Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000376
PMID 17416531
  Assay Used Enzyme assay at 1µM of ATP
  Experimently ValidatedYes
  EGFR (IC50)  0.6 nM
  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)-
  Kd (L858R)-
  Kd (T790M)-
  Kd (L858R/T790M)-
  Kd (Other mutation)-
  Note The paper describes the Dual Quinazoline-based irreversible kinase inhibitors EGFR and VEGFR-2.
  Extra 34.9nM(IC50 at 1 mM ATP)

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Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
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Activity against Receptor
  EGFR Yes
  HER2-
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFRCYS773
  HER2-
  HER4-