TABLE 2

Ki values from 3H-serotonin uptake inhibition experiments in wild-type hSERT and hSERT mutations of residues in the central binding site diverging between hSERT and hDAT

Confidence levels are provided in Supplemental Table 2.

hSERT VariantMazindolAnalog
1234
nM
Wild type48014,800194011402500
Y95F182200023098159
A169S23015,5007607401500
I172V27010,000830430610
A173G850690015604902080
Y175F3102200751240310
T439A59089008408304100
L443M380720013401770590
T497A18944001651191240
Y95F_I172V78430022036310
Y95F_L443M210320017072250
I172V_L443M36017,900290270830
Y95F_I172V_L443M77400015727360