TABLE I.
Estimated EC50 and n for the Mutations in TM1
| Mutation | EC50 (μM) | n | Fold change in EC50 a |
|---|---|---|---|
| WT | 11.8 ± 0.7 | 1.5 ± 0.1 | 1.0 |
| V49W | 8.2 ± 1.9 | 1.3 ± 0.3 | 1.4 |
| F48W | 5.5 ± 0.2 | 1.5 ± 0.1 | 2.2 |
| V47W | 1.4 ± 0.3 | 1.0 ± 0.2 | 8.4 |
| W46A | 2.0 ± 0.1 | 1.6 ± 0.1 | 5.9 |
| G45W | 0.5 ± 0.04 | 1.4 ± 0.1 | 23.6 |
| I44W | 1.5 ± 0.1 | 1.9 ± 0.3 | 7.9 |
| V43W | 1.6 ± 0.2 | 1.3 ± 0.1 | 7.4 |
| Y42W | 1.4 ± 0.1 | 1.3 ± 0.1 | 8.4 |
| A41W | 11.3 ± 0.2 | 1.6 ± 0.05 | 1.0 |
| L40W | >30 | NDb | <0.4 |
| I39W | 2.0 ± 0.2 | 1.4 ± 0.1 | 5.9 |
| L38W | 7.6 ± 0.6 | 1.2 ± 0.1 | 1.6 |
| L37W | 13.5 ± 0.7 | 1.4 ± 0.1 | 0.9 |
| Q36W | 2.7 ± 0.1 | 1.6 ± 0.1 | 4.4 |
| V35W | 14.5 ± 3.5 | 1.1 ± 0.1 | 0.8 |
| A34W | 8.7 ± 0.9 | 1.2 ± 0.1 | 1.4 |
| R33W | 6.1 ± 0.4 | 1.4 ± 0.1 | 1.9 |
| N32W | 2.9 ± 0.2 | 1.4 ± 0.1 | 4.1 |
| M31W | 6.1 ± 1.3 | 1.0 ± 0.1 | 1.9 |
| L30W | 12.2 ± 1.6 | 1.0 ± 0.1 | 1.0 |
| G29W | 9.1 ± 0.8 | 1.2 ± 0.1 | 1.3 |
| V28W | ND | ND |
a
Fold change in EC50 was calculated as EC50(WT)/EC50(mutant).
b
ND, not determined.