. Author manuscript; available in PMC: 2014 Jun 24.

Published in final edited form as: ACS Chem Biol. 2014 Jan 6;9(3):722–730. doi: 10.1021/cb4008953

Table 1.

IC₅₀ Values for the Inhibition of PfCRT^CQR-Mediated CQ Transport by Quinine Dimers

compound	IC₅₀ (µM)^a
verapamil	30 ± 3¹²
quinine	48 ± 6¹²
1	5.3 ± 0.3
3	5.8 ± 0.5
5	1.0 ± 0.1
6	1.4 ± 0.2

PfCRT^CQR-mediated CQ transport was calculated by subtracting the uptake measured in oocytes expressing D10 PfCRT^CQS from that in oocytes expressing Dd2 PfCRT^CQR. The half-maximal inhibitory concentrations (IC₅₀ values) were derived by least-squares fit of the equation Y = Y_min + [(Y_max − Y_min)/(1 + ([inhibitor]/IC₅₀)C)] where Y is PfCRT^CQR-mediated CQ transport, Y_min and Y_max are the minimum and maximum values of Y, and C is a constant. All values are mean ± SEM from n = 4 or 5 separate experiments, within which measurements were made from 10 oocytes per treatment. The data from which these values were obtained are shown in Figure 3.