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Assay Detail

CHEMBL2412780

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

Binding
Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay
10
Total Activities
10
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

Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors.
Han C, Huang Z, Zheng C, Wan L, Lai Y, Peng S, Ding K, Ding K, Ji H, Zhang Y.
Eur J Med Chem (2013) 66 : 82 -90
PubMed 23792318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.79 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL939 GEFITINIB 4.0 1 10.00
CHEMBL1229592 1 8.49
CHEMBL2408828 1 6.89
CHEMBL2408829 1 6.62
CHEMBL2408830 1 6.46
CHEMBL2408825 1 5.96
CHEMBL2408823 1 5.64
CHEMBL2408824 1 5.53
CHEMBL2408826 1 5.50
CHEMBL2408827 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL939 GEFITINIB IC50 = 0.1 nM 10.00
CHEMBL1229592 IC50 = 3.2 nM 8.49
CHEMBL2408828 IC50 = 130.0 nM 6.89
CHEMBL2408829 IC50 = 240.0 nM 6.62
CHEMBL2408830 IC50 = 350.0 nM 6.46
CHEMBL2408825 IC50 = 1090.0 nM 5.96
CHEMBL2408823 IC50 = 2280.0 nM 5.64
CHEMBL2408824 IC50 = 2940.0 nM 5.53
CHEMBL2408826 IC50 = 3150.0 nM 5.50
CHEMBL2408827 IC50 > 10000.0 nM -