GSK1059865 is a novel, potent and highly selective OX1R antagonist.

SB408124 (SB-408124; SB 408124) is a potent, novel, selective, non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, it exhibits 50-fold selectivity over OX2 receptor.

SB-649868 (GSK-649868) is a novel, potent, selective and orally bioactive orexin (OX) 1 and OX2 receptor antagonist with pKi of 9.4 and 9.5 for OX1 and OX2 receptor, respectively.

TCS-OX2-29 (TCS-OX229, TCS-OX-229), discovered from high throughput screening (HTS), is a potent, selective and non-peptide OX2 (orexin) receptor antagonist with potential usefulness in the treatment of insomnia.

IPSU is a novel, potent, selective, orally bioavailable and brain penetrant orexin receptor (OX2R) antagonist with potential to be used for insomnia.

SB-334867 is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with a pKb value of 7.2.

Almorexant (also known as ACT078573) is a novel, potent, orally bioactive, competitive and dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively.

GSK1059865 is a novel, potent and highly selective OX1R antagonist.

Lemborexant (E2006; E-2006; Dayvigo) is a novel, reversible, competitive and orally bioactive dual antagonist of the orexin OX1 and OX2 receptors (IC50 values of 6.1 nM and 2.6 nM, respectively) which was under development by Eisai for the treatment of insomnia.

SB-674042 is a novel, potent and selective non-peptide orexin OX1 receptor antagonist with Kd of 3.76 nM; It exhibits 100-fold selectivity for OX1 over OX2 receptors.