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Assay Detail

CHEMBL5120710

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

Binding
Inhibition of recombinant human N-terminal GST-tagged HER2 wild type (679 to 1255 residues) expressed in baculovirus infected Sf9 insect cells using AQT0794 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 Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824)
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 6.61 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098072 1 6.85
CHEMBL4558324 LAZERTINIB 4.0 1 6.36
CHEMBL3353410 OSIMERTINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098072 Ki = 142.0 nM 6.85
CHEMBL4558324 LAZERTINIB Ki = 437.0 nM 6.36
CHEMBL3353410 OSIMERTINIB Ki - -