Table 3

K i reversal values for substrates and antagonists

NSCKi reversal
Substrate
 38270 (S)>100
 328426 (S)5.44
 339281 (S)2.55
 359449 (S)>100
 630176 (S)>100
 633043 (S)>100
 640085 (S)>100
 666490 (S)>100
Antagonist
 68075 (A)0.37
 665333 (A)0.28
 667739 (A)5.13
 676590 (A)1.42
 676591 (A)0.28
 676597 (A)0.62
 676599 (A)2.18
 676600 (A)0.06
Overlap
 676605 (O)0.48
 668360 (O)0.25

K i reversal is the concentration (μm) at which half of the Pgp-mediated transport is blocked.