Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0001982
PMID	18182285
Assay Used	ErbB2 and EGFR isolated enzyme Kinase assays and cellular erbB2 Autophosphorylation assay in an MCF-7 cells
Experimently Validated	Yes
EGFR (IC₅₀)	1430 nM
HER2 (IC₅₀)	5 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 new novel 4-anilino-1H-pyrazolo[3,4-d]pyrimidines as potent erbB2 and EGFR 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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