Table 1.
Inhibitory activity of DAP p38 inhibitors on various targets
| Targets | IC50, μmol/l | |||
|---|---|---|---|---|
| SC74102 | SC79659 | SC79409 | SD0006 | |
| Ab-l | >10 | >10 | >10 | >30 |
| Akt-1 | >10 | >10 | >10 | >30 |
| ASK-1 | >10 | |||
| Aur-2 | >10 | >10 | ||
| CDC-7 | >10 | >10 | ||
| CDK-2 | 21.1 | >100 | >200 | >30 |
| CHK-1 | >10 | >10 | >10 | >30 |
| CK1δ | <1 | <1 | 0.017 | 0.029 |
| CK2α | >10 | >10 | >10 | >30 |
| EGFR-1 | <1 | <1 | <1 | 0.101 |
| ERK-2 | >100 | >100 | >100 | >200 |
| FGFR-1 | >10 | >10 | >10 | >30 |
| GSK3β | >10 | >10 | >10 | >30 |
| IGFR-1 | >10 | >10 | ||
| IKK-1 | >200 | >100 | >100 | >200 |
| IKK-2 | >200 | >100 | >100 | >200 |
| IKKi | >100 | >100 | >100 | >30 |
| IR | >10 | >10 | ||
| JNK-1 | 21.5 | 59.4 | >200 | >50 |
| JNK-2 | 1.35 | 2.75 | 19.7 | 9.7 |
| JNK-3 | 3.67 | 1.85 | 69.7 | >3.1 |
| Kit | >10 | |||
| Lck | >10 | >10 | >30 | >30 |
| Lyn | 2.0 | >10 | >10 | |
| MAPKAP-K2 | >10 | >10 | >200 | >200 |
| Met | >10 | >10 | >10 | >30 |
| MK-3 | >100 | >100 | >200 | >200 |
| MKK-1 | >10 | |||
| MKK-6 | >10 | |||
| MKK-7 | >10 | |||
| MNK | 6.42 | >100 | >200 | >200 |
| MSK | >200 | >200 | ||
| Nim | >10 | >10 | ||
| p38α | 0.382 | 0.111 | 0.048 | 0.016 |
| p38β | 5.08 | 1.79 | 2.32 | 0.677 |
| p38γ | >100 | >100 | >100 | >100 |
| p38δ | >100 | >100 | >100 | >100 |
| PAK-4 | >10 | >10 | >10 | >30 |
| PDGFR | >10 | >10 | ||
| PDK-1 | >10 | >10 | >10 | >30 |
| PKA | <10 | >10 | 10.5 | 3.69 |
| PKCα | >40 | |||
| PKCβ | >10 | >10 | >10 | 23.5 |
| PKCζ | >10 | >10 | >30 | >29 |
| PLK-1 | >10 | >10 | ||
| PRAK | >100 | >100 | >200 | >200 |
| Ret | >10 | >10 | ||
| RSK-2 | 40.7 | >100 | >100 | |
| RSKb | >200 | 199 | ||
| STLK-2 | >10 | >10 | ||
| SULU | >10 | >10 | ||
| TBK-1 | >100 | >100 | >100 | |
| TRKA | >10 | >10 | >10 | >30 |
| VEGFR-2 | >10 | >10 | >10 | >10 |
| VEGFR-3 | >10 | >10 | ||
| ZAP-70 | >10 | >10 | >10 | |
| COX-1 | >100 | >10 | >500 | >100 |
| COX-2 | >100 | >10 | >500 | >100 |