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Assay Detail

CHEMBL4186281

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

Binding
Inhibition of N-terminal GST-fused human EGFR cytoplasmic domain T790M/C797S mutant expressed in baculovirus expression system using TK-substrate after 20 mins by HTRF KinEASE-TK assay
3
Total Activities
3
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 3 8.66 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095447 1 8.72
CHEMBL4094959 1 8.60
CHEMBL4090601 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095447 IC50 = 1.9 nM 8.72
CHEMBL4094959 IC50 = 2.5 nM 8.60
CHEMBL4090601 IC50 < 1.0 nM -