Table 2. Preliminary Data of Thermodynamic Aqueous Solubility (μM) and Metabolic Stability (Residual Substrate %) of Selected PROTACs.
| compound | PBS 0.1 M (pH = 7.4) | HCl 0.01 N (pH = 2.0) | metabolic stabilitya,b (%) |
|---|---|---|---|
| 27 | 48 | 145 | 36 |
| 28 | 17 | 48 | 40 |
| 29 | 15 | 39 | 88 |
| 34 | 11 | 5073 | 60 |
| 37 | 8 | 18 | 89 |
| dBET1 | 60c | 171c | 66 |
Residual substrate after 1 h incubation in MLM in the presence of NADPH.
The residual substrate in control incubations without MLMs was >99%.
Literature data.58