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Assay Detail

CHEMBL3789506

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

Binding
Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Recent progress on third generation covalent EGFR inhibitors.
Cheng H, Nair SK, Murray BW.
Bioorg Med Chem Lett (2016) 26 : 1861 -1868
PubMed 26968253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.90 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3663929 NAQUOTINIB 3.0 1 8.10
CHEMBL3786343 OLMUTINIB 4.0 1 8.00
CHEMBL3787344 NAZARTINIB 2.0 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3663929 NAQUOTINIB IC50 = 8.0 nM 8.10
CHEMBL3786343 OLMUTINIB IC50 = 10.0 nM 8.00
CHEMBL3787344 NAZARTINIB IC50 = 25.0 nM 7.60