Table 3. Binding Affinities and Selectivities for Hsp90α > Hsp90β Obtained by FP Assay.
| IC50 (μM)a |
|||
|---|---|---|---|
| compd | Hsp90α | Hsp90β | fold selectivity |
| 20a | 0.480 ± 0.05 | 4.57 ± 0.07 | ∼10 |
| 20b | 0.184 ± 0.02 | 2.40 ± 0.39 | ∼13 |
| 20c | 0.229 ± 0.01 | 2.07 ± 0.08 | ∼8 |
| 20d | 11.81 ± 0.87 | >50 | >5 |
| 20e | 4.60 ± 0.87 | >50 | ∼10 |
| 20f | 0.596 ± 0.03 | 5.16 | ∼10 |
| 20g | 0.447 ± 0.02 | 4.98 ± 0.29 | ∼10 |
| 20h | 2.49 ± 0.25 | 30.5 ± 2.3 | ∼12 |
| 20i | 2.22 ± 0.21 | >50 | ∼21 |
| 20j | 0.045 ± 0.02 | 0.426 ± 0.07 | ∼10 |
| 21 | 3.71 ± 0.25 | 17.94 ± 2.80 | ∼5 |
a
IC50 values are reported as the mean of triplicates ± SD.