IC50 and Ki values of the GABAAR competitive antagonist, gabazine, on GABA-induced current for all mutants.
Mutants | IC50 | Ki | n | ||
|---|---|---|---|---|---|
| μM | |||||
| GABACR (ρ1) | WT | 97.29 ± 11.52 | 57.84 ± 7.66 | 5 | |
| Y102F | 5.77 ± 1.01 | 3.98 ± 0.69 | 3 | ||
| Y106S | 3.04 ± 0.27 | 2.13 ± 0.21 | 4 | ||
| F138Y | 14.04 ± 1.74 | 9.74 ± 1.21 | 4 | ||
| V140L | 322.85 ± 12.84 | 206.09 ± 8.20 | 4 | ||
| S168T | 19.86 ± 2.02 | 13.62 ± 1.39 | 4 | ||
| L216V | 326.72 ± 29.44 | 186.70 ± 16.83 | 3 | ||
| T218V | 20.68 ± 3.94 | 11.54 ± 2.20 | 4 | ||
| R221D | 53.37 ± 2.51 | 27.21 ± 1.28 | 4 | ||
| FYS240VF | 39.07 ± 4.66 | 27.16 ± 3.24 | 4 | ||
| Y106S+F138Y | 2.56 ± 0.18 | 1.73 ± 0.12 | 4 | ||
| Y106S+FYS240VF | 5.80 ± 0.49 | 4.12 ± 0.31 | 4 | ||
| F138F+FYS240VF | 16.68 ± 0.51 | 12.16 ± 0.37 | 3 | ||
| Y102F+Y106S+F138Y | 2.64 ± 0.05 | 1.61 ± 0.03 | 3 | ||
| Y106S+F138Y+FYS240VF | 2.69 ± 0.24 | 1.83 ± 0.16 | 3 | ||
| GABAAR | α1β2γ2_WT | 0.15 ± 0.01 | 0.12 ± 0.01 | 3 | |
|
| α1(F64Y+S68Y)β2(Y97F+L99V+VF199FYS)γ2 | 3.54 ± 0.35 | 2.67 ± 0.26 | 4 | |