Table 3.
Thermal shift data of front-pocket SAR for selected kinases.a
| ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ΔTm [K] | ||||||||||||
| Cpd. | Front pocket | EPH | FGFR1 | FGFR2 | FLT1 | GAK | Selectivitya | |||||
| A2 | A4 | A5 | A7 | B1 | B3 | |||||||
| Ref. b | 6.4 | 6.2 | 7.6 | 10.5 | 6.4 | 6.1 | 6.3 | 8.3 | 10.2 | 8.4 | ||
| 23 |
|
8.1 | 3.6 | 5.4 | 0.3 | 4.3 | 5.6 | 3.3 | 4.4 | 6.3 | 6.6 | 11/98 |
| 73 |
|
7.6 | 3.6 | 5.5 | 2.0 | 4.2 | 6.1 | 2.7 | 3.0 | −1.3 | 6.4 | 8/99 |
| 74 |
|
6.3 | 5.1 | 5.0 | 1.6 | 2.5 | 1.6 | 1.9 | 3.6 | 2.4 | 8.1 | 8/100 |
| 75 |
|
6.5 | 4.4 | 4.7 | 1.0 | 3.1 | 1.6 | 2.0 | 3.4 | 1.3 | 7.5 | 6/100 |
| 76 |
|
9.8 | 5.3 | 6.7 | 2.9 | 4.3 | 6.0 | 3.1 | 4.0 | 3.6 | 3.6 | 16/98 |
| 78 |
|
7.9 | 3.3 | 4.7 | 0.3 | 3.5 | 4.2 | 1.9 | 3.0 | 3.0 | 8.0 | 7/99 |
| 79 |
|
8.1 | 4.5 | 5.4 | 1.0 | 2.6 | 3.1 | 2.5 | 4.5 | 1.8 | 8.7 | 10/101 |
| 80 |
|
2.4 | 1.6 | 2.3 | 0.4 | 1.0 | 1.4 | 0.5 | 1.3 | 0.3 | 3.7 | 2/98 |
| 81 |
|
3.5 | 2.3 | 3.9 | 0.7 | 1.5 | 2.5 | 0.7 | 1.5 | 0.8 | 6.3 | 3/97 |
| 82 |
|
6.9 | 3.7 | 4.6 | 1.0 | 4.2 | 4.8 | 2.1 | 3.2 | 3.0 | 9.0 | 12/98 |