Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0004577
PMID 22339342
  Assay Used FRET-based Z'-Lyte assay and MTT assay
  Experimently ValidatedYes
  EGFR (IC50)  1.16 nM
  HER2 (IC50)  -
  HER4 (IC50)  -
  Mutant L858R (IC50)  1.08 nM
  Mutant T790M (IC50)  6.56 nM
  Double Mutant (IC50)  3.14 nM
  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 Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 ? Methionine790 Mutant
  Extra 1.21nM(EGFR-L861Q)

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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
  MutantT790M,L858R,L861Q,L858R/T790M,Del E746_A750

Inhibitor Binding
  EGFRCYS797
  HER2-
  HER4-