IC50 and Ki values of the GABACR competitive antagonist, 3-APA, on GABA-induced current for all mutants.
Mutants | IC50 | Ki | n | ||
|---|---|---|---|---|---|
| μM | |||||
| GABACR (ρ1) | WT | 21.03 ± 1.79 | 11.02 ± 0.94 | 3 | |
| Y102F | 237.86 ± 26.42 | 116.33 ± 12.92 | 4 | ||
| Y106S | 5.43 ± 0.75 | 3.81 ± 0.59 | 4 | ||
| F138Y | 118.57 ± 9.10 | 82.31 ± 6.32 | 4 | ||
| V140L | 523.06 ± 11.33 | 355.31 ± 7.69 | 4 | ||
| S168T | 144.67 ± 7.20 | 75.48 ± 3.75 | 4 | ||
| L216V | 106.70 ± 9.30 | 60.97 ± 5.31 | 3 | ||
| T218V | 61.67 ± 5.28 | 36.42 ± 3.12 | 4 | ||
| R221D | 16.42 ± 1.63 | 11.24 ± 1.11 | 3 | ||
| FYS240VF | 391.52 ± 11.11 | 272.24 ± 7.73 | 4 | ||
| Y106S+F138Y | 96.61 ± 8.71 | 67.67 ± 6.10 | 3 | ||
| Y106S+FYS240VF | 429.03 ± 14.41 | 305.20 ± 10.25 | 4 | ||
| F138Y+FYS240VF | 309.79 ± 36.77 | 207.37 ± 24.61 | 3 | ||
| Y106S+F138Y+FYS240VF | 87.22 ± 7.16 | 59.53 ± 4.88 | 3 | ||
| Y102F+F138Y+FYS240VF | 226.87 ± 3.47 | 151.24 ± 2.31 | 3 | ||
| Y102F+V140L+FYS240VF | 1212.82 ± 144.50 | 844.88 ± 100.67 | 4 | ||
| Y106S+F138Y+V140L+FYS240VF | >2500 | >1299.64 | 4 | ||
|
| Y102F+Y106S+F138Y+V140L+FYS240VF | >>2500 | >>1374.82 | 4 | |
>>, inhibition was 20 to 40% at the concentration indicated; >, inhibition was between 40 to 50% at the concentration indicated.