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

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: [3H]SB-674042 (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]SB-674042 (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]SB-674042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  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]-TCS 1102 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKd
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): 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: no
Median affinity: 9 pKB
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: 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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
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: suvorexant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 9.100000381469727 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 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): 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: 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: 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: YNT-185 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.559999942779541 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: no
Median affinity: 5.559999942779541 pEC50
Reference (Journal): Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models.
Published in: Proc Natl Acad Sci USA