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Assay Detail

CHEMBL3813356

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

Binding
Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate.
Tarozzi A, Marchetti C, Nicolini B, D'Amico M, Ticchi N, Pruccoli L, Tumiatti V, Simoni E, Lodola A, Mor M, Milelli A, Minarini A.
Eur J Med Chem (2016) 117 : 283 -291
PubMed 27135370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.94 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285063 1 7.44
CHEMBL3809045 1 6.06
CHEMBL52765 1 5.21
CHEMBL48802 SULFORAPHANE 3.0 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285063 IC50 = 36.0 nM 7.44
CHEMBL3809045 IC50 = 880.0 nM 6.06
CHEMBL52765 IC50 = 6100.0 nM 5.21
CHEMBL48802 SULFORAPHANE IC50 = 9000.0 nM 5.05