Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0003578
PMID 9240345
  Assay Used Kinase inhibition assay and RAVSMC growth delay assay
  Experimently ValidatedYes
  EGFR (IC50)  1360 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 Structure-Activity Relationships for a Novel Series of Pyrido[2,3-d]pyrimidine Tyrosine Kinase Inhibitors
  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
  HER2-
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-