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Assay Detail

CHEMBL5215220

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

Binding
Inhibition of human EGFR del19/T790M/C797S mutant using ATP-labelled peptide substrate by HTRF 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 Autocuration

Target

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

Publication

The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.
He J, Zhou Z, Sun X, Yang Z, Zheng P, Xu S, Zhu W.
Eur J Med Chem (2021) 210 : 112995 -112995
PubMed 33243531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.50 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5172794 1 9.70
CHEMBL5176129 1 9.70
CHEMBL5187838 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5172794 IC50 = 0.2 nM 9.70
CHEMBL5176129 IC50 = 0.2 nM 9.70
CHEMBL5187838 IC50 = 0.8 nM 9.10