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Assay Detail

CHEMBL4313654

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

Binding
Inhibition of recombinant human GST-tagged EGFR catalytic domain (668 to 1210 residues) expressed in baculovirus expression system using TK-biotin peptide as substrate measured after 10 mins by HTRF assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.
El-Sayed NA, Nour MS, Salem MA, Arafa RK.
Eur J Med Chem (2019) 183 : 111693 -111693
PubMed 31539778 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.32 6.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4535881 1 6.56
CHEMBL4561572 1 6.38
CHEMBL553 ERLOTINIB 4.0 1 6.38
CHEMBL4569755 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4535881 IC50 = 275.7 nM 6.56
CHEMBL4561572 IC50 = 412.3 nM 6.38
CHEMBL553 ERLOTINIB IC50 = 417.8 nM 6.38
CHEMBL4569755 IC50 = 1128.9 nM 5.95