Table 2. Representative SAR and Benzothiazole Ring System.
compd | R1 | R2 | X | Itk pKi | Lck pKi | AurB pKi |
---|---|---|---|---|---|---|
8 | Me | Me | C | <5a | <4.6 | 4.7 |
9 | H | H | C | 9.0 | 6.5 | 6.4 |
10 | Me | H | C | 9.4 | 6.6 | 6.5 |
11 | Cl | H | C | 9.5 | 7.1 | 6.6 |
12 | CF3 | H | C | 7.9a | 7.3 | 6.6 |
13 | Et | H | C | 9.2 | 7.0 | 6.4 |
14 | CN | H | C | 9.6 | 7.2 | 7.1 |
15 | OMe | H | N | 9.7 | 7.1 | 6.5 |
16 | H | H | N | 9.6 | 7.0 | 7.0 |
17 | Et | H | N | 8.8 | 7.0 | 7.2 |
pKi measured at low ATP concentration.21