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Assay Detail

CHEMBL5215207

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

Binding
Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)
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

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 5 7.10 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220061 1 8.12
CHEMBL5218879 1 8.05
CHEMBL4228518 1 6.94
CHEMBL5206476 1 5.28
CHEMBL321494 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220061 IC50 = 7.64 nM 8.12
CHEMBL5218879 IC50 = 8.83 nM 8.05
CHEMBL4228518 IC50 = 114.0 nM 6.94
CHEMBL5206476 IC50 = 5300.0 nM 5.28
CHEMBL321494 IC50 > 149.0 nM -