Table 4.
SAR of the R3 position.
| ||||
|---|---|---|---|---|
| Compd. | R3 | BaF3-TEL-c-KIT (GI50: μM) |
BaF3-TEL-c-KIT-T670I (GI50: μM) |
BaF3 (GI50: μM) |
| 22c |
|
0.28 ± 0.025 | 0.92 ± 0.04 | 1.3 ± 0.17 |
| 22d |
|
0.11 ± 0.016 | 0.046 ± 0.001 | 7.1 ± 0.38 |
| 22e |
|
0.43 ± 0.01 | 0.34 ± 0.025 | >10 |
| 22f |
|
0.13 ± 0.01 | 0.58 ± 0.02 | 5 ± 1.0 |
| 22g |
|
0.12 ± 0.011 | 0.48 ± 0.011 | 3 ± 0.15 |
| 22h |
|
0.038 ± 0.001 | 0.053 ± 0.001 | 2.9 ± 0.17 |
| 22i |
|
0.76 ± 0.0057 | 0.76 ± 0.1 | 1.1 ± 0.47 |
| 22j |
|
0.02 ± 0.001 | 0.32 ± 0.025 | 7 ± 0.74 |
| 22k |
|
0.087 ± 0.0015 | 0.083 ± 0.021 | 2.9 ± 0.056 |
| 22l |
|
0.16 ± 0.01 | 0.081 ± 0.006 | 1.7 ± 01 |
| 22m |
|
0.039 ± 0.041 | 0.087 ± 0.008 | 1.3 ± 0.11 |
| 22n |
|
0.059 ± 0.001 | 0.23 ± 0.0001 | 3.4 ± 1.2 |
| 22o |
|
0.13 ± 0.0057 | 0.12 ± 0.02 | 0.8 ± 0.084 |
| 22p |
|
0.13 ± 0.001 | 0.17 ± 0.05 | 0.51 ± 0.15 |
| 22q |
|
0.46 ± 0.021 | 0.65 ± 0.076 | 4.0 ± 0.32 |
| 22r |
|
0.12 ± 0.0001 | 0.037 ± 0.009 | 0.48 ± 0.006 |
| 22s |
|
0.33 ± 0.015 | 0.2 ± 0.011 | 0.87 ± 0.068 |
| 22t |
|
0.44 ± 0.03 | 0.26 ± 0.052 | 7.6 ± 0.61 |
| 22u |
|
0.19 ± 0.021 | 0.2 ± 0.02 | 1.2 ± 0.11 |
| 22v |
|
0.042 ± 0.003 | 0.059 ± 0.006 | 3.6 ± 0.89 |
| 22w |
|
3.9 ± 0.023 | 3.8 ± 0.02 | >10 |
| 22x |
|
0.034 ± 0.002 | 0.33 ± 0.029 | 6.2 ± 0.38 |
| 22y |
|
0.059 ± 0.003 | 0.95 ± 0.04 | 4.2 ± 0.36 |
| 22z |
|
0.14 ± 0.021 | 0.063 ± 0.002 | 1.9 ± 0.058 |
| 22aa |
|
0.057 ± 0.0021 | 0.063 ± 0.001 | >10 |
| 22ab |
|
0.25 ± 0.06 | 0.46 ± 0.01 | 4.4 ± 1.37 |