Target family: Opioid receptors (type: gpcr)
Target: NOP receptor

Ligand: Ac-RYYRIK-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone-inducible mammalian expression system.
Published in: Br J Pharmacol

Ligand: Ac-RYYRIK-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: Ac-RYYRIK-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pEC50
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: Ac-RYYRIK-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: Ac-RYYRWK-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: Ac-RYYRWK-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.680000305175781 pEC50
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: Ac-RYYRWK-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: Ac-RYYRWK-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone-inducible mammalian expression system.
Published in: Br J Pharmacol

Ligand: [Arg14Lys15]N/OFQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Highly potent nociceptin analog containing the Arg-Lys triple repeat.
Published in: Biochem Biophys Res Commun

Ligand: AT-076 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.760000228881836 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-403 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pKi
Reference (Journal): Anti-Parkinsonian and anti-dyskinetic profiles of two novel potent and selective nociceptin/orphanin FQ receptor agonists.
Published in: Br J Pharmacol

Ligand: BU08028 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 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: cebranopadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 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 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: 7.889999866485596 pEC50
Reference (Journal): Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: compound 24 [PMID: 16451050] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24.
Published in: Eur J Pharmacol

Ligand: compound 24 [PMID: 16451050] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.619999885559082 pKi
Reference (Journal): Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24.
Published in: Eur J Pharmacol

Ligand: compound 24 [PMID: 16451050] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
Published in: J Med Chem

Ligand: [F/G]N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone-inducible mammalian expression system.
Published in: Br J Pharmacol

Ligand: J-113397 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: J-113397 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).
Published in: J Med Chem

Ligand: JTC-801 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
Published in: J Med Chem

Ligand: LY2940094 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKi
Reference (Journal): Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.
Published in: J Med Chem

Ligand: LY2940094 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKi
Reference (Journal): Detailed In Vitro Pharmacological Characterization of the Clinically Viable Nociceptin/Orphanin FQ Peptide Receptor Antagonist BTRX-246040.
Published in: J Pharmacol Exp Ther

Ligand: MCOPPB (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.40999984741211 pEC50
Reference (Journal): Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug.
Published in: J Med Chem

Ligand: MCOPPB (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.069999694824219 pKi
Reference (Journal): Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug.
Published in: J Med Chem

Ligand: NiK-21273 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.380000114440918 pKB
Reference (Journal): Acute and chronic antiparkinsonian effects of the novel nociceptin/orphanin FQ receptor antagonist NiK-21273 in comparison with SB-612111.
Published in: Br J Pharmacol

Ligand: nociceptin/orphanin FQ (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: nociceptin/orphanin FQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: nociceptin/orphanin FQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the effects of [Phe1psi(CH2-NH)Gly2]nociceptin(1-13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors.
Published in: Br J Pharmacol

Ligand: nociceptin/orphanin FQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Relationship between binding affinity and functional activity of nociceptin/orphanin FQ.
Published in: Neuropeptides

Ligand: nociceptin/orphanin FQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone-inducible mammalian expression system.
Published in: Br J Pharmacol

Ligand: N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide.
Published in: J Med Chem

Ligand: N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the effects of [Phe1psi(CH2-NH)Gly2]nociceptin(1-13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors.
Published in: Br J Pharmacol

Ligand: N/OFQ-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.4 pKi
Reference (Journal): Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone-inducible mammalian expression system.
Published in: Br J Pharmacol

Ligand: [Nphe1]N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor.
Published in: Br J Pharmacol

Ligand: peptide III-BTD (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Ligands for kappa-opioid and ORL1 receptors identified from a conformationally constrained peptide combinatorial library.
Published in: J Biol Chem

Ligand: [(pF)Phe4]N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [(pF)Phe4]N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
Published in: J Med Chem

Ligand: [(pF)Phe4]N/OFQ-(1-13)-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.119999885559082 pEC50
Reference (Journal): N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
Published in: J Med Chem

