Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T21945 Target Info
Target Name Norepinephrine transporter (NET)
Synonyms
Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1
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Target Type Successful Target
Gene Name SLC6A2
Biochemical Class Neurotransmitter:sodium symporter
UniProt ID
SC6A2_HUMAN
Co-Targets of This Target  Top
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) Duloxetine Drug Info Ki = 0.24 nM Click to Show More [1]
2 Imipramine Drug Info Ki = 0.52 nM [3]
3 METHYLENEDIOXYMETHAMPHETAMINE Drug Info Ki = 0.73 nM [4]
4 Amitriptyline Drug Info Ki = 4.3 nM [8]
5 Venlafaxine Drug Info Ki = 11 nM [1]
6 Amitifadine Drug Info IC50 = 12.3 nM [10]
7 Desipramine Drug Info Ki = 20 nM [12]
8 Milnacipran Drug Info Ki = 22 nM [13]
9 Cocaine Drug Info Ki = 45 nM [16]
10 Mazindol Drug Info Ki = 45 nM [11]
11 Atomoxetine Drug Info IC50 = 48 nM [17]
12 Bupropion Drug Info IC50 ~ 100 nM [7]
13 Bicifadine Drug Info IC50 = 117 nM [20]
14 Levomilnacipran Drug Info IC50 = 320 nM [24]
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) Desipramine Drug Info Ki = 0.49 nM Click to Show More [2]
2 Mazindol Drug Info IC50 = 13 nM [11]
3 Cocaine Drug Info Ki = 32 nM [15]
4 Amitifadine Drug Info Ki = 79.43 nM [18]
5 Duloxetine Drug Info Ki = 240 nM [23]
6 Bupropion Drug Info Ki = 441 nM [25]
7 Venlafaxine Drug Info Ki ~ 890 nM [1]
8 METHYLENEDIOXYMETHAMPHETAMINE Drug Info Ki = 897 nM [26]
9 Bicifadine Drug Info IC50 = 910 nM [20]
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) Amitriptyline Drug Info Ki = 1.12 nM Click to Show More [5]
2 Maprotiline Drug Info Ki = 1.67 nM [5]
3 Imipramine Drug Info IC50 = 27 nM [14]
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) Amoxapine Drug Info Ki = 1.77 nM Click to Show More [6]
2 Imipramine Drug Info Ki = 94 nM [19]
3 Desipramine Drug Info Ki = 160 nM [21]
Co-Target Name Neuronal acetylcholine receptor alpha-3/beta-4 (CHRNA3/B4) Successful Target
UniProt ID ACHA3_HUMAN-ACHB4_HUMAN
Gene Name CHRNA3-CHRNB4
Synonyms
Neuronal acetylcholine receptor
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Representative Drug(s) Bupropion Drug Info IC50 = 1.8 nM [7]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) Cocaine Drug Info IC50 = 4.4 nM [9]
Co-Target Name Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2) Successful Target
UniProt ID ACHA4_HUMAN-ACHB2_HUMAN
Gene Name CHRNA4-CHRNB2
Synonyms
CHRN; nAChR
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Representative Drug(s) Bupropion Drug Info IC50 = 12 nM [7]
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) Amoxapine Drug Info Ki = 34 nM [6]
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) Amitriptyline Drug Info Ki = 89 nM Click to Show More [5]
2 Maprotiline Drug Info Ki = 402 nM [5]
Co-Target Name 5-HT 2C receptor (HTR2C) Successful Target
UniProt ID 5HT2C_HUMAN
Gene Name 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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Representative Drug(s) Imipramine Drug Info Ki = 160 nM [19]
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) Amitriptyline Drug Info Ki = 170 nM Click to Show More [5]
2 Maprotiline Drug Info Ki = 429 nM [5]
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) Amitriptyline Drug Info Ki = 196 nM Click to Show More [5]
2 Imipramine Drug Info IC50 = 410 nM [14]
3 Maprotiline Drug Info Ki = 665 nM [5]
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) Amitriptyline Drug Info Ki = 206 nM Click to Show More [5]
2 Maprotiline Drug Info Ki = 504 nM [5]
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) Amoxapine Drug Info Ki = 221 nM [6]
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) Mazindol Drug Info IC50 = 234.42 nM [22]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) Duloxetine Drug Info IC50 = 1000 nM [27]
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) Duloxetine Drug Info IC50 = 440 nM [28]
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) Amoxapine Drug Info Ki = 500 nM [29]
Co-Target Name Voltage-gated sodium channel alpha Nav1.7 (SCN9A) Clinical trial Target
UniProt ID SCN9A_HUMAN
Gene Name SCN9A
Synonyms
hNE-Na; Voltage-gated sodium channel subunit alpha Nav1.7; Sodium channel proteintype IX subunit alpha; Sodium channel proteintype 9 subunit alpha; Sodium channel protein type IX subunit alpha; Sodium channel protein type 9 subunit alpha; Peripheral sodium channel 1; PN1; Neuroendocrine sodium channel; NENA
