Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0001225
PMID 16078851
  Assay Used Enzymatic assay and Cellular assay
  Experimently ValidatedYes
  EGFR (IC50)  0.07 ± 0.03 nM
  HER2 (IC50)  25-50 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 High-Affinity Epidermal Growth Factor Receptor (EGFR) Irreversible Inhibitors with Diminished Chemical Reactivities as Positron Emission Tomography (PET)-Imaging Agent Candidates of EGFR Overexpressing Tumors.
  Extra 5-15nM(DHER14-EGFR)

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1A431immediately after removal of the inhibitor 5 - 25 nM -- -- ----
2A4318h after removal of the inhibitor 25-50 nM -- -- ----

Activity against Receptor
  EGFR Yes
  HER2-
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFRCYS773
  HER2-
  HER4-