Table 5.
SAR exploration focused on the L2/R1 moieties.
| |||||
|---|---|---|---|---|---|
| Compd. | L2 | R1 | Parental BaF3 (GI50: μM) |
BaF3-Tel-c-KIT (GI50: μM) |
BaF3-Tel-c-KIT-T670I (GI50: μM) |
| CHMFL-KIT-8140 | - | - | >10 | 0.057 | 0.063 |
| 35a |
|
|
>10 | >10 | >10 |
| 35b |
|
|
5.13 | 4.17 | 6.99 |
| 36 |
|
|
>10 | >10 | >10 |
| 35c |
|
|
2.16 | 0.022 | 0.001 |
| 35d |
|
|
1.89 | 0.020 | 0.001 |
| 35e |
|
|
1.0 | 0.923 | 0.342 |
| 35f |
|
|
2.78 | 0.293 | 0.339 |
| 35g |
|
|
1.03 | 0.024 | 0.013 |
| 35h |
|
|
5.97 | 0.001 | 0.004 |
| 35i |
|
|
7.26 | 0.017 | 0.014 |
| 35j |
|
|
6.42 | 0.027 | 0.015 |
| 35k |
|
|
4.13 | 0.319 | 0.179 |
| 35l |
|
|
0.67 | 0.312 | 0.309 |
| 35m |
|
|
2.03 | 0.342 | 0.037 |
| 35n |
|
|
6.70 | 0.424 | 0.309 |
| 35o |
|
|
1.93 | 2.78 | 1.70 |
| 35p |
|
|
0.704 | 0.040 | 0.285 |
| 35q |
|
|
3.10 | 0.11 | 0.167 |
| 35r |
|
|
6.23 | 0.112 | 0.034 |
| 35s |
|
|
2.47 | 0.635 | 0.362 |
| 35t |
|
|
8.70 | 7.33 | 8.52 |
| 43 |
|
|
6.18 | 2.90 | 0.668 |
| 44 |
|
|
10 | 2.35 | 4.61 |