Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T31424 Target Info
Target Name Adrenergic receptor Alpha-2 (ADRA2)
Synonyms
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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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 Adrenergic receptor alpha-1D (ADRA1D) Successful Target
UniProt ID ADA1D_HUMAN
Gene Name ADRA1D
Synonyms
Alpha-adrenergic receptor 1a; Alpha-1D adrenoreceptor; Alpha-1D adrenoceptor; Alpha-1D adrenergic receptor; Alpha adrenergic receptor 1a; Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; ADRA1A
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Representative Drug(s) Drug Info Ki = 0.015 nM Click to Show More [1]
2 Yohimbine Drug Info Ki = 1.6 nM [3]
3 Guanabenz Drug Info Ki = 232 nM [6]
4 Clonidine Drug Info Ki = 595 nM [6]
5 Brimonidine Drug Info Ki = 933.25 nM [14]
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) Oxymetazoline Drug Info Ki = 0.3 nM [2]
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) Oxymetazoline Drug Info Ki = 0.4 nM [2]
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) Yohimbine Drug Info Ki = 1.1 nM Click to Show More [3]
2 Oxymetazoline Drug Info Ki = 831.76 nM [5]
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) Yohimbine Drug Info IC50 = 8.4 nM Click to Show More [4]
2 Oxymetazoline Drug Info IC50 = 200 nM [6]
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) Oxymetazoline Drug Info Ki = 15.85 nM Click to Show More [5]
2 Clonidine Drug Info Ki = 512.86 nM [13]
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) Yohimbine Drug Info Ki = 47 nM Click to Show More [6]
2 Guanabenz Drug Info Ki = 62 nM [6]
Co-Target Name Trace amine-associated receptor-1 (TAAR1) Successful Target
UniProt ID TAAR1_HUMAN
Gene Name TAAR1
Synonyms
Trace amine receptor 1; TaR-1; TAAR1
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Representative Drug(s) Guanabenz Drug Info EC50 = 90 nM [7]
Co-Target Name Monoamine oxidase (MAO) Successful Target
UniProt ID AOFA_HUMAN; AOFB_HUMAN
Gene Name NO-GeName
Synonyms
Human monoamine oxidase
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Representative Drug(s) Clonidine Drug Info Ki ~ 100 nM [8]
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) Guanabenz Drug Info Ki = 107 nM Click to Show More [6]
2 Oxymetazoline Drug Info Ki = 303 nM [6]
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) Guanabenz Drug Info Ki = 112 nM Click to Show More [6]
2 Oxymetazoline Drug Info Ki = 367 nM [6]
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) Lofexidine Drug Info Ki = 125.89 nM [9]
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) Meperidine Drug Info IC50 = 315 nM [10]
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) Meperidine Drug Info IC50 = 323.59 nM [11]
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) Oxymetazoline Drug Info Ki = 455 nM [6]
Co-Target Name Opioid receptor delta (OPRD1) Successful Target
UniProt ID OPRD_HUMAN
Gene Name OPRD1
Synonyms
OPRD; Delta-type opioid receptor; Delta opioid receptor; DOR-1; D-OR-1
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Representative Drug(s) Meperidine Drug Info IC50 = 500 nM [12]
Co-Target Name Opioid receptor kappa (OPRK1) Successful Target
UniProt ID OPRK_HUMAN
Gene Name OPRK1
Synonyms
OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1
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Representative Drug(s) Meperidine Drug Info IC50 = 500 nM [12]
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) Yohimbine Drug Info Ki = 687 nM [6]
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) Oxymetazoline Drug Info Ki = 957 nM [6]
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) Oxymetazoline Drug Info Ki = 775 nM Click to Show More [6]
2 Yohimbine Drug Info Ki = 784 nM [6]
Co-Target Name Imidazoline receptor 1 (IR1) Literature-reported Target
UniProt ID NISCH_HUMAN
Gene Name NISCH
Synonyms
hIRAS; KIAA0975; Imidazoline-1 receptor candidate protein; Imidazoline-1 receptor; Imidazoline receptor antisera-selected protein; IRAS; IR1; I1R candidate protein; I-1 receptor candidate protein; I-1
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Representative Drug(s) Oxymetazoline Drug Info Ki = 6.194 nM Click to Show More [15]
2 Clonidine Drug Info Ki = 8.9 nM [16]
3 Tizanidine Drug Info Ki = 28.3 nM [15]
4 Guanabenz Drug Info Ki = 34.67 nM [15]
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) Apraclonidine Drug Info EC50 = 180 nM Click to Show More [17]
2 Clonidine Drug Info EC50 = 290 nM [17]
Co-Target Name Solute carrier family 22 member 1 (SLC22A1) Co-Target
UniProt ID S22A1_HUMAN
Gene Name SLC22A1
Synonyms
Organic cation transporter 1; hOCT1
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Representative Drug(s) Clonidine Drug Info Ki = 550 nM [18]
References  Top
REF 1 Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes. J Med Chem. 2001 Mar 15;44(6):863-72.
REF 2 Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. J Med Chem. 1998 Jun 18;41(13):2243-51.
REF 3 Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J Med Chem. 1995 Sep 1;38(18):3415-44.
REF 4 Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition. J Med Chem. 2004 Oct 21;47(22):5340-6.
REF 5 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues. J Med Chem. 2002 May 23;45(11):2229-39.
REF 6 DrugMatrix in vitro pharmacology data. National Toxicology Program
REF 7 Discovery of trace amine-associated receptor 1 ligands by molecular docking screening against a homology model. Medchemcomm. 2015;6:2216-23.
REF 8 Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716.
REF 9 Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect. ACS Med Chem Lett. 2012 Jun 8;3(7):535-9.
REF 10 From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J Med Chem. 2001 Oct 11;44(21):3378-90.
REF 11 A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2886-90.
REF 12 Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics. J Med Chem. 1980 Sep;23(9):985-90.
REF 13 A convenient synthesis of 2-amino-2-oxazolines and their pharmacological evaluation at cloned human alpha adrenergic receptors. Bioorg Med Chem Lett. 1994 Oct 6;4(19):2317-22.
REF 14 Pharmacological evaluation of UK-14,304 analogs at cloned human alpha adrenergic receptors. Bioorg Med Chem Lett. 1995 Oct 5;5(19):2255-8.
REF 15 QSAR study of imidazoline antihypertensive drugs. Bioorg Med Chem. 2008 Aug 1;16(15):7134-40.
REF 16 Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J Med Chem. 1996 Mar 15;39(6):1193-5.
REF 17 Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist. J Med Chem. 1996 Aug 30;39(18):3533-8.
REF 18 Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61.

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