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Assay Detail

CHEMBL1640839

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

Binding
Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CAL-27
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
Mahboobi S, Sellmer A, Winkler M, Eichhorn E, Pongratz H, Ciossek T, Baer T, Maier T, Beckers T.
J Med Chem (2010) 53 : 8546 -8555
PubMed 21080629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.30 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630109 1 6.30
CHEMBL1630107 1 -
CHEMBL554 LAPATINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630109 IC50 = 500.0 nM 6.30
CHEMBL1630107 IC50 < 32.0 nM -
CHEMBL554 LAPATINIB IC50 < 32.0 nM -