Table 1 Summary of in situ click chemistry experiments and dissociation constants.
Compound | In situ hita (HRAS) | In situ hita (c-kit2) |
|
|
|---|---|---|---|---|
9 | Yes | Yes | 6.0 | 1.8 |
10 | Yes | Yes | 5.6 | 2.0 |
11 | No | No | 8.0 | 4.8 |
12 | Yes | Yes | 7.1 | 2.7 |
13 | Yes | Yes | 12.9 | 4.3 |
14 | No | No | 25.9 | 3.1 |
15 | No | Yes | −b | 6.1 |
1 | − | − | 37.9 | 13.9 |
(μM)
(μM)