Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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 | Naloxone | 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 | Morphine | Drug Info | Ki = 6.9 nM | [12] | ||
8 | Carfentanil | Drug Info | Ki = 43.1 nM | [10] | ||
9 | NOCICEPTIN | 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 | Hydrocodone | 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) | Met-enkephalin | 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 | Morphine | Drug Info | EC50 = 15.6 nM | [13] | ||
5 | Naloxone | 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 | NOCICEPTIN | 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) | NOCICEPTIN | 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 | ||||
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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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