Ligand: PWT2-N/OFQ (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pEC50
Reference (Journal): In vitro and in vivo pharmacological characterization of nociceptin/orphanin FQ tetrabranched derivatives.
Published in: Br J Pharmacol

Ligand: PWT2-N/OFQ (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pKi
Reference (Journal): In vitro and in vivo pharmacological characterization of nociceptin/orphanin FQ tetrabranched derivatives.
Published in: Br J Pharmacol

Ligand: Ro64-6198 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.40999984741211 pKi
Reference (Journal): Synthesis of (1S,3aS)-8-(2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4. 5]decan-4-one, a potent and selective orphanin FQ (OFQ) receptor agonist with anxiolytic-like properties.
Published in: Eur J Med Chem

Ligand: Ro64-6198 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.409999847412109 pEC50
Reference (Journal): Synthesis of (1S,3aS)-8-(2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4. 5]decan-4-one, a potent and selective orphanin FQ (OFQ) receptor agonist with anxiolytic-like properties.
Published in: Eur J Med Chem

Ligand: Ro64-6198 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.40999984741211 pKi
Reference (Journal): A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat.
Published in: Proc Natl Acad Sci USA

Ligand: (R)-Ro65-6570 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.
Published in: Bioorg Med Chem Lett

Ligand: (R)-Ro65-6570 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pEC50
Reference (Journal): 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.
Published in: Bioorg Med Chem Lett

Ligand: SB 612111 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).
Published in: J Pharmacol Exp Ther

Ligand: SB 612111 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).
Published in: J Pharmacol Exp Ther

Ligand: SB 612111 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: in vitro studies.
Published in: J Pharmacol Exp Ther

Ligand: SB 612111 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: in vitro studies.
Published in: J Pharmacol Exp Ther

Ligand: SCH221510 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pEC50
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: SCH221510 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 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: SCH221510 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.9399995803833 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: SCH221510 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.380000114440918 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: SCH486757 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.34000015258789 pKi
Reference (Journal): Pharmacological profile of the NOP agonist and cough suppressing agent SCH 486757 (8-[Bis(2-Chlorophenyl)Methyl]-3-(2-Pyrimidinyl)-8-Azabicyclo[3.2.1]Octan-3-Ol) in preclinical models.
Published in: Eur J Pharmacol

Ligand: SCH486757 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): Pharmacological profile of the NOP agonist and cough suppressing agent SCH 486757 (8-[Bis(2-Chlorophenyl)Methyl]-3-(2-Pyrimidinyl)-8-Azabicyclo[3.2.1]Octan-3-Ol) in preclinical models.
Published in: Eur J Pharmacol

Ligand: SR16835 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.340000152587891 pEC50
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: SR16835 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.940000057220459 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]Leu-N/OFQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.199999809265137 pKd
Reference (Journal): Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone-inducible mammalian expression system.
Published in: Br J Pharmacol

Ligand: [3H]N/OFQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Replacement of Gln280 by His in TM6 of the human ORL1 receptor increases affinity but reduces intrinsic activity of opioids.
Published in: FEBS Lett

Ligand: [3H]N/OFQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
Published in: J Pharmacol Exp Ther

Ligand: [3H]Tyr14-N/OFQ (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Relationship between binding affinity and functional activity of nociceptin/orphanin FQ.
Published in: Neuropeptides

Ligand: TRAP-101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.75 pA2
Reference (Journal): Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist.
Published in: Bioorg Med Chem

Ligand: UFP-101 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.199999809265137 pKi
Reference (Journal): [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor.
Published in: Br J Pharmacol

Ligand: UFP-102 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.7 pKd
Reference (Journal): [(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.
Published in: J Pharmacol Exp Ther

Ligand: UFP-112 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): In vitro and in vivo studies on UFP-112, a novel potent and long lasting agonist selective for the nociceptin/orphanin FQ receptor.
Published in: Peptides

Ligand: UFP-112 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein G alpha qi5.
Published in: Naunyn Schmiedebergs Arch Pharmacol