Inhibitory properties of PF-3644022 against recombinant MK2 enzyme and other MAPKAP kinase family members
Data are expressed as mean values ± S.E.M. for multiple independent experiments as indicated by n or for duplicate experiments with MAPKAP kinase family members.
| Kinase | Property | Result |
|---|---|---|
| MK2 | IC50 (nM) | 5.2 ± 1.9 (n = 13) |
| MK2 | Ki (nM) | 3.0 ± 1.0 (n = 6) |
| MK2 | Binding Kd (nM) | 5.9 ± 3.8 (n = 3) |
| MK2 | kon (M−1s−1) | 2.1e6 ± 0.3e6 |
| MK2 | koff (s−1) | 1.26 ± 0.17 |
| MK2 | t1/2 (s) | 146 ± 51 |
| MAPKAP | IC50 (nM) | |
| MK3 | 53 | |
| PRAK | 5 | |
| MNK1 | 3000 | |
| MNK2 | 148 | |
| MSK1/2 | >1000 | |
| RSK1/2/3/4 | >1000 |