Table 2. Ki Values for Inhibition of [3H]WIN35,428 Binding by Indicated Compounds to hDAT WT and hDAT Y156Fa.
| compound | WT Ki (nM) | n | Y156F Ki (nM) | n | affinity ratio |
|---|---|---|---|---|---|
| cocaine | 287 [244; 336] | 3 | 326 [247; 431] | 3 | 1.1 |
| 1 | 1020 [927; 1130] | 3 | 7560 [3980; 14400] | 3 | 7.4 |
| 9k | 55.4 [49.4; 62.2] | 3 | 402 [360; 450] | 3 | 7.3 |
| 10b | 6.74 [6.44; 7.05] | 3 | 248 [195; 317] | 5 | 37 |
| 10i | 50.6 [49.3; 51.9] | 3 | 618 [469; 882] | 4 | 12 |
| 10k | 37.5 [35.4; 39.7] | 3 | 346 [309; 387] | 3 | 9.2 |
| 10l | 244 [219; 272] | 3 | 1090 [7610; 1560] | 4 | 4.5 |
| 21a | 86.9 [84.8; 89] | 3 | 1130 [1040; 1230] | 3 | 13 |
a
The Ki values are determined from their respective IC50 values in inhibiting [3H]WIN35,428 binding using the Cheng–Prusoff equation. Experiments were performed on intact COS7 cells transiently expressing hDAT WT or hDAT Y156F mutant. All measurements were performed in technical triplicate with the indicated n number of biological replicates. Values are shown as mean [SEM interval] and are calculated from pIC50 and the SE interval from pIC50 ± SE. See Experimental Methods section for details.