Table 2.
Inhibition of the maximal current amplitude of the three compounds tested on all substitution constructs made
| Constructs | AZ868 (1 μM) | A-967079 (0.2 μM) | HC-030031 (10 μM) |
|---|---|---|---|
| Wild-type | 72 ± 2 (n = 7) | 60 ± 1 (n = 12) | 80 ± 2 (n = 14)) |
| M911A/M912A | 26 ± 2a (n = 10) | 61 ± 3 (n = 5) | 84 ± 2 (n = 10) |
| L941A | 71 ± 3 (n = 5) | 74 ± 4 (n = 3) | 81 ± 4 (n = 2) |
| S943A | 69 ± 3 (n = 10) | 63 ± 3 (n = 7) | 78 ± 1 (n = 6) |
| F944A | −5 ± 2a (n = 8) | 3 ± 2a (n = 16) | 75 ± 3 (n = 11) |
| T945A | 45 ± 2 (n = 8) | 46 ± 2 (n = 12) | 74 ± 2 (n = 10) |
| I946M | 57 ± 4 (n = 10) | 67 ± 2 (n = 7) | 81 ± 2 (n = 5) |
| V948A | 41 ± 4b (n = 11) | 27 ± 2c (n = 10) | 77 ± 3 (n = 15) |
| I950F | 33 ± 2a (n = 13) | 36 ± 1 (n = 5) | 75 ± 3 (n = 16) |
| Rat substitutions | 3 ± 1a (n = 5) | 30 ± 2c (n = 11) | 73 ± 1 (n = 9) |
Values are mean ± SE and statistical significance is based on a one-way ANOVA test versus the WT inhibition and significance is given by the p values as stated.
a
p < 0.001.
b
p = 0.05–0.01.
c
p = 0.01–0.001.