TABLE 1
Kinetic constants for CYP3A4 time-dependent inactivation by dasatinib analogs
Dasatinib Analogs: Modification of Piperazine and Methylpyrimidine | ||||||
|---|---|---|---|---|---|---|
 | ||||||
| Compound | R | KI | kinact | |||
| μM | min-1 | |||||
| Dasatinib |
| 6.3 | 0.034 | |||
| 984 |
| 15.8 | 0.038 | |||
| 1920 |
| 4.5 | 0.027 | |||
| 1235 |
| 11.9 | 0.022 | |||