Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0000003
PMID	21732342
Assay Used	Kinase and Cellular assay
Experimently Validated	Yes
EGFR (IC₅₀)	52.2 nM
HER2 (IC₅₀)	36.3 nM
HER4 (IC₅₀)	> 1000 nM
Mutant L858R (IC₅₀)	-
Mutant T790M (IC₅₀)	> 1000 nM
Double Mutant (IC₅₀)	> 1000 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 antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models
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']."

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" .$row2['ED50']."

" .$row2['ED50_CONVERTED']."

" .$row2['GI50_cell_assay']."

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" .$row2['KD_CELL_ASSAY']."

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" .$row2['per_Inhibition_Cellular']."

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" .$row2['Cell_lines_used']."