moieties. Bioorg Med Chem. 2015 Nov 15;23(22):7219-25.
REF 14 Discovery of Potent and Selective Agonists of delta Opioid Receptor by Revisiting the "Message-Address" Concept. ACS Med Chem Lett. 2016 Feb 10;7(4):391-6.
REF 15 Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives. J Med Chem. 2003 Dec 18;46(26):5638-50.
REF 16 Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. J Med Chem. 2012 Jun 14;55(11):4896-933.

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