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Assay Detail

CHEMBL5120707

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

Binding
Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) L858R/T790M mutant expressed in baculovirus infected Sf21 insect cells using AQT0734 as substrate measured up to 240 mins by fluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).
Heppner DE, Wittlinger F, Beyett TS, Shaurova T, Urul DA, Buckley B, Pham CD, Schaeffner IK, Yang B, Ogboo BC, May EW, Schaefer EM, Eck MJ, Laufer SA, Hershberger PA.
ACS Med Chem Lett (2022) 13 : 1856 -1863
PubMed 36518696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.90 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4558324 LAZERTINIB 4.0 1 7.47
CHEMBL4098072 1 6.65
CHEMBL3353410 OSIMERTINIB 4.0 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4558324 LAZERTINIB Ki = 34.0 nM 7.47
CHEMBL4098072 Ki = 224.0 nM 6.65
CHEMBL3353410 OSIMERTINIB Ki = 256.0 nM 6.59