Table 2.
Summary of apparent binding affinities of compounds with different electron withdrawing groups at C2 or with a cyclopentenone scaffold
| ERK2 Kiapp/µM | p38 Kiapp/µM | JNK1 Kiapp/µM | logP | ||
|---|---|---|---|---|---|
| 18 |  |
> 200 | 74.7 ± 14.0 | > 200 | 1.370 |
| 19 |  |
> 200 | 19.3 ± 3.1 | > 200 | 2.094 |
| 20 |  |
32.8 ± 2.7 | 42.2 ± 2.9 | 97.4 ± 24.1 | 1.771 |
| 21 |  |
71.4 ± 9.2 | 38.9 ± 6.2 | > 200 | 2.642 |
| 22 |  |
> 200 | 53.0 ± 11.1 | > 200 | 0.342 |
| 23 |  |
> 200 | 55.9 ± 6.5 | > 200 | 0.342 |
| 24 |  |
42.7 ± 3.6 | 21.2 ± 2.8 | 112.2 ± 32.7 | 1.909 |
| 25 |  |
135.7 ± 14.1 | 28.0 ± 2.4 | > 200 | 1.085 |
| 26 |  |
168.7 ± 8.7 | 27.4 ± 3.3 | > 200 | 2.254 |
| 27 |  |
37.2 ± 4.0 | 9.4 ± 2.1 | 2.1 ± 0.3 | 1.808 |
Data show the mean ± parameter error estimates from weighted least square method, see Supplementary Fig. 12; logP are calculated values.