Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0003171
PMID	16249085
Assay Used	Enzyme assay
Experimently Validated	Yes
EGFR (IC₅₀)	5200 nM
HER2 (IC₅₀)	5000 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 papse describes the Pyrazoloheteroaryls as novel p38a MAP kinase inhibiting scaffolds with oral activity
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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