Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0001888
PMID 16777410
  Assay Used Inhibition of ErbB-1 and ErbB-2 tyrosine Kinase activity was evaluated in Enzyme assays using the purified recombinant human intracellular domain of each receptor and Cellular assay
  Experimently ValidatedYes
  EGFR (IC50)  -
  HER2 (IC50)  -
  HER4 (IC50)  -
  Mutant L858R (IC50)  -
  Mutant T790M (IC50)  -
  Double Mutant (IC50)  -
  Average ERBB2 and ERBB1 (IC50) 68 nM
  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 6-furanylquinazoline series of dual ErbB-1/ErbB-2 tyrosine kinase inhibitors
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1-- - -- -- ----

Activity against Receptor
  EGFR Yes
  HER2Yes
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-