Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0000214
PMID	10753475
Assay Used	Inhibition of phos-phorylation of a random glutamic acid/tyrosine copolymer substrate by isolated EGFR enzyme, inhibition of EGF-stimulated Autophosphorylation of EGFR in A431 cells
Experimently Validated	Yes
EGFR (IC₅₀)	3 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	-
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 ppaer describes the Irreversible Inhibitors of the Epidermal Growth Factor Receptor 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides.
Extra	Isolated enzyme IC50 Values are the averages from at least two independent dose response curves; variation was generally 15%

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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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