TABLE 4
Hydrolysis of amino acid ester derivatives of p38 MAP kinase, IκB-K2 kinase, and HSP-90 inhibitors by hCE-1+ve and hCE-1−ve cell lysates
| Compound | Structure | R | Target Protein | Enzyme Potency of Parent or Acid Product (IC50)* | Ester Hydrolysis by Cell Lysates** | |
|---|---|---|---|---|---|---|
| U-937 (hCE-1+ve) | HuT-78 (hCE-1−ve) | |||||
| nM | pg/ml/min | |||||
| CHR-3464 |  | H | p38 MAP kinase | 2 | Not applicable | |
| CHR-5623 |  | p38 MAP kinase | 1 | 3036 ± 69 | 0 | |
| CHR-5805 |  | H | IκB-K2 kinase | 23 | Not applicable | |
| CHR-5250 |  | IκB-K2 kinase | 26 | 12150 ± 60 | 0 | |
| CHR-6907 |  | H | HSP-90 | 7 | Not applicable | |
| CHR-6576 |  | HSP-90 | 3 | 8100 ± 122 | 13 + 13 | |
* Values shown are the means derived from at least four individual experiments.
** Values shown are means ± S.D.