Table 2.
In vitro inhibitory profiling of Lwk-n019 against human kinases
| Target | Lwk-n019 | Target | Lwk-n019 |
|---|---|---|---|
|
| |||
| Gene Symbol | % Ctrl | Gene symbol | Kd (µM) |
| ALK | 29 | ALK | 7.6 |
| ALK (C1156Y) | 31 | ALK (C1156Y) | 4.7 |
| ALK (L1196M) | 70 | ALK (L1196M) | 9.3 |
| CSNK1A1L | 26 | CSNK1A1L | 6.2 |
| CSNK2A1 | 25 | CSNK2A1 | 9.9 |
| FLT3 | 74 | FLT3 | 12 |
| FLT3 (D835H) | 32 | FLT3 (D835H) | 8.4 |
| FLT3 (N841I) | 57 | FLT3 (N841l) | 14 |
| FLT3 (D835V) | 3.2 | FLT3 (D835V) | 2.3 |
| FLT3 (D835Y) | 18 | FLT3 (D835Y) | 3.2 |
| FLT3 (ITD) | 12 | FLT3 (ITD) | 4.5 |
| FLT3 (ITD, D835V) | 0.85 | FLT3 (ITD, D835V) | 0.77 |
| FLT3 (ITD, F691L) | 25 | FLT3 (ITD, F691L) | 6.3 |
| MINK | 15 | MINK | 3.3 |
| MKNK2 | 31 | MKNK2 | 4.6 |
| MYLK | 17 | MYLK | 2.4 |
| STK33 | 31 | STK33 | 7.2 |
| PAK3 | 35 | ||
| PIM3 | 34 | ||
| ARK5 | 33 | ||
Lwk-N019 was screened at 10 µM. % Ctrl, results of primary screen binding interactions where lower numbers indicate stronger hits in the matrix. Kd, dissociation constant for Lwk-n019-kinase interactions.