Table 6. Profiles of Hit Bicycle 10 Versus Partially Optimized Lead 45 and Final Optimized Bicycle 58.
| in vitro
plasma stability (t 1/2, h) |
|||||
|---|---|---|---|---|---|
| Bicycle number | affinity Ki (nM) | solubility phosphate buffer pH 7.4 (mg/mL) | mouse | human | CHIlogP |
| 10 | 17.6 | 0.16 | 1.9 | >24 | 4.07 |
| 45 | 8.9 | 0.50 | >24 | >24 | 2.12 |
| 58 | 2.8 | 4.6 | >24 | >24 | 1.50 |