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Assay Detail

CHEMBL5259686

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

Binding
Inhibition of wild type EGFR (unknown origin) pre-incubated for 10 mins followed by substrate addition measured after 60 mins in presence of ATP by mobility shifting 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

Synthesis and evaluation of sulfonamide derivatives targeting EGFR<sup>790M/L858R</sup> mutations and ALK rearrangement as anticancer agents.
Cao L, Yao H, Yu L, Ren Y, Liu J, Li X, Jia X.
Bioorg Med Chem (2023) 85 : 117241 -117241
PubMed 37087886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.52 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173655 AFATINIB 4.0 1 10.10
CHEMBL3353410 OSIMERTINIB 4.0 1 7.83
CHEMBL5284780 1 7.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173655 AFATINIB IC50 = 0.08 nM 10.10
CHEMBL3353410 OSIMERTINIB IC50 = 14.67 nM 7.83
CHEMBL5284780 IC50 = 23.25 nM 7.63