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

Ligand: 2F-MT-45 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): Activation of μ-opioid receptors by MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) and its fluorinated derivatives.
Published in: Br J Pharmacol

Ligand: 3F-MT-45 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.210000038146973 pEC50
Reference (Journal): Activation of μ-opioid receptors by MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) and its fluorinated derivatives.
Published in: Br J Pharmacol

Ligand: 4F-MT-45 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pEC50
Reference (Journal): Activation of μ-opioid receptors by MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) and its fluorinated derivatives.
Published in: Br J Pharmacol

Ligand: ADL5747 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 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: no
Median affinity: 7.489999771118164 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: alvimopan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008)
Primary target: yes
Median affinity: 9.329999923706055 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: no
Median affinity: 5.420000076293945 pIC50
Reference (Patent): Opioid receptor subtype-selective agents.

Ligand: AT-076 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.779999732971191 pKi
Reference (Journal): Discovery of the first small-molecule opioid pan antagonist with nanomolar affinity at mu, delta, kappa, and nociceptin opioid receptors.
Published in: ACS Chem Neurosci

Ligand: AT-076 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.779999732971191 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: atoxifent (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.40999984741211 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: 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: 9.5 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: 9.5 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: bilorphin (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.960000038146973 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-986121 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BMS-986121 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pKB
Reference (Journal): Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BMS-986122 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKB
Reference (Journal): Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BMS-986122 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pEC50
Reference (Journal): Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BMS-986123 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Primary target: no
Median affinity: 6 pKB
Reference (Journal): Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BMS-986124 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pKB
Reference (Journal): Discovery of positive allosteric modulators and silent allosteric modulators of 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: 7.199999809265137 pKi
Reference (Journal): Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors.
Published in: Mol Pharmacol

Ligand: BNTX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: (-)-bremazocine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 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: brorphine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.319999694824219 pEC50
Reference (Journal): Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.
Published in: J Med Chem

Ligand: brorphine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.6899995803833 pEC50
Reference (Journal): Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide.
Published in: Drug Alcohol Depend

Ligand: brorphine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pKi
Reference (Journal): Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide.
Published in: Drug Alcohol Depend

Ligand: BU08028 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.670000076293945 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: BU72 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.819999694824219 pIC50
Reference (Journal): Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: high affinity opioid agonists
Published in: Bioorg Med Chem Lett

Ligand: buprenorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1981), EMA (2006)
Primary target: yes
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: butorphanol (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: yes
Median affinity: 9.920000076293945 pKi
Reference (Journal): Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: BW373U86 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 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: no
Median affinity: 6.590000152587891 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: 10.619999885559082 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: 8.619999885559082 pKi
Reference (Journal): Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: cebranopadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pKi
Reference (Journal): Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: codeine (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 2009)
Primary target: yes
Median affinity: 6.900000095367432 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: compound 16 [PMID: 31498617] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 5.429999828338623 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: compound 3 [PMID: 23134120] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.079999923706055 pKi
Reference (Journal): Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Published in: J Med Chem

Ligand: CTAP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Potent morphiceptin analogs: structure activity relationships and morphine-like activities.
Published in: J Pharmacol Exp Ther

Ligand: CTOP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors.
Published in: Life Sci

Ligand: CTOP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: (-)-cyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: 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: DADLE (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: DAMGO (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: DAMGO (Peptide)
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: DAMGO (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): Analogues of beta-LPH61-64 possessing selective agonist activity at mu-opiate receptors.
Published in: Eur J Pharmacol

Ligand: DC 128.1 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.25 pKi
Reference (Journal): A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.
Published in: Molecules

Ligand: DC-1-76.1 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.720000267028809 pKi
Reference (Journal): A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.
Published in: Molecules

Ligand: DC-1-76.2 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.
Published in: Molecules

Ligand: DC-1-90.2 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.739999771118164 pKi
Reference (Journal): A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists.
Published in: Molecules

