Category I: unambiguous substrates (YYY)
| Compound Name | Papp A → B | Mass Balance A → B | Papp B → A | Mass Balance B → A | BA/AB Ratio | Effluxed (Y/N) | ATPase Assay Ratio | ATPase Activator (Y/N) | Calcein-AM Assay | Calcein-AM Inhibitor (Y/N) |
|---|---|---|---|---|---|---|---|---|---|---|
| nm/s | nm/s | % max | ||||||||
| Amprenavir | 21.7 ± 1.16 | 69.0 | 703 ± 30.7 | 76.5 | 32.4 | Y7-a | 5.30 | Y | 17.6 | Y |
| BW 1019W91 | 242 ± 15.1 | 76.1 | 598 ± 11.0 | 91.4 | 2.47 | Y7-a | 6.46 | Y | 82.0 | Y |
| BW 1288U89 | 216 ± 31.9 | 88.3 | 627 ± 35.5 | 94.5 | 2.90 | Y7-a | 4.13 | Y | 75.7 | Y |
| BW 1351W91 | 268 ± 3.20 | 75.1 | 408 ± 34.1 | 75.6 | 1.52 | Y7-a | 8.57 | Y | 77.0 | Y |
| BW 1379W91 | 157 ± 14.3 | 97.7 | 778 ± 31.6 | 101 | 4.95 | Y | 4.77 | Y | 54.7 | Y |
| Loratidine | 264 ± 4.05 | 58.8 | 502 ± 37.0 | 121 | 1.90 | Y7-a 7-b | 12.1 | Y | 99.4 | Y |
| Diltiazem | 413 ± 3.52 | 99.9 | 676 ± 14.9 | 96.0 | 1.64 | Y7-a | 2.64 | Y | 37.3 | Y |
| Dipyridamole | 28.5 ± 6.33 | 70.7 | 646 ± 30.0 | 75.9 | 22.7 | Y7-a | 10.8 | Y | 98.2 | Y |
| Loperamide | 99.8 ± 13.2 | 92.0 | 776 ± 28.6 | 96.6 | 7.77 | Y7-a | 3.75 | Y | 76.3 | Y |
| Monensin | 102 ± 10.8 | 87.7 | 294 ± 12.8 | 89.6 | 2.88 | Y | 6.71 | Y | 52.2 | Y |
| Nelfinavir | 38.1 ± 11.8 | 66.8 | 338 ± 15.0 | 74.4 | 8.86 | Y7-a | 5.21 | Y | 30.6 | Y |
| Prazosin | 143 ± 6.48 | 87.4 | 661 ± 27.3 | 86.4 | 4.63 | Y | 3.40 | Y | 26.6 | Y |
| Quinidine | 36.4 ± 5.50 | 77.8 | 990 ± 66.4 | 88.8 | 27.2 | Y7-a | 2.54 | Y | 30.0 | Y |
| Reserpine | 68.1 ± 8.27 | 42.0 | 253 ± 11.6 | 60.6 | 3.71 | Y7-a | 3.85 | Y | 51.1 | Y |
| Ritonavir | 15.8 ± 5.61 | 81.3 | 852 ± 61.9 | 85.7 | 54.4 | Y | 8.16 | Y | 74.1 | Y |
| Saquinavir | 3.01 ± 0.78 | 92.9 | 495 ± 18.9 | 98.9 | 165 | Y7-a | 7.11 | Y | 35.5 | Y |
| Terfenadine | 65.6 ± 21.4 | 40.0 | 306 ± 48.2 | 70.0 | 4.66 | Y7-a 7-b | 3.13 | Y | 100 | Y |
| Vinblastine | <107-c | 94.2 | 232 ± 25.9 | 94.9 | >23 | Y | 4.31 | Y | 24.4 | Y |
| Mean | 131 | 544 | 18.7 | 5.43 | 57.9 | |||||
| Median | 102 | 550 | 4.63 | 4.45 | 53.5 | |||||
| Minimum | 3.01 | 232 | 1.52 | 2.19 | 17.6 | |||||
| Maximum | 413 | 990 | 165 | 12.1 | 100 |
n = 18 compounds.
Y, yes; N, no; BW, Burroughs Wellcome compounds, which are a series of acrivastine derivatives (Christensen et al., 1997).
↵7-a Run in the presence and absence of 2 μM GF120918 to confirm whether the compound is transported by Pgp.
↵7-b Run twice with the results and mass balances similar between experiments.
↵7-c Compound concentrations in samples below the limit quantification (BQL). Papp value is calculated from the lowest detectable standard.