Inhibition of BFC debenzylase activity
| Compound | Calculated Molecular Volume | Molecular Weight | EstimatedKi | Ki Ratio | |||
|---|---|---|---|---|---|---|---|
| Wild Type (WT) | L211F | L211Y | L211F/WT | L211Y/WT | |||
| Diazepam | 242 | 285 | 80 ± 23 | 71 ± 7 | 75 ± 5 | 0.9 | 0.9 |
| Nifedipine | 292 | 346 | 3.0 ± 1.6 | 7 ± 2 | 3.4 ± 0.8 | 2.2 | 1.1 |
| Diltiazem | 298 | 451 | 18 ± 4 | 33 ± 3 | 32 ± 3 | 1.8 | 1.8 |
| Progesterone | 312 | 315 | 55 ± 12 | 57 ± 2 | 61 ± 9 | 1.0 | 1.1 |
| Haloperidol | 332 | 376 | 9.0 ± 0.8 | 10 ± 1 | 23 ± 5 | 1.1 | 2.5 |
| Verapamil | 437 | 455 | 12 ± 2 | 14 ± 2 | 25 ± 3 | 1.2 | 2.1 |
| Bromocriptine | 551 | 657 | 0.31 ± 0.06 | 0.45 ± 0.05 | 0.41 ± 0.10 | 1.5 | 1.3 |
| Erythromycin | 681 | 734 | 21 ± 0.6 | 42 ± 5 | 147 ± 11 | 2.0 | 7.1 |
| Vinblastine | 742 | 811 | 1.5 ± 0.4 | 18 ± 1 | 35 ± 4 | 12.0 | 23.0 |
| Troleadomycin | 751 | 814 | 1.1 ± 0.3 | 13 ± 3 | 46 ± 3 | 13.0 | 43.0 |
| Cyclosporin A | 1164 | 1201 | 0.14 ± 0.04 | 1.5 ± 0.2 | 3.2 ± 0.8 | 11.0 | 23.0 |
Calculated molecular volumes are in Å3, molecular weights in grams per mole, and estimated Kl values are in micromolar concentration. Sample profiles from this data set are shown in Fig. 2.