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Assay Detail

CHEMBL4332286

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

Binding
Inhibition of recombinant human His6-tagged EGFR cytoplasmic domain (645 to 1186 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in autophosphorylation preincubated for 10 mins followed by ATP-MgCl2 addition and measured after 1 hr by DELFIA/time-resolved fluorometric analysis
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

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

Publication

The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
Li Y, Xiao J, Zhang Q, Yu W, Liu M, Guo Y, He J, Liu Y.
Bioorg Med Chem (2019) 27 : 568 -577
PubMed 30600149 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.60 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94061 1 7.96
CHEMBL607707 PELITINIB 2.0 1 7.42
CHEMBL4578561 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94061 IC50 = 11.0 nM 7.96
CHEMBL607707 PELITINIB IC50 = 38.5 nM 7.42
CHEMBL4578561 IC50 = 38.5 nM 7.42