Table 1

Pgp inhibition parameters of several example compounds

Data are nonlinear regression solutions to Hill function followed by SE. Imax is a percentage of inhibition by verapamil. Inhibition of DNR transport function was evaluated using NIH3T3-G185 cell line.
CompoundIC50, μmImax, %n (Hill coefficient)
SCH663362.7 ± 0.1101 ± 23.2 ± 0.5
Cyclosporin A1.4 ± 0.1112 ± 43.6 ± 1.0
Paclitaxel54 ± 1.354 ± 0.63.1 ± 0.2
Verapamil4.2 ± 1.11001.0 ± 0.2
Vinblastine18 ± 0.390 ± 0.44.9 ± 0.2
Tamoxifen7.1 ± 0.373 ± 1.43.1 ± 0.3
Trifluoperazine7.2 ± 0.276 ± 12.2 ± 0.1
Ketoconazole5.6 ± 0.4112 ± 21.6 ± 0.2