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

Ligand: 5'-guanidinonaltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: 5'-guanidinonaltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.
Published in: J Med Chem

Ligand: 5'-guanidinonaltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist.
Published in: Eur J Pharmacol

Ligand: ADL5747 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 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: 7.429999828338623 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:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: α-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: α-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a human kappa opioid receptor from the brain.
Published in: Life Sci

Ligand: α-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: α-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a rat kappa opioid receptor.
Published in: Biochem J

Ligand: alvimopan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008)
Primary target: no
Median affinity: 7 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: 5.130000114440918 pIC50
Reference (Patent): Opioid receptor subtype-selective agents.

Ligand: asimadoline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists
Published in: Bioorg Med Chem Lett

Ligand: AT-076 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.9399995803833 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: 8.9399995803833 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: β-endorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: β-endorphin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
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: β-endorphin (Peptide)
Interaction type: Agonist
Action: Partial 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: β-endorphin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: β-FNA (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: β-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: β-neoendorphin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: bilorphin (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.110000133514404 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: 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: (-)-bremazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: (-)-bremazocine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 10.5 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: BU08028 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.25 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: buprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981), EMA (2006)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: buprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981), EMA (2006)
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: 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: 7.46999979019165 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: 6.889999866485596 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: 7.369999885559082 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: 7.190000057220459 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: 8.59000015258789 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: 4.920000076293945 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: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.229999542236328 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: compound 3 [PMID: 23134120] (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pEC50
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: (-)-cyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
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: [D-Ala2,F5,Phe4]dynorphin-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: [D-Ala2,F5,Phe4]dynorphin-(1-17)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: DAMGO (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.5 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: DAMGO (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: difelikefalin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2021), EMA (2022)
Primary target: yes
Median affinity: 9.800000190734863 pEC50
Reference (Patent): Synthetic peptide amides.

Ligand: difelikefalin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2021), EMA (2022)
Primary target: no
Median affinity: 10.319999694824219 pEC50
Reference (Patent): Synthetic peptide amides.

Ligand: dihydromorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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: diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a human kappa opioid receptor from the brain.
Published in: Life Sci

Ligand: dynorphin-(1-11) (Peptide)
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: dynorphin-(1-17)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
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: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a rat kappa opioid receptor.
Published in: Biochem J

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of a human kappa opioid receptor from the brain.
Published in: Life Sci

Ligand: dynorphin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A-(1-13) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.9 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A-(1-13) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: dynorphin A-(1-13) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
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: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
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: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: dynorphin A-(1-8) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.
Published in: J Med Chem

Ligand: dynorphin B (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: dynorphin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: dynorphin B (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
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: dynorphin B (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: E2078 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Opioid efficacy in a C6 glioma cell line stably expressing the human kappa opioid receptor.
Published in: J Pharmacol Exp Ther

Ligand: E2078 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: enadoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Published in: J Med Chem

Ligand: enadoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): CI-977, a novel and selective agonist for the kappa-opioid receptor.
Published in: Br J Pharmacol

Ligand: enadoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Radioligand-dependent discrepancy in agonist affinities enhanced by mutations in the kappa-opioid receptor.
Published in: Mol Pharmacol

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKd
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKd
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: 8.8 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: ethylketocyclazocine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: etonitazene (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: etorphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: fentanyl (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1968), EMA (2008)
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: GR 89696 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pKi
Reference (Journal): [(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers.
Published in: Nucl Med Biol

Ligand: HS665 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.3100004196167 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: HS665 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.4399995803833 pEC50
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: no
Median affinity: 6.590000152587891 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: no
Median affinity: 8.550000190734863 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: 10.399999618530273 pKi
Reference (Journal): Amino acid conjugates as kappa opioid receptor agonists.
Published in: Bioorg Med Chem Lett

Ligand: ICI 204448 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: ICI 204448 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: JDTic (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  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: JDTic (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 11.220000267028809 pKi
Reference (Journal): Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Published in: J Med Chem

Ligand: JDTic (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters.
Published in: PLoS ONE

Ligand: JDTic (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Published in: J Med Chem

Ligand: [Leu]enkephalin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: LY2456302 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.09000015258789 pKB
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: LY2456302 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9.09000015258789 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: 6 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: (-)-methadone (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.5 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: methylnaltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (2008)
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: [Met5]dynorphin-(1-17) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: morphine (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
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: morphine (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: morphine (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1984), prior history not available
Median affinity:  pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: MP1104 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.479999542236328 pKi
Reference (Journal): Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor.
Published in: Cell

Ligand: nalbuphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: nalbuphine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1979)
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: nalfurafine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.1 pKd
Reference (Journal): Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
Published in: J Pharmacol Exp Ther

