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Assay Detail

CHEMBL5120450

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

Binding
Inhibition of wild type EGFR expressed in human A-431 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Obst-Sander U, Ricci A, Kuhn B, Friess T, Koldewey P, Kuglstatter A, Hewings D, Goergler A, Steiner S, Rueher D, Imhoff MP, Raschetti N, Marty HP, Dietzig A, Rynn C, Ehler A, Burger D, Kornacker M, Schaffland JP, Herting F, Pao W, Bischoff JR, Martoglio B, Alice Nagel Y, Jaeschke G.
J Med Chem (2022) 65 : 13052 -13073
PubMed 36178776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.29 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 7.04
CHEMBL3353410 OSIMERTINIB 4.0 1 6.49
CHEMBL5177023 1 6.24
CHEMBL4443062 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB IC50 = 92.0 nM 7.04
CHEMBL3353410 OSIMERTINIB IC50 = 322.0 nM 6.49
CHEMBL5177023 IC50 = 577.0 nM 6.24
CHEMBL4443062 IC50 = 4213.0 nM 5.38