Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000370
PMID 15993078
  Assay Used Phosphorylation of a peptide substrate in the presence of 10 µM inhibitor 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) -
  Inhibition EGFR (%) 21.10%
  Inhibitory Concentration 10 µM
  Inhibition HER2 (%) 7.20%
  Inhibitory Concentration % inhibition at 10 µM
  Ki (EGFR)-
  Ki (HER2)-
  Ki (HER4)-
  Kd (EGFR)-
  Kd (L858R)-
  Kd (T790M)-
  Kd (L858R/T790M)-
  Kd (Other mutation)-
  Note The paper describes the 5-substituted-4-hydroxy-8-nitroquinazolines as EGFR signaling inhibitors
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1MDA-MB-468- - -- -- --29.00%10 µM
2MDA-MB-468- 4200 nM -- -- ----
3SKBR3- 7000 nM -- -- ----

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

Inhibitor Binding
  EGFR-
  HER2-
  HER4-