Target family: Opioid receptors (type: gpcr)
Target: &delta; receptor

Ligand: ADL5747 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.569999694824219 pKi
Reference (Journal): Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Published in: J Med Chem

Ligand: ADL5859 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.079999923706055 pKi
Reference (Journal): Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Published in: J Med Chem

Ligand: α-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: alvimopan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008)
Primary target: no
Median affinity: 7.920000076293945 pKi
Reference (Journal): Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.
Published in: Bioorg Med Chem Lett

Ligand: AR-M1000390 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.050000190734863 pIC50
Reference (Patent): Opioid receptor subtype-selective agents.

Ligand: AR-M1000390 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.96999979019165 pKi
Reference (Journal): Pharmacological characterization of AR-M1000390 at human delta opioid receptors.
Published in: Life Sci

Ligand: AT-076 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.710000038146973 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: AT-076 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.710000038146973 pKi
Reference (Journal): Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents.
Published in: Life Sci

Ligand: atoxifent (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.65999984741211 pEC50
Reference (Journal): Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.
Published in: J Med Chem

Ligand: AZD7268 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.520000457763672 pKi
Reference (Webpage): AZD7268 &delta;‐Opioid receptor agonist.

Ligand: β-endorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: β-endorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: β-FNA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: bilorphin (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pKi
Reference (Journal): A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BMS-986187 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pKi

Ligand: BNTX (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Constitutive activity of the delta-opioid receptor expressed in C6 glioma cells: identification of non-peptide delta-inverse agonists.
Published in: Br J Pharmacol

Ligand: BNTX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: BNTX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: (-)-bremazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: BU08028 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mouse models of acute pain and cocaine-induced reward.
Published in: J Pharmacol Exp Ther

Ligand: BW373U86 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.739999771118164 pKi
Reference (Journal): A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.
Published in: J Pharmacol Exp Ther

Ligand: BW373U86 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.489999771118164 pKi
Reference (Journal): Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Published in: J Med Chem

Ligand: carfentanil (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 pKi
Reference (Journal): Molecular determinants of mu receptor recognition for the fentanyl class of compounds.
Published in: Mol Pharmacol

Ligand: cebranopadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pKi
Reference (Journal): Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: compound 16 [PMID: 31498617] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 5.610000133514404 pKi
Reference (Journal): Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.
Published in: J Med Chem

Ligand: CTAP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: (-)-cyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: DADLE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: DADLE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: [D-Ala2]deltorphin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding sites.
Published in: Proc Natl Acad Sci USA

Ligand: deltorphin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: deltorphin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: dihydromorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: diprenorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: DPDPE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: DPDPE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.
Published in: Proc Natl Acad Sci USA

Ligand: DPDPE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: DSLET (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: DSLET (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: DSTBULET (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): [3H][D-Ser2(O-tert-butyl),Leu5]enkephalyl-Thr6 and [D-Ser2(O-tert-butyl),Leu5]enkephalyl-Thr6(O-tert-butyl). Two new enkephalin analogs with both a good selectivity and a high affinity toward delta-opioid binding sites.
Published in: J Biol Chem

Ligand: dynorphin-(1-11) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: dynorphin A-(1-13) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: dynorphin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: eluxadoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 8.890000343322754 pKi
Reference (Journal): Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
Published in: Bioorg Med Chem Lett

Ligand: endomorphin-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Endomorphins fully activate a cloned human mu opioid receptor.
Published in: FEBS Lett

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: etonitazene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: etorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: fentanyl (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1968), EMA (2008)
Median affinity: 6.8 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: hydromorphone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity: 7.420000076293945 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: ICI 174,864 (Peptide)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Constitutive activity of the delta-opioid receptor expressed in C6 glioma cells: identification of non-peptide delta-inverse agonists.
Published in: Br J Pharmacol

Ligand: [Leu]enkephalin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: [Leu]enkephalin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: LY2456302 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.809999942779541 pKi
Reference (Journal): LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders.
Published in: Neuropharmacology

Ligand: [Met]enkephalin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: (-)-methadone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: methylnaltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (2008)
Primary target: no
Median affinity: 6.050000190734863 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: morphine (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
Median affinity: 6.9 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: nalbuphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity: 6.239999771118164 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: naldemedine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2017), EMA (2019)
Primary target: no
Median affinity: 9.039999961853027 pKi
Reference (Journal): Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects.
Published in: Bioorg Med Chem Lett

Ligand: nalmefene (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2013), FDA (2023)
Median affinity: 8.1 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: nalorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Median affinity: 7.4 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Median affinity: 6.2 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Primary target: yes
Median affinity: 7.199999809265137 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Median affinity: 7.8 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: naltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998), UK (2011)
Median affinity: 6.8 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: naltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998), UK (2011)
Primary target: yes
Median affinity: 8 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: naltriben (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: naltriben (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.9 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: naltriben (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKi
Reference (Journal): Differential antagonism of delta opioid agonists by naltrindole and its benzofuran analog (NTB) in mice: evidence for delta opioid receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: naltriben (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 10 pKi
Reference (Journal): Constitutive activity of the delta-opioid receptor expressed in C6 glioma cells: identification of non-peptide delta-inverse agonists.
Published in: Br J Pharmacol

