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SAR exploration of the linker moiety (L).
| ||||
|---|---|---|---|---|
| Compd. | Linker (L) | BaF3 (GI50: μM) |
BaF3-Tel-c-KIT (GI50: μM) |
BaF3-Tel-c-KIT-T670I (GI50: μM) |
| Axitinib | - | 1.64 | 0.105 | 0.108 |
| 57a |
|
7.4 | 0.025 | 0.002 |
| 58a |
|
1.71 | 2.97 | 1.71 |
| 58b |
|
3.79 | 5.5 | 3.18 |
| 59 |
|
1.9 | 1.6 | 1.15 |
| 57b |
|
>10 | 1 | 0.23 |
