TABLE 1

Relative inhibitory potencies of CGPs on MRP1-mediated E217βG uptake

CGPChalcogen AtomIC50a (E217βG Uptake)Log Pb
μM
Class I
 I-2S3.9 ± 1.9 (3)1.6 ± 0.1
 I-3S1.8 ± 0.1 (3)1.5 ± 0.2c
 I-4Se0.7 ± 0.3 (3)1.6 ± 0.1c
 I-5Te2.5 ± 0.5 (4)1.6 ± 0.1
Class II
 II-13S7.6 ± 3.1 (3)1.0 ± 0.1
 II-14Se4.9 ± 3.9 (3)1.1 ± 0.1
Class III
 III-1S1.6 ± 0.4 (3)2.1 ± 0.1
 III-2S2.0, 1.80.5 ± 0.1
Class IV
 IV-1Te5.3 ± 0.7 (3)1.4 ± 0.1
 IV-3Te3.3 ± 0.6 (3)1.1 ± 0.1
Class V
 V-1Te4.7, 3.22.5 ± 0.2
 V-3Se1.1 ± 0.4 (4)1.9 ± 0.1
 V-4Te1.2 ± 0.2 (3)1.9 ± 0.1
 V-5Te1.2, 0.91.8 ± 0.2
 V-6Se0.9 ± 0.1 (3)1.9 ± 0.1d
 V-7Te1.4, 1.42.4 ± 0.1d
  • a The values shown represent the means ± S.D. (n) of IC50 values obtained in 2–4 independent experiments. When the compound was tested only twice, both values obtained are shown.

  • b The values shown are experimental log P values that were derived as described in Materials and Methods.

  • c From Sawada et al. (2008).

  • d From Detty et al. (1990).