Table 3. K_i Values for Inhibition of [³H]DA Uptake by Indicated Compounds to hDAT WT and the Y335A Mutant^a.

compound	WT Ki (nM)	n	Y335A Ki (nM)	n	affinity ratio
cocaine	219 [191; 250]	5	13800 [12700; 15100]	6	70
9b	39.8 [30.6; 51.8]	6	1010 [895; 1140]	4	25
9k	78.8 [73.2; 84.8]	3	1670 [1540; 1810]	3	21
10b	7.93 [6.99; 8.99]	3	573 [469; 700]	5	72
10i	50.5 [42.1; 60.5]	4	1580 [1450; 1730]	3	31
10k	42.7 [40.2; 45.4]	3	2930 [2660; 3230]	3	69
10l	225 [179; 283]	3	6130 [5740; 6540]	3	27
21a	238 [217; 262]	3	8660 [7840; 9560]	3	36

^aThe K_i values are determined from their respective IC₅₀ values in inhibiting [³H]DA uptake using the Cheng–Prusoff equation. Experiments were performed on intact COS7 cells transiently expressing hDAT WT or hDAT Y335A. 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.