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SAR exploration of the R1/R2 positions.
| |||||
|---|---|---|---|---|---|
| Compd. | R1 | R2 | BaF3-TEL-c-KIT (GI50: μM) |
BaF3-TEL-c-KIT-T670I (GI50: μM) |
BaF3 (GI50: μM) |
| I |
|
|
0.4 ± 0.011 | 2.7 ± 0.058 | >10 |
| 22a |
|
|
0.12 ± 0.016 | 0.071 ± 0.0011 | 1.5 ± 0.17 |
| 33 |
|
|
>10 | >10 | >10 |
| 22b |
|
|
>10 | >10 | >10 |
| 27 |
|
|
0.34 ± 0.01 | >10 | >10 |
