Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0002877
PMID	8145236
Assay Used	Tyrosine Kinase activity associated with EGFR was evaluated using ER 22 cell membranes as an enzyme source and the tridecapeptide RR-Src (RRLIEDAEYAARG) as the phosphoryl-acceptor substrate
Experimently Validated	Yes
EGFR (IC₅₀)	27000 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 5-[(2,5-Dihydroxybenzyl)amino]salicylate Inhibitors of EGF-Receptor
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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