Target family: Orexin receptors (type: gpcr)
Target: OX<sub>2</sub> receptor

Ligand: YNT-185 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.550000190734863 pEC50
Reference (Journal): Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists.
Published in: J Med Chem

Ligand: YNT-185 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.550000190734863 pEC50
Reference (Journal): Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models.
Published in: Proc Natl Acad Sci USA

Ligand: TCS-OX2-29 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.
Published in: Bioorg Med Chem Lett

Ligand: TCS-OX2-29 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands.
Published in: Br J Pharmacol

Ligand: TCS 1102 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKB
Reference (Journal): Proline bis-amides as potent dual orexin receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: TCS 1102 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKB
Reference (Journal): Pharmacological characterization of the orexin/hypocretin receptor agonist Nag 26.
Published in: Eur J Pharmacol

Ligand: T-516 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.369999885559082 pEC50
Reference (Journal): TAK-925, an orexin 2 receptor-selective agonist, shows robust wake-promoting effects in mice.
Published in: Pharmacol Biochem Behav

Ligand: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: yes
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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 8.300000190734863 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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 9.199999809265137 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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 9.5 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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 9 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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 9.399999618530273 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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands.
Published in: Br J Pharmacol

Ligand: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: yes
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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: yes
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: [3H]-TCS 1102 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: [3H]T-516 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pKd
Reference (Journal): TAK-925, an orexin 2 receptor-selective agonist, shows robust wake-promoting effects in mice.
Published in: Pharmacol Biochem Behav

Ligand: [3H]SB-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKd
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: [3H]SB-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKd
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: [3H]EMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [3H]EMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [3H]EMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [3H]Cp-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [3H]-almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [3H]-almorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
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: [125I]orexin A (human, mouse, rat) (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery.
Published in: Br J Pharmacol

Ligand: [125I]orexin A (human, mouse, rat) (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.
Published in: Cell

Ligand: [125I]orexin A (human, mouse, rat) (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): OX2 orexin/hypocretin receptor signal transduction in recombinant Chinese hamster ovary cells.
Published in: Cell Signal

Ligand: seltorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 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: yes
Median affinity: 8 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: 8.800000190734863 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: 8 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: SB-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 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: no
Median affinity: 6.860000133514404 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-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.480000019073486 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-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-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: 8.800000190734863 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: 9.600000381469727 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: 9.699999809265137 pKB
Reference (Journal): Kinetic properties of &quot;dual&quot; orexin receptor antagonists at OX1R and OX2R orexin receptors.
Published in: Front Neurosci

Ligand: SB-408124 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 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 pKB
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: 5.699999809265137 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): 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Published in: Bioorg Med Chem Lett

Ligand: SB-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands.
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: 6.300000190734863 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-334867 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 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): A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.
Published in: J Pharmacol Exp Ther

Ligand: (R)-YNT-3708 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pEC50
Reference (Journal): Design and Synthesis of Orexin 1 Receptor-Selective Agonists.
Published in: J Med Chem

Ligand: RTOXA-43 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pEC50

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: 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): 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): 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): Effects of orexin (hypocretin) on GIRK channels.
Published in: J Neurophysiol