Ligand: dihydromorphine (Synthetic organic)
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: diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.1 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: DSLET (Peptide)
Interaction type: Agonist
Action: Full agonist
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: dynorphin-(1-11) (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: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
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: dynorphin A-(1-13) (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: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Full 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: 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: EG-1-203 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9.020000457763672 pEC50
Reference (Journal): G-Protein biased opioid agonists: 3-hydroxy-<i>N</i>-phenethyl-5-phenylmorphans with three-carbon chain substituents at C9.
Published in: RSC Med Chem

Ligand: EG-1-230 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pKi
Reference (Journal): Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
Published in: J Med Chem

Ligand: eluxadoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 8.770000457763672 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: eluxadoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 9.050000190734863 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
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): Endomorphins fully activate a cloned human mu opioid receptor.
Published in: FEBS Lett

Ligand: endomorphin-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): A potent and selective endogenous agonist for the mu-opiate receptor.
Published in: Nature

Ligand: endomorphin-2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): A potent and selective endogenous agonist for the mu-opiate receptor.
Published in: Nature

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 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: etonitazene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.180000305175781 pKi
Reference (Journal): Alkoxy chain length governs the potency of 2-benzylbenzimidazole 'nitazene' opioids associated with human overdose.
Published in: Psychopharmacology (Berl)

Ligand: etonitazene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.520000457763672 pEC50
Reference (Journal): Alkoxy chain length governs the potency of 2-benzylbenzimidazole 'nitazene' opioids associated with human overdose.
Published in: Psychopharmacology (Berl)

Ligand: etonitazene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 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: 9.5 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: EWB-3-14 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pKi
Reference (Journal): Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
Published in: J Med Chem

Ligand: fentanyl (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1968), EMA (2008)
Primary target: yes
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: fentanyl (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1968), EMA (2008)
Median affinity: 9.4 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: GSK1521498 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.380000114440918 pKi
Reference (Journal): The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours.
Published in: Psychopharmacology (Berl.)

Ligand: HS665 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.269999980926514 pKi
Reference (Journal): Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Published in: J Med Chem

Ligand: hydrocodone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (no approval history prior to 2013)
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
Published in: J Med Chem

Ligand: hydromorphone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: yes
Median affinity: 9.550000190734863 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: ICI-199441 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.28000020980835 pKi
Reference (Journal): Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Published in: Bioorg Med Chem Lett

Ligand: isotonitazene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pEC50
Reference (Journal): Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide.
Published in: Drug Alcohol Depend

Ligand: isotonitazene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.949999809265137 pKi
Reference (Journal): Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide.
Published in: Drug Alcohol Depend

Ligand: [Leu]enkephalin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
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: levallorphan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Generation of novel radiolabeled opiates through site-selective iodination.
Published in: Bioorg Med Chem Lett

Ligand: levorphanol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: yes
Median affinity: 9.890000343322754 pIC50
Reference (Journal): The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.
Published in: J Med Chem

Ligand: loperamide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity: 9.279999732971191 pKi
Reference (Journal): Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Published in: Bioorg Med Chem Lett

Ligand: LY2456302 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 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: 9.2 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: (-)-methadone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 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: methadone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1947, prior history not available)
Primary target: yes
Median affinity: 8.390000343322754 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: methylnaltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (2008)
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: mitragynine (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pEC50
Reference (Journal): A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.
Published in: J Med Chem

Ligand: mitragynine (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.690000057220459 pEC50
Reference (Journal): Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit &#x3b2;-Arrestin-2.
Published in: J Med Chem

Ligand: morphine (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
Primary target: yes
Median affinity: 9 pKi
Reference (Journal): Multiple opioid receptors: ligand selectivity profiles and binding site signatures.
Published in: Mol Pharmacol

Ligand: morphine (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
Primary target: yes
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: morphine (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
Median affinity: 7.9 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: MT-45 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.639999866485596 pEC50
Reference (Journal): Activation of μ-opioid receptors by MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) and its fluorinated derivatives.
Published in: Br J Pharmacol