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Representative Drug(s) Amitriptyline Drug Info IC50 = 1000 nM [30]
Co-Target Name Histamine H3 receptor (H3R) Clinical trial Target
UniProt ID HRH3_HUMAN
Gene Name HRH3
Synonyms
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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Representative Drug(s) Maprotiline Drug Info Ki ~ 1000 nM Click to Show More [5]
2 Amitriptyline Drug Info Ki ~ 1000 nM [5]
Co-Target Name Acetylcholine receptor alpha-1/beta-1/delta/gamma (CHRNA1/CHRNA1/CHRND/CHRNG) Co-Target
UniProt ID ACHA_HUMAN-ACHB_HUMAN-ACHD_HUMAN-ACHG_HUMAN
Gene Name CHRNA1-CHRNB1-CHRND-CHRNG
Representative Drug(s) Bupropion Drug Info IC50 = 7.9 nM [7]
Co-Target Name Neuronal acetylcholine receptor alpha4/beta4 (CHRNA4/CHRNB4) Co-Target
UniProt ID ACHA4_HUMAN; ACHB4_HUMAN
Gene Name CHRNA4; CHRNB4
Representative Drug(s) Bupropion Drug Info IC50 = 15 nM [7]
Co-Target Name Solute carrier family 22 member 2 (SLC22A2) Co-Target
UniProt ID S22A2_HUMAN
Gene Name SLC22A2
Synonyms
Organic cation transporter 2; hOCT2
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Representative Drug(s) Imipramine Drug Info IC50 = 600 nM [31]
Co-Target Name Neuronal acetylcholine receptor alpha3/beta2 (CHRNA3/CHRNB2) Co-Target
UniProt ID ACHA3_HUMAN; ACHB2_HUMAN
Gene Name CHRNA3; CHRNB2
Representative Drug(s) Bupropion Drug Info IC50 = 1000 nM [32]
References  Top
REF 1 Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor. ACS Med Chem Lett. 2013 May 7;4(6):560-4.
REF 2 Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography. J Med Chem. 2003 Mar 13;46(6):925-35.
REF 3 Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. Eur J Med Chem. 2013 May;63:85-94.
REF 4 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 5 Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42.
REF 6 New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. J Med Chem. 2012 Feb 23;55(4):1572-82.
REF 7 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. J Med Chem. 2010 Mar 11;53(5):2204-14.
REF 8 The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. Bioorg Med Chem Lett. 2014 Jan 15;24(2):576-9.
REF 9 Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers. J Med Chem. 2002 Aug 29;45(18):3844-53.
REF 10 Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6.
REF 11 Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. J Med Chem. 2017 Apr 13;60(7):3109-3123.
REF 12 Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phen... J Med Chem. 2010 Nov 11;53(21):7869-73.
REF 13 Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HT. Bioorg Med Chem. 2017 Jan 1;25(1):293-304.
REF 14 Polypharmacology-foe or friend? J Med Chem. 2013 Nov 27;56(22):8955-71.
REF 15 Synthesis and ligand binding of eta(6)-(2beta-carbomethoxy-3beta-phenyltropane) transition metal complexes. J Med Chem. 1996 Mar 29;39(7):1560-3.
REF 16 Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes. J Med Chem. 2005 Nov 17;48(23):7437-44.
REF 17 Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4929-31.
REF 18 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor. J Med Chem. 2010 Jul 8;53(13):4989-5001.
REF 19 Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA). Bioorg Med Chem Lett. 2004 May 3;14(9):2279-83.
REF 20 Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges. J Med Chem. 2018 Mar 22;61(6):2133-65.
REF 21 Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene. Bioorg Med Chem Lett. 2001 Mar 12;11(5):655-8.
REF 22 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 23 Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4477-80.
REF 24 Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3328-32.
REF 25 A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone. Bioorg Med Chem. 2009 Jun 1;17(11):3770-4.
REF 26 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 27 4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships. Bioorg Med Chem Lett. 2009 May 15;19(10):2829-34.
REF 28 Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3234-7.
REF 29 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 30 3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models. J Med Chem. 2012 Aug 9;55(15):6866-80.
REF 31 Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. J Med Chem. 2011 Jul 14;54(13):4548-58.
REF 32 Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. J Med Chem. 2005 Jul 28;48(15):4705-45.

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