Skip to main content

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