Ligand: nalbuphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity: 8.800000190734863 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: yes
Median affinity: 8.949999809265137 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: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2013), FDA (2023)
Primary target: yes
Median affinity: 9.5 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: nalorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.899999618530273 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: naloxonazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.3 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Primary target: no
Median affinity: 8.899999618530273 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: 9 pKi
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: naloxone benzoylhydrazone (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: naloxone benzoylhydrazone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: naltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998), UK (2011)
Primary target: yes
Median affinity:  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: naltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998), UK (2011)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours.
Published in: Psychopharmacology (Berl.)

Ligand: naltriben (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: naltrindole (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: NFP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.4399995803833 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: 6.960000038146973 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: 7.7 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: normorphine (Synthetic organic)
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: oxycodegol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.630000114440918 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: Partial agonist
Ligand approved: yes
Approval source: FDA (1967)
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: pethidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1942)
Primary target: yes
Median affinity: 6.5 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: PL017 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 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: PL017 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Potent morphiceptin analogs: structure activity relationships and morphine-like activities.
Published in: J Pharmacol Exp Ther

Ligand: PZM21 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.34000015258789 pEC50
Reference (Journal): Structure-based discovery of opioid analgesics with reduced side effects.
Published in: Nature

Ligand: PZM21 (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.960000038146973 pKi
Reference (Journal): Structure-based discovery of opioid analgesics with reduced side effects.
Published in: Nature

Ligand: quadazocine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: 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: samidorphan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2021)
Primary target: no
Median affinity: 10.279999732971191 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: 7.190000057220459 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: SR16835 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKi
Reference (Journal): Comparison of the antinociceptive and antirewarding profiles of novel bifunctional nociceptin receptor/mu-opioid receptor ligands: implications for therapeutic applications.
Published in: J Pharmacol Exp Ther

Ligand: SRI22141 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 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: SRI22141 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.710000038146973 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: sufentanil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1984), EMA (2015)
Primary target: yes
Median affinity: 9.899999618530273 pKi
Reference (Journal): Uniform assessment and ranking of opioid μ receptor binding constants for selected opioid drugs.
Published in: Regul Toxicol Pharmacol

Ligand: sufentanil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1984), EMA (2015)
Median affinity: 9.1 pKi
Reference (Journal): Comparative binding of mu and delta selective ligands in whole brain and pons/medulla homogenates from rat: affinity profiles of fentanyl derivatives.
Published in: Neuropharmacology

Ligand: [3H]CTOP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Mu-opioid receptor binding in intact SH-SY5Y neuroblastoma cells.
Published in: Eur J Pharmacol

Ligand: [3H]DAMGO (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKd
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: [3H]diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKd
Reference (Journal): Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Published in: Mol Pharmacol

Ligand: [3H]naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Agonist-induced functional desensitization of the mu-opioid receptor is mediated by loss of membrane receptors rather than uncoupling from G protein.
Published in: Mol Pharmacol

Ligand: [3H]PL017 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Autoradiographic localization of [3H] [MePhe3,D-Pro4]morphiceptin ([3H]PL017) to mu opioid receptors in rat brain.
Published in: Eur J Pharmacol

Ligand: tapentadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008)
Primary target: yes
Median affinity: 6.800000190734863 pKi
Reference (Journal): (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties.
Published in: J Pharmacol Exp Ther

Ligand: thebaine (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.25 pEC50
Reference (Journal): Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.
Published in: J Biol Chem

Ligand: tramadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995), UK (2003)
Primary target: no
Median affinity: 5.800000190734863 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: U-47700 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor.
Published in: J Med Chem

Ligand: UFP-505 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.789999961853027 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: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.789999961853027 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: no
Median affinity: 8 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: 5.230000019073486 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