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Assay Detail

CHEMBL3372999

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

Binding
Inhibition of wild type EGFR (unknown origin) by Z'-Lyte kinase assay
19
Total Activities
19
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

Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia.
Cheng W, Zhu S, Ma X, Qiu N, Peng P, Sheng R, Hu Y.
Eur J Med Chem (2015) 89 : 826 -834
PubMed 25462282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.74 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355877 1 9.49
CHEMBL939 GEFITINIB 4.0 1 9.35
CHEMBL3355875 1 9.33
CHEMBL3355881 1 9.31
CHEMBL3355882 1 9.30
CHEMBL3355876 1 9.29
CHEMBL3355889 1 9.28
CHEMBL3355880 1 9.25
CHEMBL3355878 1 9.18
CHEMBL3355874 1 9.05
CHEMBL3355879 1 8.97
CHEMBL3355890 1 8.93
CHEMBL3355873 1 8.52
CHEMBL3355888 1 8.46
CHEMBL3355887 1 8.31
CHEMBL3355886 1 7.82
CHEMBL3355884 1 7.54
CHEMBL3355883 1 7.42
CHEMBL3355885 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355877 IC50 = 0.32 nM 9.49
CHEMBL939 GEFITINIB IC50 = 0.45 nM 9.35
CHEMBL3355875 IC50 = 0.47 nM 9.33
CHEMBL3355881 IC50 = 0.49 nM 9.31
CHEMBL3355882 IC50 = 0.5 nM 9.30
CHEMBL3355876 IC50 = 0.51 nM 9.29
CHEMBL3355889 IC50 = 0.53 nM 9.28
CHEMBL3355880 IC50 = 0.56 nM 9.25
CHEMBL3355878 IC50 = 0.66 nM 9.18
CHEMBL3355874 IC50 = 0.89 nM 9.05
CHEMBL3355879 IC50 = 1.08 nM 8.97
CHEMBL3355890 IC50 = 1.18 nM 8.93
CHEMBL3355873 IC50 = 3.05 nM 8.52
CHEMBL3355888 IC50 = 3.43 nM 8.46
CHEMBL3355887 IC50 = 4.9 nM 8.31
CHEMBL3355886 IC50 = 15.1 nM 7.82
CHEMBL3355884 IC50 = 28.5 nM 7.54
CHEMBL3355883 IC50 = 38.3 nM 7.42
CHEMBL3355885 IC50 = 51.2 nM 7.29