Table 3.
Effect of SERT mutations on the allosteric potency of cpd 3 relative to S‐CIT
| Construct | S‐CIT allosteric potency IC 50 (μM) | n | Cpd 3 allosteric potency IC 50 (μM) | n |
|---|---|---|---|---|
| WT | 5.8 [5.4; 6.3] | 10 | 3.6 [3.3; 3.8] | 6 |
| L99H | 17 [13; 20] | 4 | 7.6 [6.7; 8.8] | 3 |
| W103H | 28 [23; 34] | 6 | 8.8 [8.1; 9.5] | 5 |
| R104K | >200 | 6 | >200 | 5 |
| I179H | 35 [30; 41] | 4 | 3.7 [2.2; 6.3] | 3 |
| A486E | 28 [25; 31] | 3 | 12 [8.9; 17] | 3 |
The allosteric potencies are the IC50 values obtained from non‐linear regression analysis of data from [3H]‐S‐CIT dissociation experiments in the presence of increasing concentrations of S‐CIT or cpd 3. Data were calculated and experiments performed as described in Methods section. Data are based on the indicated number (n) of independent experiments.