Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000006
PMID 16475937
  Assay Used Cell-free In vitro Kinase assays and Cellular assay
  Experimently ValidatedYes
  EGFR (IC50)  0.3 nM
  HER2 (IC50)  30 nM
  HER4 (IC50)  -
  Mutant L858R (IC50)  0.4 nM
  Mutant T790M (IC50)  26 nM
  Double Mutant (IC50)  -
  Average ERBB2 and ERBB1 (IC50) -
  Inhibition EGFR (%) -
  Inhibitory Concentration -
  Inhibition HER2 (%) -
  Inhibitory Concentration -
  Ki (EGFR)-
  Ki (HER2)-
  Ki (HER4)-
  Kd (EGFR)-
  Kd (L858R)-
  Kd (T790M)-
  Kd (L858R/T790M)-
  Kd (Other mutation)-
  Note The paper describes the BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1H1666- 198 nM -- -- ----
2H3255- 1 nM -- -- ----
3NCI1975- 101 nM -- -- ----

Activity against Receptor
  EGFR Yes
  HER2Yes
  HER4-
  Wild typeYes
  MutantL858R , L858R/T790M

Inhibitor Binding
  EGFRCYS773
  HER2CYS805
  HER4-