Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0000649
PMID	17062696
Assay Used	Recombinant protein Kinases, aswell as in cell proliferation assays
Experimently Validated	Yes
EGFR (IC₅₀)	22 /L nM
HER2 (IC₅₀)	32 nM
HER4 (IC₅₀)	190 nM
Mutant L858R (IC₅₀)	-
Mutant T790M (IC₅₀)	-
Double Mutant (IC₅₀)	-
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 Preclinical Antitumor Activity of BMS-599626 Kinase Inhibitor That Inhibits HER1/HER2 Homodimer and Heterodimer Signaling.
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['IC80_cell_assay']."

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" .$row2['ED50']."

" .$row2['ED50_CONVERTED']."

" .$row2['GI50_cell_assay']."

" .$row2['GI50_SIGN']." ".$row2['GI50_CONVERTED']."

" .$row2['GI90_CELL_ASSAY']."

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" .$row2['KD_CELL_ASSAY']."

" .$row2['KD_CELL_ASSAY_CONVERTED']."

" .$row2['per_Inhibition_Cellular']."

" .$row2['Inhibition_conc3']."

" .$row2['Cell_lines_used']."