From: Emerging strategies to overcome resistance to third-generation EGFR inhibitors
Compound (reference) | Structure | Activity | Interaction with EGFR allosteric site |
---|---|---|---|
7, DDC4002 [100] |
| EGFRL858R/T790M IC50 = 10 nmol/L EGFRL858R/T790M/C797S IC50 = 59 nmol/L | Phe856 |
8 [100] |
| EGFRL858R/T790M/C797S IC50 = 19 nmol/L | Phe856 |
9 [100] |
| EGFRL858R/T790M/C797S IC50 = 23 nmol/L | Phe856 |
10 [100] |
| EGFRL858R/T790M/C797S IC50 = 13 nmol/L | Phe856 |
| EGFRL858R/T790M IC50 = 1 nmol/L EGFRL858R/T790M/C797S IC50 = 5 nmol/L | Phe856 | |
| EGFRL858R/T790M IC50 = 3 nmol/L EGFRL858R/T790M/C797S IC50 = 4 nmol/L | Phe856 |