Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0004827
PMID	8667360
Assay Used	Membrane receptor Autophosphorylation Assays in 3T3 Cells
Experimently Validated	Yes
EGFR (IC₅₀)	6500 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 paper describes the Tyrphostins as Potent Inhibitors of Platelet-Derived Growth Factor Receptor Tyrosine Kinase and Structure-Activity Relationships in Quinoxalines, Quinolines,and Indole Tyrphostins
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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