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Assay Detail

CHEMBL3609987

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of EGFR L858R/T790M double mutant in human H1975 cells assessed as inhibition of phosphorylation at Y1068 after 2 hrs by sandwich ELISA method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H1975
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of the Epidermal Growth Factor Receptor (EGFR) May Provide Effective Treatment for Lung Adenocarcinoma.
Abdel-Magid AF.
ACS Med Chem Lett (2015) 6 : 732 -733
PubMed 26191356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.34 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3608434 1 8.22
CHEMBL3608433 1 8.22
CHEMBL3608429 1 8.15
CHEMBL3608430 1 7.85
CHEMBL3608431 1 6.41
CHEMBL3608432 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3608434 IC50 = 6.0 nM 8.22
CHEMBL3608433 IC50 = 6.0 nM 8.22
CHEMBL3608429 IC50 = 7.0 nM 8.15
CHEMBL3608430 IC50 = 14.0 nM 7.85
CHEMBL3608431 IC50 = 387.0 nM 6.41
CHEMBL3608432 IC50 = 6138.0 nM 5.21