Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0004275
PMID	19888761
Assay Used	Enzymatic and Cell proliferation assay
Experimently Validated	Yes
EGFR (IC₅₀)	13 nM
HER2 (IC₅₀)	42 nM
HER4 (IC₅₀)	< 100 nM
Mutant L858R (IC₅₀)	-
Mutant T790M (IC₅₀)	-
Double Mutant (IC₅₀)	24 nM
Average ERBB2 and ERBB1 (IC₅₀)	-
Inhibition EGFR (%)	-
Inhibitory Concentration	-
Inhibition HER2 (%)	-
Inhibitory Concentration	-
K_i (EGFR)	-
K_i (HER2)	-
K_i (HER4)	-
K_d (EGFR)	-
K_d (L858R)	-
K_d (T790M)	-
K_d (L858R/T790M)	-
K_d (Other mutation)	-
Note	The paper describes the Discovery of A Novel Her-1/Her-2 Dual Tyrosine Kinase Inhibitor for the Treatment of Her-1 Selective Inhibitor-Resistant Non-small Cell Lung Cancer.
Extra	-

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Cellular Activity

S.No.

Cell Line

Desp.

IC₅₀

IC₈₀

ED₅₀

GI₅₀

GI₉₀

EC₅₀

K_d

Inhibition (%)

Inhibitory Conc.

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" .$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['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']."