|
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
|
- 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.
- Kd, binding constant; KOFF, dissociation constant; KON, association constant; T1/2 OFF, half-life off-rates; T1/2 ON, binding half-life.
