Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T60693 Target Info
Target Name Opioid receptor kappa (OPRK1)
Synonyms
OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1
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Target Type Successful Target
Gene Name OPRK1
Biochemical Class GPCR rhodopsin
UniProt ID
OPRK_HUMAN
Co-Targets of This Target  Top
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) Carfentanil Drug Info EC50 = 0.0049 nM Click to Show More [1]
2 AIKO-150 Drug Info Ki = 0.19 nM [2]
3 Nalbuphine Drug Info Ki = 0.89 nM [3]
4 Nalfurafine hcl Drug Info EC50 = 1.7 nM [4]
5 LY-2456302 Drug Info Ki = 16.4 nM [6]
6 Enadoline Drug Info Ki = 22 nM [7]
7 Dezocine Drug Info EC50 = 38 nM [9]
8 SALVINORIN A Drug Info Ki ~ 1000 nM [12]
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) Carfentanil Drug Info Ki = 3.28 nM Click to Show More [5]
2 AIKO-150 Drug Info IC50 = 23 nM [8]
3 LY-2456302 Drug Info Ki = 122 nM [6]
4 Nalbuphine Drug Info Ki = 240 nM [3]
5 Nalfurafine hcl Drug Info Ki = 693 nM [10]
6 Enadoline Drug Info Ki ~ 1000 nM [7]
7 BRL-52656 Drug Info Ki = 1000 nM [11]
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 [10]
References  Top
REF 1 Synthesis and mu-Opioid Activity of the Primary Metabolites of Carfentanil. ACS Med Chem Lett. 2019 Oct 16;10(11):1568-1572.
REF 2 Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8.
REF 3 Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid r... J Med Chem. 2007 May 3;50(9):2254-8.
REF 4 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 5 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 6 Development of kappa opioid receptor antagonists. J Med Chem. 2013 Mar 28;56(6):2178-95.
REF 7 Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors. J Med Chem. 2003 Nov 20;46(24):5162-70.
REF 8 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 9 Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1228-32.
REF 10 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 11 (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics. J Med Chem. 1991 Aug;34(8):2624-33.
REF 12 Synthesis of salvinorin A analogues as opioid receptor probes. J Nat Prod. 2006 Jun;69(6):914-8.

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