Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0004923
PMID 22888144
  Assay Used Kinase and Cellular assay
  Experimently ValidatedYes
  EGFR (IC50)  0.8 nM
  HER2 (IC50)  84 nM
  HER4 (IC50)  544 nM
  Mutant L858R (IC50)  1 nM
  Mutant T790M (IC50)  -
  Double Mutant (IC50)  57 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 target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker.
  Extra -

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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
  HER2Yes
  HER4Yes
  Wild typeYes
  MutantL858R,L858R/T790M

Inhibitor Binding
  EGFR-
  HER2-
  HER4-