Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0001905
PMID 15711537
  Assay Used Kinase assay
  Experimently ValidatedYes
  EGFR (IC50)  17 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)9.5 nM
  Kd (L858R)8.7 nM
  Kd (T790M)-
  Kd (L858R/T790M)-
  Kd (Other mutation)7.9 nM( L747-S752del P753S),12 nM( L747-E749del A750P),8.9 nM( L747-T751del insS),11 nM( L861Q),9.6 nM( G719C),4.8 nM( E746-A750del),5.9 nM( G719S),12 nM( S752-I759del)
  Note The paper presents A small molecule kinase interaction map for clinical 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
  HER2Yes
  HER4-
  Wild typeYes
  MutantL858R(Ka -value only)

Inhibitor Binding
  EGFR-
  HER2-
  HER4-