Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000006
PMID 18667312
  Assay Used Kinase and Cellular assay
  Experimently ValidatedYes
  EGFR (IC50)  2.3 nM
  HER2 (IC50)  48 nM
  HER4 (IC50)  14 nM
  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 discuss the cross reactivity of irreversiable inhibitors of ErbB family PD168393,CI-1033
  Extra -

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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
  HER4Yes
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFRCYS773
  HER2-
  HER4-