Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T58992 Target Info
Target Name Opioid receptor delta (OPRD1)
Synonyms
OPRD; Delta-type opioid receptor; Delta opioid receptor; DOR-1; D-OR-1
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Target Type Successful Target
Gene Name OPRD1
Biochemical Class GPCR rhodopsin
UniProt ID
OPRD_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 Butorphanol Drug Info Ki = 0.12 nM [4]
3 AIKO-150 Drug Info Ki = 0.19 nM [4]
4 Hydromorphone Drug Info Ki = 0.28 nM [5]
5 Loperamide Drug Info Ki = 0.53 nM [6]
6 Eluxadoline Drug Info EC50 = 1 nM [7]
7 Oxycodone Drug Info Ki = 12 nM [8]
8 Met-enkephalin Drug Info IC50 = 13 nM [9]
9 Codeine Drug Info IC50 = 105 nM [12]
10 Codeine Drug Info IC50 = 520 nM [13]
11 SALVINORIN A Drug Info Ki ~ 1000 nM [14]
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) SALVINORIN A Drug Info EC50 = 0.015 nM Click to Show More [2]
2 Butorphanol Drug Info Ki = 0.12 nM [3]
3 AIKO-150 Drug Info Ki = 0.48 nM [4]
4 Hydromorphone Drug Info Ki = 2.8 nM [5]
5 Carfentanil Drug Info Ki = 43.1 nM [11]
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) Loperamide Drug Info IC50 = 33 nM [10]
Co-Target Name Voltage-gated sodium channel alpha Nav1.5 (SCN5A) Successful Target
UniProt ID SCN5A_HUMAN
Gene Name SCN5A
Synonyms
Voltage-gated sodium channel subunit alpha Nav1.5; Sodium channel protein type V subunit alpha; Sodium channel protein type 5 subunit alpha; Sodium channel protein cardiac muscle subunit alpha; HH1
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Representative Drug(s) Loperamide Drug Info IC50 = 239 nM [10]
Co-Target Name Brain sodium channel alpha (Types I, II, III) Co-Target
UniProt ID SCN1A_HUMAN; SCN2A_HUMAN; SCN3A_HUMAN
Gene Name SCN1A; SCN2A; SCN3A
Representative Drug(s) Loperamide Drug Info IC50 = 270 nM [15]
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 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 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 4 Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8.
REF 5 Syntheses of novel high affinity ligands for opioid receptors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94.
REF 6 Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9.
REF 7 Identification of a dual delta OR antagonist/mu OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d). Bioorg Med Chem Lett. 2012 Jul 15;22(14):4869-72.
REF 8 4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual mu-Opioid Receptor Agonists and sigma 1 Receptor Antagonists for the Treatment of Pain. J Med Chem. 2020 Mar 12;63(5):2434-2454.
REF 9 Discovery of Novel Multifunctional Ligands with mu/delta Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain. J Med Chem. 2015 Nov 12;58(21):8573-83.
REF 10 Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K. Bioorg Med Chem Lett. 2018 Feb 1;28(3):446-51.
REF 11 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 12 The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity. J Med Chem. 2003 Jan 2;46(1):34-48.
REF 13 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 14 Synthesis of salvinorin A analogues as opioid receptor probes. J Nat Prod. 2006 Jun;69(6):914-8.
REF 15 [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985 Mar;28(3):381-8.

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