Database of Papp and efflux ratio data for the FG dataset obtained in MDCK-MDR1 and Caco-2 cells
| Substratea | PSA | HBD | MDCK-MDR1 | Caco-2 | ||
|---|---|---|---|---|---|---|
| Papp (A-B) | ER | Papp (A-B) | ER | |||
| nm/s | nm/s | |||||
| Alfentanil | 85.5 | 0 | 376 | 0.7 | 293 | 1.1 |
| Alprazolam | 43.1 | 0 | 369 | 0.9 | 255 | 0.9 |
| Buspirone | 69.6 | 0 | 398 | 1.0 | 254 | 1.1 |
| Cisapride | 86.1 | 3 | 299 | 0.6 | 299 | 0.9 |
| Cyclosporine | 278.8 | 5 | 6 | 20 | 5 | 5.6 |
| Felodipine | 64.6 | 1 | 139 | 0.5 | 42 | 1.0 |
| Indinavir | 118 | 4 | 19 | 12 | 12 | 15 |
| Lovastatin | 72.8 | 1 | 261 | 1.1 | 145 | 0.8 |
| Methadone | 20.3 | 0 | 259 | 1.4 | 219 | 1.2 |
| Midazolam | 30.2 | 0 | 369 | 0.8 | 324 | 1.0 |
| Nifedipine | 107.8 | 1 | 389 | 1.0 | 235 | 1.0 |
| Nisoldipine | 108 | 1 | N.D. | N.D. | N.D. | N.D. |
| Quinidine | 45.6 | 1 | 176 | 4.4 | 85 | 3.8 |
| Repaglinide | 78.9 | 2 | 282 | 1.0 | 241 | 0.6 |
| Rifabutin | 206 | 5 | 52 | 6.0 | 95 | 3.3 |
| Saquinavir | 166.8 | 6 | 8 | 75 | 4 | 57 |
| Sildenafil | 113 | 1 | 262 | 2.0 | 256 | 1.8 |
| Simvastatin | 72.8 | 1 | 215 | 1.3 | 68 | 0.7 |
| Tacrolimus | 178.4 | 3 | 105 | 4.6 | 131 | 2.1 |
| Terfenadine | 43.7 | 2 | N.D. | N.D. | N.D. | N.D. |
| Trazodone | 42.3 | 0 | 295 | 1.1 | 242 | 0.9 |
| Triazolam | 43.1 | 0 | 350 | 0.9 | 280 | 0.6 |
| Verapamil | 64 | 0 | 318 | 1.0 | 138 | 1.8 |
| Zolpidem | 37.6 | 0 | 365 | 1.0 | 319 | 1.1 |
PSA, polar surface area; HBD, hydrogen bond donor; N.D., not determined.
↵a Papp (A-B) data were supplemented from the literature for atorvastatin: 60 nm/s in Caco-2 cells (Wu et al., 2000; Hochman et al., 2004); terfenadine: 106 nm/s in MDCK-MDR1 cells (Polli et al., 2001; Doan et al., 2002); and nisoldipine: > 200 nm/s, given its structural similarity to nifedipine and nitrendipine, both of which show high permeability (Polli et al., 2001).