Table 3. Physicochemical Properties and Cell-Based Activity of Key Compounds.
| compound | pH 7 solubilitya (μM) | MDCKII Papp (×10–6 cm/s)b | pVASP (ser 239) cell assay (μM) |
|---|---|---|---|
| 1 | 120 | 2 | >164 |
| 2 | 154 | 15 | 12 |
| 21 | 60 | 19 | 8.8 |
| 22 | 74 | 14 | 28 |
| 23 | 85 | 16 | 15 |
| 26 | 154 | 11 | 141 |
| 27 | 128 | 4 | 140 |
See the Supporting Information for the assay protocol.
Permeability measured according to a published procedure.36