Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2090278

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

Binding
Inhibition of EGFR-mediated intracellular tyrosine phosphorylation in EGF-stimulated human A431 cells after 2.5 hrs by SDS-PAGE analysis
11
Total Activities
11
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

Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.
Hu S, Xie G, Zhang DX, Davis C, Long W, Hu Y, Wang F, Kang X, Tan F, Ding L, Wang Y.
Bioorg Med Chem Lett (2012) 22 : 6301 -6305
PubMed 22959248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.31 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2087360 1 7.35
CHEMBL2087361 ICOTINIB 3.0 1 7.35
CHEMBL2087355 1 7.30
CHEMBL2087356 1 7.30
CHEMBL2087358 1 7.26
CHEMBL1198361 1 -
CHEMBL2087352 1 -
CHEMBL2087353 1 -
CHEMBL2087354 1 -
CHEMBL2087357 1 -
CHEMBL2087359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2087360 IC50 = 45.0 nM 7.35
CHEMBL2087361 ICOTINIB IC50 = 45.0 nM 7.35
CHEMBL2087355 IC50 = 50.0 nM 7.30
CHEMBL2087356 IC50 = 50.0 nM 7.30
CHEMBL2087358 IC50 = 55.0 nM 7.26
CHEMBL1198361 IC50 - -
CHEMBL2087352 IC50 - -
CHEMBL2087353 IC50 - -
CHEMBL2087354 IC50 - -
CHEMBL2087357 IC50 > 1000.0 nM -
CHEMBL2087359 IC50 > 1000.0 nM -