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Assay Detail

CHEMBL5581451

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

Binding
Inhibition of EGFR T790M/L858R mutant (unknown origin)
4
Total Activities
4
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

Discovery of new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation.
Yao H, Ren Y, Wu F, Liu J, Li J, Cao L, Yan M, Li X.
Eur J Med Chem (2024) 275 : 116590 -116590
PubMed 38908104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.42 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353410 OSIMERTINIB 4.0 1 9.47
CHEMBL5590430 1 8.32
CHEMBL5590689 1 7.99
CHEMBL5594833 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353410 OSIMERTINIB IC50 = 0.34 nM 9.47
CHEMBL5590430 IC50 = 4.76 nM 8.32
CHEMBL5590689 IC50 = 10.24 nM 7.99
CHEMBL5594833 IC50 = 12.57 nM 7.90