Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.

Afatinib E-isomer is an irreversible inhibitor of dual EGFR and HER2 that shows obvious activitives of EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM respectively.

Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.

AST-1306 p-toluenesulfonic acid is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

TAK-285 is a dual HER2 and EGFR (HER1) inhibitor with IC50 of 17 nM and 23 nM, > 10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.

AST-1306 is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.

AZ5104 is an irreversible inhibitor of EGFR-L858R/T790M, EGFR-L858R, EGFR-L861Q, and EGFR (IC50s of < 1 nM, 6 nM, 1 nM, and 25 nM respectively). AZ5104 is the demethylated metabolite of AZD-9291.

AEE788 is an inhibitor of both EGFR and VEGFR, the IC50s for EGFR and ErbB2 is 2 nM, 6 nM respectively.

AC480 is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, > 100-fold to VEGFR2, c-Kit, Lck, MET etc.