Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000010
PMID 16279804
  Assay Used Enzymatic assay
  Experimently ValidatedYes
  EGFR (IC50)  0.66 ± 0.12 nM
  HER2 (IC50)  143 ± 52 nM
  HER4 (IC50)  49 ± 16 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 describes the Anilinodialkoxyquinazolines as Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Potential Tumor Imaging Probes
  Extra 2.6 ± 0.5nM(receptor phosphorylation)
Molecule Id EGIN0000010
PMID 16279804
  Assay Used Enzymatic assay
  Experimently ValidatedYes
  EGFR (IC50)  0.029 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 Anilinodialkoxyquinazolines as Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Potential Tumor Imaging Probes
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1-- - -- -- ----
2-- - -- -- ----

Activity against Receptor
  EGFR Yes
  HER2Yes
  HER4Yes
  Wild typeYes
  Mutant-
  EGFR Yes
  HER2Yes
  HER4Yes
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-