Table 2.
Thermal shift data of 5’-trisubstituted cpds for selected kinases. The selectivity was determined as in Table 1.a
| ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ΔTm [K] | ||||||||||||
| Cpd. ID | 5’ | 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 |
| 56 |
|
6.9 | 2.8 | 5.0 | 0.4 | 3.3 | 3.9 | 2.7 | 3.6 | 3.4 | 7.3 | 7/101 |
| 57 |
|
6.0 | 2.2 | 2.9 | −0.3 | 2.2 | 2.4 | 0.8 | 1.2 | 0.7 | 5.9 | 3/101 |
| 58 |
|
8.8 | 4.9 | 5.4 | −2.5 | 5.6 | 4.8 | 5.2 | 5.8 | 8.8 | 6.8 | 14/100 |
| 59 |
|
5.0 | 1.2 | 1.9 | −3.3 | 2.7 | 2.3 | 2.2 | 2.9 | 3.0 | 4.1 | 1/100 |
| 60 |
|
7.5 | 3.2 | 5.7 | 0.1 | 3.3 | 4.3 | 3.1 | 4.7 | 4.3 | 5.8 | 18/99 |
| 61 |
|
9.8 | 4.7 | 6.0 | 0.4 | 4.9 | 5.8 | 2.7 | 3.4 | 3.0 | 9.3 | 14/99 |
| 62 |
|
6.2 | 2.6 | 3.5 | 0.5 | 3.2 | 0.0 | 2.4 | 3.6 | 2.7 | 4.9 | 3/99 |
| 63 |
|
9.5 | 3.8 | 5.6 | 0.4 | 3.5 | 5.4 | 4.5 | 5.7 | 5.4 | 6.5 | 9/99 |