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Assay Detail

CHEMBL4186285

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

Binding
Inhibition of recombinant human EGFR d746-750/T790M/C797S mutant using poly-Glu-Tyr (4:1) as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.
Chen L, Fu W, Zheng L, Liu Z, Liang G.
J Med Chem (2018) 61 : 4290 -4300
PubMed 29136465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.40 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218431 1 7.77
CHEMBL4207984 1 7.64
CHEMBL4214588 1 7.34
CHEMBL1328065 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218431 IC50 = 17.0 nM 7.77
CHEMBL4207984 IC50 = 23.0 nM 7.64
CHEMBL4214588 IC50 = 46.0 nM 7.34
CHEMBL1328065 IC50 = 149.0 nM 6.83