Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0001050
PMID 11495584
  Assay Used Autophosphorylation of EGFR and HER-2 Kinases using a solid-phase ELISA assay and Cell Growth Inhibitory Activity
  Experimently ValidatedYes
  EGFR (IC50)  59 nM
  HER2 (IC50)  122 nM
  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 6-Substituted-4-(3-bromophenylamino)quinazolines as Putative Irreversible Inhibitors of the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor (HER-2) Tyrosine Kinases.
  Extra -

'; echo "" ; echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; echo "" ; echo "" ; #echo "" ; echo ''; } if($j%2==0){ echo ''; echo "" ; echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; #echo "" ; echo "" ; echo "" ; echo "" ; #echo "" ; echo ''; } $j++; } echo ''; echo ''; echo "" ; echo ''; mysql_free_result($result2); ?>
Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
" .$j."" .$row2['Cell_Line']."" .$row2['Cell_line_desc']."" .$row2['IC50_cell_assay']."" .$row2['IC50_SIGN']." ".$row2['IC50_CONVERTED']."" .$row2['IC80_cell_assay']."" .$row2['IC80_SIGN']." ".$row2['IC80_CONVERTED']."" .$row2['ED50']."" .$row2['ED50_CONVERTED']."" .$row2['GI50_cell_assay']."" .$row2['GI50_SIGN']." ".$row2['GI50_CONVERTED']."" .$row2['GI90_CELL_ASSAY']."" .$row2['GI90_CELL_ASSAY']."" .$row2['EC50_cell_assay']."" .$row2['EC50_SIGN']." ".$row2['EC50_CONVERTED']."" .$row2['KD_CELL_ASSAY']."" .$row2['KD_CELL_ASSAY_CONVERTED']."" .$row2['per_Inhibition_Cellular']."" .$row2['Inhibition_conc3']."" .$row2['Cell_lines_used']."
" .$j."" .$row2['Cell_Line']."" .$row2['Cell_line_desc']."" .$row2['IC50_cell_assay']."" .$row2['IC50_SIGN']." ".$row2['IC50_CONVERTED']."" .$row2['IC80_cell_assay']."" .$row2['IC80_SIGN']." ".$row2['IC80_CONVERTED']."" .$row2['ED50']."" .$row2['ED50_CONVERTED']."" .$row2['GI50_cell_assay']."" .$row2['GI50_SIGN']." ".$row2['GI50_CONVERTED']."" .$row2['GI90_CELL_ASSAY']."" .$row2['GI90_CELL_ASSAY']."" .$row2['EC50_cell_assay']."" .$row2['EC50_SIGN']." ".$row2['EC50_CONVERTED']."" .$row2['KD_CELL_ASSAY']."" .$row2['KD_CELL_ASSAY_CONVERTED']."" .$row2['per_Inhibition_Cellular']."" .$row2['Inhibition_conc3']."" .$row2['Cell_lines_used']."

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

Inhibitor Binding
  EGFRCYS773
  HER2CYS805
  HER4-