Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T47768 Target Info
Target Name Opioid receptor mu (MOP)
Synonyms
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Target Type Successful Target
Gene Name OPRM1
Biochemical Class GPCR rhodopsin
UniProt ID
OPRM_HUMAN
Co-Targets of This Target  Top
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) Nalfurafine hcl Drug Info EC50 = 0.0082 nM Click to Show More [1]
2 SALVINORIN A Drug Info EC50 = 0.015 nM [2]
3 Buprenorphine Drug Info Ki = 0.04 nM [3]
4 Drug Info Ki = 0.25 nM [4]
5 AIKO-150 Drug Info Ki = 0.48 nM [6]
6 Hydromorphone Drug Info Ki = 2.8 nM [9]
7 Drug Info Ki = 6.9 nM [12]
8 Carfentanil Drug Info Ki = 43.1 nM [10]
9 Drug Info EC50 = 78.5 nM [17]
10 Alvimopan Drug Info Ki = 100 nM [18]
11 Fentanyl Drug Info Ki = 196.5 nM [10]
12 Drug Info Ki = 260 nM [20]
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) Vanoxerine Drug Info Ki = 0.36 nM [5]
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) Vanoxerine Drug Info IC50 = 1 nM Click to Show More [7]
2 Fentanyl Drug Info IC50 = 354 nM [21]
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) Drug Info EC50 = 1.03 nM Click to Show More [8]
2 Carfentanil Drug Info Ki = 3.28 nM [10]
3 Alvimopan Drug Info Ki = 5.012 nM [11]
4 Drug Info EC50 = 15.6 nM [13]
5 Drug Info Ki = 19 nM [14]
6 AIKO-150 Drug Info IC50 = 23 nM [15]
7 Hydromorphone Drug Info Ki = 38 nM [9]
8 Fentanyl Drug Info IC50 = 187 nM [19]
9 Methylnaltrexone bromide Drug Info Ki = 501.19 nM [22]
10 Nalfurafine hcl Drug Info Ki = 693 nM [23]
11 Drug Info Ki ~ 1000 nM [24]
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) Vanoxerine Drug Info IC50 = 73 nM [16]
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) Vanoxerine Drug Info IC50 = 79 nM [16]
Co-Target Name Nociceptin receptor (OPRL1) Clinical trial Target
UniProt ID OPRX_HUMAN
Gene Name OPRL1
Synonyms
Orphanin FQ receptor; Opioid-receptor-like 1; Opioid receptor like-1 receptor; Opioid receptor 4; ORL-1 receptor; ORL-1; OPRL1; OP(4); Kappa-type 3 opioid receptor; KOR-3
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Representative Drug(s) Drug Info Ki = 0.04898 nM Click to Show More [25]
2 GRT-6005 Drug Info Ki = 0.9 nM [26]
Co-Target Name Orexin receptor type 1 (HCRTR1) Clinical trial Target
UniProt ID OX1R_HUMAN
Gene Name HCRTR1
Synonyms
Ox1r; Ox1-R; Ox-1-R; Orexin-1 receptor; Hypocretin receptor type 1; HFGAN72 receptor; 7-transmembrane G-protein coupledneuropeptide receptor
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Representative Drug(s) Nalfurafine hcl Drug Info Ki = 250 nM [23]
References  Top
REF 1 Discovery of highly selective kappa-opioid receptor agonists: 10alpha-Hydroxy TRK-820 derivatives. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3920-4.
REF 2 Development of Novel Quinoxaline-Based kappa-Opioid Receptor Agonists for the Treatment of Neuroinflammation. J Med Chem. 2019 Jan 24;62(2):893-907.
REF 3 Selective kappa opioid antagonists for treatment of addiction, are we there yet?. Eur J Med Chem. 2017 Dec 1;141:632-47.
REF 4 Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for kappa, mu, and delta opioid receptors. Bioorg Med Chem. 2011 May 1;19(9):2808-16.
REF 5 Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography. J Med Chem. 2000 Feb 24;43(4):639-48.
REF 6 Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8.
REF 7 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 8 Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5.
REF 9 Syntheses of novel high affinity ligands for opioid receptors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94.
REF 10 Subramanian G, Paterlini MG, Portoghese PS, Ferguson DM: Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor. J Med Chem. 2000 Feb 10;43(3):381-91.
REF 11 Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of mu-opioid receptor antagonists. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2926-30.
REF 12 Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton. Bioorg Med Chem Lett. 2010 Jan 1;20(1):418-21.
REF 13 Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies. J Med Chem. 2011 Feb 24;54(4):980-8.
REF 14 Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. J Med Chem. 1994 Sep 16;37(19):3121-7.
REF 15 Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol. J Med Chem. 1992 Jun 26;35(13):2374-84.
REF 16 Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter. J Med Chem. 2002 Sep 12;45(19):4371-4.
REF 17 Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. J Med Chem. 2011 Oct 13;54(19):6531-7.
REF 18 Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12.
REF 19 Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs. Bioorg Med Chem Lett. 1995 Jun 8;5(11):1177-82.
REF 20 Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. J Med Chem. 2012 Apr 26;55(8):3878-90.
REF 21 Affinity of fentanyl and its derivatives for the sigma 1-receptor. Med. Chem. Commun. 2019;10:1187-1191.
REF 22 Discovery of Axelopran (TD-1211): A Peripherally Restricted mu-Opioid Receptor Antagonist. ACS Med Chem Lett. 2019 Nov 26;10(12):1641-1647.
REF 23 Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies. J Med Chem. 2017 Feb 9;60(3):1018-40.
REF 24 Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug. J Med Chem. 2009 Feb 12;52(3):610-25.
REF 25 N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands. J Med Chem. 2005 Mar 10;48(5):1421-7.
REF 26 Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. J Med Chem. 2016 Aug 11;59(15):7011-28.

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