Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0004827
PMID 8667360
  Assay Used Membrane receptor Autophosphorylation Assays in 3T3 Cells
  Experimently ValidatedYes
  EGFR (IC50)  6500 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 Tyrphostins as Potent Inhibitors of Platelet-Derived Growth Factor Receptor Tyrosine Kinase and Structure-Activity Relationships in Quinoxalines, Quinolines,and Indole Tyrphostins
  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
  HER2-
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-