Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000005
PMID 17349580
  Assay Used fluorescence quenching assay
  Experimently ValidatedYes
  EGFR (IC50)  -
  HER2 (IC50)  -
  HER4 (IC50)  -
  Mutant L858R (IC50)  -
  Mutant T790M (IC50)  -
  Double Mutant (IC50)  -
  Average ERBB2 and ERBB1 (IC50) -
  Inhibition EGFR (%) -
  Inhibitory Concentration -
  Inhibition HER2 (%) -
  Inhibitory Concentration -
  Ki (EGFR)-
  Ki (HER2)-
  Ki (HER4)-
  Kd (EGFR)53.5±1.8 nM
  Kd (L858R)2.6±0.2 nM
  Kd (T790M)-
  Kd (L858R/T790M)-
  Kd (Other mutation)123.6±5.9 nM(G719S)
  Note The paper describes the Structures of lung cancer-derived EGFR mutants and inhibitor complexes: Mechanism of activation and insights into differential inhibitor sensitivity.
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.

Activity against Receptor
  EGFR Yes
  HER2-
  HER4-
  Wild typeYes
  MutantL858R,G719S

Inhibitor Binding
  EGFR-
  HER2-
  HER4-