Table 2.
IC50 values of heterocyclic derivatives against Hsp90α and Hsp90β determined using fluorescence polarization (FP) assay.
Entry | Compound | HSP90β [IC50 in μM] | HSP90α [IC50 in μM] | Selectivity |
---|---|---|---|---|
1 | KUNB31 [a] | 0.18 ± 0.01 | 9.55 ± 1.08 | > 50 |
2 | 5 | 0.27 ± 0.09 | > 100 | > 370 |
3 | 18 | > 100 | > 100 | NA |
4 | 19 | > 100 | > 100 | NA |
5 | 20 | > 100 | > 100 | NA |
6 | 21 | 0.45 ± 0.15 | 2.22 ± 0.19 | 4.9 |
7 | 29a | > 100 | > 100 | NA |
8 | 29 b | 0.15 ± 0.04 | 0.79 ± 0.14 | >5 |
9 | 31 | 5.23 ± 0.13 | > 100 | > 19.1 |
10 | 32a | 8.29 ± 0.17 | > 100 | >12 |
11 | 32b | 1.86 ± 0.11 | > 100 | > 53 |
12 | 40 | 8.83 ± 1.48 | > 100 | >11 |
13 | 41 | > 100 | > 100 | NA |
14 | 42 | 0.34 ± 0.01 | 2.42 ± 0.07 | 7.1 |
15 | 43 | 18.19 ± 1.3 | > 100 | >5 |
16 | 44 | 19.59 ± 2.2 | > 100 | >5 |
17 | 45 | > 100 | > 100 | NA |
18 | 46 | > 100 | > 100 | NA |
19 | 50 | 6.75 ± 0.01 | 43.13 ± 11.5 | >5 |
20 | 51 | > 100 | > 100 | NA |
21 | 52 | > 100 | > 100 | NA |
22 | 59a | > 100 | > 100 | NA |
23 | 59 b | > 100 | > 100 | NA |
KUNB31 IC50 values were taken from Ref. [27].