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Table 1 EGFR allosteric inhibitors

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
11 [100, 101] EGFRL858R/T790M
IC50 = 1 nmol/L
EGFRL858R/T790M/C797S
IC50 = 5 nmol/L
Phe856
12 [100, 101] EGFRL858R/T790M
IC50 = 3 nmol/L
EGFRL858R/T790M/C797S
IC50 = 4 nmol/L
Phe856