Table 4. Binding Affinities and Selectivities for Hsp90α > Hsp90β Obtained by FP Assaya.
| IC50 (μM) |
||||
|---|---|---|---|---|
| compd | n | Hsp90α | Hsp90β | fold selectivity |
| 23a | 0 | 3.87 ± 0.32 | 39.32 ± 2.64 | ∼10 |
| 23b | 1 | 3.84 ± 0.31 | >50 | >13 |
| 23c | 2 | 3.03 ± 0.19 | >50 | >13 |
| 23d | 3 | 0.25 ± 0.01 | 3.67 ± 0.14 | ∼15 |
| 23e | 4 | 0.33 ± 0.87 | 4.28 ± 0.07 | ∼13 |
| KUNA-111 | 3 | 0.25 ± 0.01 | 3.79 ± 0.18 | ∼15 |
IC50 values are reported as the mean of triplicates ± SD.