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Assay Detail

CHEMBL5620517

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

Binding
Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) expressed in Bac-to-Bac baculovirus expression system measured after 2 hrs by ELISA method
5
Total Activities
5
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

Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy.
Xu L, Xu B, Wang J, Gao Y, He X, Xie T, Ye XY.
Eur J Med Chem (2023) 245 : 114900 -114900
PubMed 36417820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.22 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5624606 1 9.55
CHEMBL5190294 1 8.51
CHEMBL4294743 1 8.24
CHEMBL4214567 1 7.89
CHEMBL4098072 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5624606 IC50 = 0.28 nM 9.55
CHEMBL5190294 IC50 = 3.1 nM 8.51
CHEMBL4294743 IC50 = 5.8 nM 8.24
CHEMBL4214567 IC50 = 13.0 nM 7.89
CHEMBL4098072 IC50 = 130.0 nM 6.89