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Inhibitor dissociation constants for the WT and mutant EGFR kinases
| Kinase |
Kd, nM |
Kd /Km[ATP], ×10−3 |
||
|---|---|---|---|---|
| Gefitinib | AEE788 | Gefitinib | AEE788 | |
| WT | 35.3 ± 0.4 | 5.3 ± 0.3 | 6.8 | 1.0 |
| T790M | 4.6 ± 0.1 | 27.6 ± 0.7 | 0.78 | 4.7 |
| L858R | 2.4 ± 0.1 | 1.1 ± 0.1 | 0.016 | 0.0074 |
| L858R/T790M | 10.9 ± 0.6 | 18.6 ± 0.5 | 1.3 | 2.2 |
The ratio Kd /Km[ATP] provides a relative estimate of inhibitor potency.
