Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0000787
PMID	16483772
Assay Used	Autophosphorylation assay and cellular proliferation assays
Experimently Validated	Yes
EGFR (IC₅₀)	74 nM
HER2 (IC₅₀)	140 nM
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 alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
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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