Skip to main content

Table 2 Orexin 2 receptor binding kinetic parameters for DORAs

From: The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold

Compound Kd(nM) T1/2ON (min) KON(mol-1 · min-1) T1/2OFF (min) KOFF(min-1)
Almorexant 0.048 162a 1.58 × 107 268 2.696 × 10-3
Suvorexant 0.401 80.1 7.63 × 106 89.4 7.784 × 10-3
DORA-12 0.157 57.5 2.77 × 107 232 3.154 × 10-3
MK-6096 0.338 62.9 1.69 × 107 118 6.754 × 10-3
DORA-22 0.834 24.7 9.19 × 106 37.8 1.878 × 10-2
SB-649868 0.163 37.0 2.56 × 107 57.0 1.258 × 10-2
  1. aAlmorexant T1/2 ON represents an underestimate as almorexant was applied at concentrations 3-fold above its Kd in order to measure its kinetics alongside other DORAs.
  2. Kd, binding constant; KOFF, dissociation constant; KON, association constant; T1/2 OFF, half-life off-rates; T1/2 ON, binding half-life.