Target family: Orexin receptors (type: gpcr)
Target: OX<sub>1</sub> receptor

Ligand: ACT-335827 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKB
Reference (Journal): Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.
Published in: ChemMedChem

Ligand: ACT-462206 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.199999809265137 pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: ACT-462206 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKB
Reference (Journal): Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.
Published in: ChemMedChem

Ligand: [Ala11, D-Leu15]orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Agonist ligand discrimination by the two orexin receptors depends on the expression system.
Published in: Neurosci Lett

Ligand: [Ala11, D-Leu15]orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.
Published in: Bioorg Med Chem Lett

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.
Published in: J Pharmacol Exp Ther

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKB
Reference (Journal): The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.
Published in: J Pharmacol Exp Ther

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA).
Published in: Mol Pharmacol

Ligand: almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: compound 11 [PMID: 15261275] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKi
Reference (Journal): Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 1 [PMID: 33547286] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.449999809265137 pEC50
Reference (Journal): Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.
Published in: Nat Commun

Ligand: Cp-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.590000152587891 pKi
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: CVN45502 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKB
Reference (Journal): Pharmacological targeting of glutamatergic neurons within the brainstem for weight reduction.
Published in: Nat Metab

Ligand: CVN766 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Discovery and first-time disclosure of CVN766, an exquisitely selective orexin 1 receptor antagonist.
Published in: Bioorg Med Chem Lett

Ligand: danavorexton (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): TAK-925, an orexin 2 receptor-selective agonist, shows robust wake-promoting effects in mice.
Published in: Pharmacol Biochem Behav

Ligand: daridorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2022)
Primary target: no
Median affinity: 9 pKB
Reference (Journal): Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia.
Published in: Psychopharmacology (Berl)

Ligand: daridorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2022)
Primary target: no
Median affinity: 9.5 pKB
Reference (Journal): Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia.
Published in: Psychopharmacology (Berl)

Ligand: daridorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2022)
Primary target: no
Median affinity:  pKB
Reference (Journal): The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.
Published in: J Pharmacol Exp Ther

Ligand: daridorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2022)
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: EMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.340000152587891 pKi
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: EMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: EMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.050000190734863 pKi
Reference (Journal): Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.
Published in: Br J Pharmacol

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Published in: J Med Chem

Ligand: filorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of MK-6096 - A dual orexin receptor antagonist for insomnia.
Published in: Neuropharmacology

Ligand: firazorexton (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.849999904632568 pEC50
Reference (Journal): TAK-994, a Novel Orally Available Brain-Penetrant Orexin 2 Receptor-Selective Agonist, Suppresses Fragmentation of Wakefulness and Cataplexy-Like Episodes in Mouse Models of Narcolepsy.
Published in: J Pharmacol Exp Ther

Ligand: HTL6641 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: HTL6641 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKi
Reference (Journal): Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties
Published in: Medicinal Chemistry Communications

Ligand: JH112 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.140000343322754 pKi
Reference (Journal): Structure-based development of a subtype-selective orexin 1 receptor antagonist.
Published in: Proc Natl Acad Sci U S A

Ligand: JNJ-10397049 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 pKB
Reference (Journal): Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Published in: Bioorg Med Chem Lett

Ligand: JNJ-10397049 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKB
Reference (Journal): Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists.
Published in: Eur J Pharmacol

Ligand: JNJ-10397049 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Published in: Bioorg Med Chem Lett

Ligand: lemborexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: yes
Median affinity: 8.220000267028809 pKi
Reference (Journal): Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.
Published in: J Med Chem

Ligand: lemborexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: LSN2424100 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.409999847412109 pKi
Reference (Journal): LSN2424100: a novel, potent orexin-2 receptor antagonist with selectivity over orexin-1 receptors and activity in an animal model predictive of antidepressant-like efficacy.
Published in: Front Neurosci

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Published in: ChemMedChem

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Published in: ChemMedChem

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pKi
Reference (Journal): Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Published in: ChemMedChem

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: MK-1064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Published in: ChemMedChem

Ligand: MK-3697 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.440000057220459 pKi
Reference (Journal): Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Published in: Bioorg Med Chem Lett

Ligand: MK-3697 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: MK-3697 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: MK-3697 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: MK-3697 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 pKi
Reference (Journal): Orexin 2 receptor (OX2R) protein distribution measured by autoradiography using radiolabeled OX2R-selective antagonist EMPA in rodent brain and peripheral tissues.
Published in: Sci Rep

