Compound | rD0, µM | Pe ± S.D. × 10^{−6} cm/s | % Cell ± S.D. | % Recovery | Pe _{BL/AP} | Pe _{c/l} | P-gp | P-gp Inhibition % | Comments | ||
---|---|---|---|---|---|---|---|---|---|---|---|

5 µM | 25 µM | ||||||||||

M2 | P-gp inhibited | Yes | 0 | 0 | Very slow Pe, very low % cell, inhibition unlikely | ||||||

A-B | 3.5 | 1.1 ± 0.25 | 0.34 ± 0.00 | 102 ± 0.56 | 0.71 | 29 | |||||

B-A | 3.3 | 0.80 ± 0.00 | 0.31 ± 0.00 | 100 ± 5.1 | |||||||

P-gp active | |||||||||||

A-B | 3.3 | 0.57 ± 0.05 | 0.30 ± 0.02 | 100 ± 1.4 | 21 | ||||||

B-A | 3.4 | 12 ± 0.26 | 0.27 ± 0.02 | 89 ± 3.6 | |||||||

M16 | P-gp inhibited | Yes | 1 | 21 | Fast Pe, moderate % cell, inhibition unlikely | ||||||

A-B | 3.5 | 53 ± 0.14 | 20 ± 0.18 | 154 ± 0.40 | 0.99 | 6.1 | |||||

B-A | 2.8 | 53 ± 0.04 | 19 ± 0.73 | 130 ± 3.9 | |||||||

P-gp active | |||||||||||

A-B | 2.6 | 16 ± 2.1 | 11 ± 0.09 | 115 ± 5.7 | 6.0 | ||||||

B-A | 2.6 | 97 ± 0.62 | 7.9 ± 0.42 | 125 ± 4.1 | |||||||

Parent | P-gp inhibited | No | 6 | 25 | Fast Pe, high partitioning, inhibition unlikely | ||||||

A-B | 2.1 | 19 ± 2.3 | 50 ± 0.53 | 92 ± 8.6 | 1.2 | 1.5 | |||||

B-A | 2.4 | 21 ± 0.02 | 28 ± 0.00 | 97 ± 5.5 | |||||||

P-gp active | |||||||||||

A-B | 2.8 | 15 ± 0.13 | 49 ± 1.6 | 88 ± 0.25 | 1.8 | ||||||

B-A | 2.7 | 27 ± 1.1 | 27 ± 5.4 | 94 ± 1.4 |

rD0 is the measured concentration of recovered donor solution at

*t*= 60 min. Pe is the apparent permeability coefficient (*n*= 2) with 60-min time interval: AB, BA>15, fast; AB, BA is 2–15, moderate; AB, BA is 1–2, slow; AB, BA is <1, very slow. % Cell is the amount extracted from cell with methanol relative to recovered mass: <1%, very low; 1%–5%, low; 6%–20%, moderate; 21%–89%, high; ≥90%, very high (invalidates Pe values because compound prefers lipid environment, assay artifact). %Recovery is the mass of D60 + cell60 + R60/D0 (measured concentration of donor solution at*t*= 0) × 100. If >100%, then D0 is underestimated. Pe_{BL/AP}is the ratio of Pe values in B-to-A and A-to-B directions; >3.0 + active efflux; Pe_{C/I}is the net efflux ratio = inhibited BA/AB and control BA/AB ratio. P-gp Yes (Y), No (*N*), or Unknown (U): if ≥3, Y; <3,*N*; if % Cell > 90, U. P-gp inhibition, two concentrations (5 and 25 µM) tested for calcein AM uptake assay in MDCK-MDR1 cells; % inhibition vs. LSN335984 (EC_{50}= 0.15–0.3 µM), pending at 5 µM: 0–20, inhibition unlikely, 21–50, partial inhibition possible, >51%, partial inhibition likely.