Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0000376
PMID	15711537
Assay Used	Kinase assay
Experimently Validated	Yes
EGFR (IC₅₀)	1 nM
HER2 (IC₅₀)	77 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)	0.44 nM
K_d (L858R)	0.41 nM
K_d (T790M)	-
K_d (L858R/T790M)	-
K_d (Other mutation)	0.27 nM( L747-S752del P753S),0.24 nM( L747-E749del A750P),0.23 nM( L747-T751del insS),0.44 nM( L861Q),0.24 nM( G719C),0.38 nM( E746-A750del),0.42 nM( G719S),0.33 nM( S752-I759del)
Note	The paper presents A small molecule kinase interaction map for clinical 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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