Ligand: Nag 26 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of the orexin/hypocretin receptor agonist Nag 26.
Published in: Eur J Pharmacol

Ligand: Nag 26 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists.
Published in: J Med Chem

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterization of recombinant human orexin receptor pharmacology in a Chinese hamster ovary cell-line using FLIPR.
Published in: Br J Pharmacol

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): OX(1)  orexin/hypocretin receptor activation of phospholipase D.
Published in: Br J Pharmacol

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): OX1 orexin/hypocretin receptor signaling through arachidonic acid and endocannabinoid release.
Published in: Mol Pharmacol

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Requirement of intact disulfide bonds in orexin-A-induced stimulation of gastric acid secretion that is mediated by OX1 receptor activation.
Published in: Biochem Biophys Res Commun

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Orexin signaling in recombinant neuron-like cells.
Published in: FEBS Lett

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Regulation of OX1 orexin/hypocretin receptor-coupling to phospholipase C by Ca2+ influx.
Published in: Br J Pharmacol

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.
Published in: Cell

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Effects of orexin (hypocretin) on GIRK channels.
Published in: J Neurophysiol

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Arachidonic acid release mediated by OX1 orexin receptors.
Published in: Br J Pharmacol

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): OX2 orexin/hypocretin receptor signal transduction in recombinant Chinese hamster ovary cells.
Published in: Cell Signal

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Multiple phospholipase activation by OX(1) orexin/hypocretin receptors.
Published in: Cell Mol Life Sci

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
Published in: Bioorg Med Chem Lett

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Distinct recognition of OX1 and OX2 receptors by orexin peptides.
Published in: J Pharmacol Exp Ther

Ligand: orexin-A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Published in: Br J Pharmacol

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Distinct recognition of OX1 and OX2 receptors by orexin peptides.
Published in: J Pharmacol Exp Ther

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Arachidonic acid release mediated by OX1 orexin receptors.
Published in: Br J Pharmacol

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Published in: Br J Pharmacol

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Multiple phospholipase activation by OX(1) orexin/hypocretin receptors.
Published in: Cell Mol Life Sci

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.
Published in: Cell

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Requirement of intact disulfide bonds in orexin-A-induced stimulation of gastric acid secretion that is mediated by OX1 receptor activation.
Published in: Biochem Biophys Res Commun

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Agonist ligand discrimination by the two orexin receptors depends on the expression system.
Published in: Neurosci Lett

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Orexin signaling in recombinant neuron-like cells.
Published in: FEBS Lett

Ligand: orexin-B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterization of recombinant human orexin receptor pharmacology in a Chinese hamster ovary cell-line using FLIPR.
Published in: Br J Pharmacol

Ligand: RTOXA-43 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pEC50
Reference (Journal): Discovery of Arylsulfonamides as Dual Orexin Receptor Agonists.
Published in: J Med Chem

Ligand: (R)-YNT-3708 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.109999656677246 pEC50
Reference (Journal): Design and Synthesis of Orexin 1 Receptor-Selective Agonists.
Published in: J Med Chem

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.840000152587891 pKi
Reference (Journal): A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.
Published in: J Pharmacol Exp Ther

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pKB
Reference (Journal): Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.
Published in: Br J Pharmacol

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.
Published in: J Pharmacol Exp Ther

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKi
Reference (Journal): Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.
Published in: Br J Pharmacol

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Published in: J Med Chem

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Published in: Br J Pharmacol

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Published in: Bioorg Med Chem Lett

Ligand: SB-408124 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKB
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: SB-408124 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: SB-408124 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pKi
Reference (Journal): A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.
Published in: J Pharmacol Exp Ther

Ligand: SB-408124 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pKi
Reference (Journal): A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.
Published in: J Pharmacol Exp Ther

Ligand: SB-410220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Published in: Br J Pharmacol

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Published in: Bioorg Med Chem Lett

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Published in: Bioorg Med Chem Lett

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Published in: J Med Chem

Ligand: SB-649868 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: SB-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Published in: Br J Pharmacol

Ligand: SB-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Published in: Mol Pharmacol

Ligand: seltorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pKB
Reference (Journal): Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.
Published in: J Pharmacol Exp Ther

Ligand: seltorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKB
Reference (Journal): Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.
Published in: J Pharmacol Exp Ther

Ligand: seltorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pKi
Reference (Journal): Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.
Published in: J Pharmacol Exp Ther

Ligand: seltorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pKi
Reference (Journal): Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.
Published in: J Pharmacol Exp Ther