Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0001581
PMID 18842405
  Assay Used Enzyme and cell assays
  Experimently ValidatedYes
  EGFR (IC50)  50 nM
  HER2 (IC50)  20 nM
  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 novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines based dual EGFR/ErbB-2 inhibitors.
  Extra 17%( % covalent modification of EGFR after 3 h.)

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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
  EGFR-
  HER2-
  HER4-