Table 10.
Optimization of compounds based on QSAR.
| |||||||
|---|---|---|---|---|---|---|---|
| Name | R | X1 | X2 | TLK2 IC50 (nM) | FLT3(%) | TRKC (%) | TLK1(%) |
| 128 | Me | N | C-H | 18 | 24 | 35 | 84 |
| 129 | H | C-H | N | 2600 | 87 | 86 | 92 |
8-point dose response (n=1);
percentage inhibition at 0.5 μM (n=2)
Optimization of compounds based on QSAR.
| |||||||
|---|---|---|---|---|---|---|---|
| Name | R | X1 | X2 | TLK2 IC50 (nM) | FLT3(%) | TRKC (%) | TLK1(%) |
| 128 | Me | N | C-H | 18 | 24 | 35 | 84 |
| 129 | H | C-H | N | 2600 | 87 | 86 | 92 |
8-point dose response (n=1);
percentage inhibition at 0.5 μM (n=2)