Ligand: naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.7 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): Naltrindole, a highly selective and potent non-peptide delta opioid receptor antagonist.
Published in: Eur J Pharmacol

Ligand: NFP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pKi
Reference (Journal): Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands.
Published in: J Med Chem

Ligand: NMRA-140 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.190000057220459 pIC50
Reference (Journal): Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).
Published in: J Med Chem

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: normorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: oxycodegol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.380000114440918 pKi
Reference (Journal): NKTR-181: A Novel Mu-Opioid Analgesic with Inherently Low Abuse Potential.
Published in: J Pharmacol Exp Ther

Ligand: (-)-pentazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity: 7.3 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: pethidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1942)
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.
Published in: J Med Chem

Ligand: PN6047 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.25 pKi
Reference (Journal): A Novel G Protein-Biased Agonist at the <i>δ</i> Opioid Receptor with Analgesic Efficacy in Models of Chronic Pain.
Published in: J Pharmacol Exp Ther

Ligand: quadazocine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: samidorphan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2021)
Primary target: no
Median affinity: 8.59000015258789 pKi
Reference (Journal): Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
Published in: Bioorg Med Chem Lett

Ligand: SCH221510 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.539999961853027 pKi
Reference (Journal): The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510).
Published in: J Pharmacol Exp Ther

Ligand: SNC80 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pKi
Reference (Journal): Relative efficacies of delta-opioid receptor agonists at the cloned human delta-opioid receptor.
Published in: Eur J Pharmacol

Ligand: SNC80 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pKi
Reference (Journal): Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
Published in: J Med Chem

Ligand: SRI22141 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pKi
Reference (Journal): A Novel Mu-Delta Opioid Agonist Demonstrates Enhanced Efficacy With Reduced Tolerance and Dependence in Mouse Neuropathic Pain Models.
Published in: J Pain

Ligand: SRI22141 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pEC50
Reference (Journal): A Novel Mu-Delta Opioid Agonist Demonstrates Enhanced Efficacy With Reduced Tolerance and Dependence in Mouse Neuropathic Pain Models.
Published in: J Pain

Ligand: [3H][D-Ala2]deltorphin I (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.350000381469727 pKd
Reference (Journal): [D-Ala2]deltorphin I binding and pharmacological evidence for a special subtype of delta opioid receptor on human and invertebrate immune cells.
Published in: Proc Natl Acad Sci USA

Ligand: [3H]deltorphin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [3H]deltorphin II.
Published in: Life Sci

Ligand: [3H]diprenorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): Specific reduction of delta-opioid receptor binding in transfected NG108-15 cells.
Published in: J Biol Chem

Ligand: [3H]diprenorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: [3H]DPDPE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKd
Reference (Journal): Characterization of [3H][2-D-penicillamine, 5-D-penicillamine]-enkephalin binding to delta opiate receptors in the rat brain and neuroblastoma--glioma hybrid cell line (NG 108-15).
Published in: Proc Natl Acad Sci USA

Ligand: [3H]naltriben (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Selective in vivo binding of [3H]naltriben to delta-opioid receptors in mouse brain.
Published in: Eur J Pharmacol

Ligand: [3H]naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.430000305175781 pKd
Reference (Journal): Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain.
Published in: Life Sci

Ligand: TAN-67 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 pIC50
Reference (Journal): Synthesis of optically active TAN-67, a highly selective delta opioid receptor agonist, and investigation of its pharmacological properties.
Published in: Drug Des Discov

Ligand: TIPPψ (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.
Published in: J Med Chem

Ligand: TIPPψ (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Published in: NIDA Res Monogr

Ligand: tramadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995), UK (2003)
Primary target: no
Median affinity: 8.029999732971191 pKi
Reference (Journal): Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Published in: Bioorg Med Chem Lett

Ligand: UFP-505 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.819999694824219 pKi
Reference (Journal): Pharmacological characterization of the bifunctional opioid ligand H-Dmt-Tic-Gly-NH-Bzl (UFP-505).
Published in: Br J Anaesth

Ligand: UFP-505 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.819999694824219 pKi
Reference (Journal): In vitro and in vivo characterization of the bifunctional μ and δ opioid receptor ligand UFP-505.
Published in: Br J Pharmacol

Ligand: UFP-512 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 10.199999809265137 pKi
Reference (Journal): Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonist.
Published in: Peptides

Ligand: zyklophin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): [Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the &quot;address&quot; domain is a novel kappa-opioid receptor antagonist.
Published in: J Med Chem