Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000215
PMID 10753475
  Assay Used Inhibition of phos-phorylation of a random glutamic acid/tyrosine copolymer substrate by isolated EGFR enzyme, inhibition of EGF-stimulated Autophosphorylation of EGFR in A431 cells
  Experimently ValidatedYes
  EGFR (IC50)  0.78 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 ppaer describes the Irreversible Inhibitors of the Epidermal Growth Factor Receptor 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides.
  Extra Isolated enzyme IC50 Values are the averages from at least two independent dose response curves; variation was generally 15%

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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
  HER2Yes
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFRCYS773
  HER2Yes
  HER4-