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: Agonist
Action: Partial agonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: nalorphine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: 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: (+)-naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.7 pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
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)
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a rat kappa opioid receptor.
Published in: Biochem J

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Cloning of a human kappa opioid receptor from the brain.
Published in: Life Sci

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Primary target: yes
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
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:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: naloxone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1971), EMA (2017)
Median affinity: 8.3 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:  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)
Primary target: yes
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
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)
Median affinity:  pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: naloxone benzoylhydrazone (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
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: 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): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: naltrexone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998), UK (2011)
Median affinity: 9.2 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: 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 (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: naltriben (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: naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: naltrindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Molecular cloning and expression of a rat kappa opioid receptor.
Published in: Biochem J

Ligand: NFP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.319999694824219 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: yes
Median affinity: 9.100000381469727 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
Primary target: no
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 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
Primary target: no
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
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: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
Published in: J Med Chem

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a rat kappa opioid receptor.
Published in: Biochem J

Ligand: nor-binaltorphimine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning of a human kappa opioid receptor from the brain.
Published in: Life Sci

Ligand: normorphine (Synthetic organic)
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: (-)-pentazocine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1967)
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: (-)-pentazocine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: pethidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1942)
Primary target: no
Median affinity: 5.630000114440918 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: probe 1.1 [PMID: 24187130] (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pEC50
Reference (Journal): Development of functionally selective, small molecule agonists at kappa opioid receptors.
Published in: J Biol Chem

Ligand: probe 1.1 [PMID: 24187130] (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 5.380000114440918 pEC50
Reference (Journal): Development of functionally selective, small molecule agonists at kappa opioid receptors.
Published in: J Biol Chem

Ligand: probe 1.1 [PMID: 24187130] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Development of functionally selective, small molecule agonists at kappa opioid receptors.
Published in: J Biol Chem

Ligand: probe 2.1 [PMID: 24187130] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.460000038146973 pKi
Reference (Journal): Development of functionally selective, small molecule agonists at kappa opioid receptors.
Published in: J Biol Chem

Ligand: probe 2.1 [PMID: 24187130] (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.070000171661377 pEC50
Reference (Journal): Development of functionally selective, small molecule agonists at kappa opioid receptors.
Published in: J Biol Chem

Ligand: probe 2.1 [PMID: 24187130] (Synthetic organic)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Development of functionally selective, small molecule agonists at kappa opioid receptors.
Published in: J Biol Chem

Ligand: quadazocine (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: salvinorin A (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Published in: Bioorg Med Chem Lett

Ligand: salvinorin A (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Published in: Proc Natl Acad Sci USA

Ligand: samidorphan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2021)
Primary target: no
Median affinity: 9.640000343322754 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: 6.880000114440918 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: spiradoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: spiradoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: SR16835 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.170000076293945 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: [3H]diprenorphine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
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: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: [3H]enadoline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Analysis of [3H]bremazocine binding in single and combinatorial opioid receptor knockout mice.
Published in: Eur J Pharmacol

Ligand: [3H]U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: [3H]U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: [3H]U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [3H]U-69593 a highly selective ligand for the opioid kappa receptor.
Published in: Eur J Pharmacol

Ligand: tifluadom (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: tramadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995), UK (2003)
Primary target: no
Median affinity: 7.849999904632568 pKi
Reference (Journal): Syntheses of novel high affinity ligands for opioid receptors.
Published in: Bioorg Med Chem Lett

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Salvinorin A, an active component of the hallucinogenic sage salvia divinorum is a highly efficacious kappa-opioid receptor agonist: structural and functional considerations.
Published in: J Pharmacol Exp Ther

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and expression of a rat kappa opioid receptor.
Published in: Biochem J

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning of a human kappa opioid receptor from the brain.
Published in: Life Sci

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Book): Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.
Published in: The Delta Receptor

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
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: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Published in: J Pharmacol Exp Ther

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
Published in: Proc Natl Acad Sci USA

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): U-50,488: a selective and structurally novel non-Mu (kappa) opioid agonist.
Published in: J Pharmacol Exp Ther

Ligand: U50488 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pKi
Reference (Journal): [3H]U-69593 a highly selective ligand for the opioid kappa receptor.
Published in: Eur J Pharmacol

Ligand: U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors.
Published in: Biochem J

Ligand: U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a rat kappa opioid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: U69593 (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: U69593 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
Published in: Proc Natl Acad Sci USA

Ligand: UFP-512 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 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: yes
Median affinity: 7.519999980926514 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

Ligand: zyklophin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.079999923706055 pKB
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