Table 1.
Binding affinity at α×β3 γ2 GABAA/BZ site subtypes. Measurements were made in duplicate. Ki values are reported in nM.
| Compound | α1 | α2 | α3 | α4 | α5 | α6 |
|---|---|---|---|---|---|---|
| diazepam | 14.0 | 7.8 | 13.9 | NDa | 13.4 | NDa |
| zolpidem | 29.6 | 160.0 | 380.0 | NDa | >10000 | NDa |
| SH-053-2'N | 300.0 | 160.0 | 527.0 | NDb | 82.0 | >5000 |
| SH-053-2'Nc | 118.0 | 148.0 | 365.0 | >5000 | 77.0 | >5000 |
| SH-053-R-CH3-2'F | 759.1 | 948.2 | 768.8 | NDb | 95.2 | NDb |
| SH-053-S-CH3-2'F | 468.2 | 33.3 | 291.5 | NDb | 19.2 | >5000 |
| JY-XHe-053 | 22.0 | 12.3 | 34.9 | NDb | 0.7 | NDb |
a
ND, not determined
b
Binding at α4 and α6 subtypes have not been determined, but since the 6-phenyl group is present, the ligand will not bind to α4 and α6 subtypes
c
The second independent set of experiments with SH-053-2'N