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Assay Detail

CHEMBL680018

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

Binding
Inhibition of epidermal growth factor receptor using enzyme assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
Tsou HR, Mamuya N, Johnson BD, Reich MF, Gruber BC, Ye F, Nilakantan R, Shen R, Discafani C, DeBlanc R, Davis R, Koehn FE, Greenberger LM, Wang YF, Wissner A.
J Med Chem (2001) 44 : 2719 -2734
PubMed 11495584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.20 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285063 1 8.70
CHEMBL94062 1 8.70
CHEMBL329856 1 8.22
CHEMBL91867 1 8.10
CHEMBL91009 1 8.05
CHEMBL94061 1 7.96
CHEMBL328704 1 7.92
CHEMBL93783 1 7.85
CHEMBL93386 1 7.70
CHEMBL90595 1 7.24
CHEMBL93049 1 7.23
CHEMBL328245 1 7.21
CHEMBL442754 1 7.21
CHEMBL327838 1 7.19
CHEMBL92356 1 7.19
CHEMBL93784 1 7.19
CHEMBL94109 1 7.17
CHEMBL414220 1 7.15
CHEMBL91925 1 7.14
CHEMBL316127 1 7.13
CHEMBL91811 1 7.07
CHEMBL419501 1 7.07
CHEMBL92731 1 7.05
CHEMBL328977 1 7.02
CHEMBL92961 1 7.01
CHEMBL94068 1 6.97
CHEMBL94066 1 6.97
CHEMBL92902 1 6.94
CHEMBL2112370 1 6.88
CHEMBL2112369 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285063 IC50 = 2.0 nM 8.70
CHEMBL94062 IC50 = 2.0 nM 8.70
CHEMBL329856 IC50 = 6.0 nM 8.22
CHEMBL91867 IC50 = 8.0 nM 8.10
CHEMBL91009 IC50 = 9.0 nM 8.05
CHEMBL94061 IC50 = 11.0 nM 7.96
CHEMBL328704 IC50 = 12.0 nM 7.92
CHEMBL93783 IC50 = 14.0 nM 7.85
CHEMBL93386 IC50 = 20.0 nM 7.70
CHEMBL90595 IC50 = 57.0 nM 7.24
CHEMBL93049 IC50 = 59.0 nM 7.23
CHEMBL328245 IC50 = 62.0 nM 7.21
CHEMBL442754 IC50 = 62.0 nM 7.21
CHEMBL93784 IC50 = 65.0 nM 7.19
CHEMBL92356 IC50 = 65.0 nM 7.19
CHEMBL327838 IC50 = 65.0 nM 7.19
CHEMBL94109 IC50 = 68.0 nM 7.17
CHEMBL414220 IC50 = 71.0 nM 7.15
CHEMBL91925 IC50 = 73.0 nM 7.14
CHEMBL316127 IC50 = 74.0 nM 7.13
CHEMBL419501 IC50 = 85.0 nM 7.07
CHEMBL91811 IC50 = 85.0 nM 7.07
CHEMBL92731 IC50 = 90.0 nM 7.05
CHEMBL328977 IC50 = 95.0 nM 7.02
CHEMBL92961 IC50 = 97.0 nM 7.01
CHEMBL94068 IC50 = 106.0 nM 6.97
CHEMBL94066 IC50 = 107.0 nM 6.97
CHEMBL92902 IC50 = 115.0 nM 6.94
CHEMBL2112370 IC50 = 131.0 nM 6.88
CHEMBL2112369 IC50 = 194.0 nM 6.71
CHEMBL93537 IC50 = 203.0 nM 6.69
CHEMBL94123 IC50 = 215.0 nM 6.67
CHEMBL93464 IC50 = 236.0 nM 6.63
CHEMBL91748 IC50 = 250.0 nM 6.60
CHEMBL329642 IC50 = 269.0 nM 6.57
CHEMBL92086 IC50 = 339.0 nM 6.47
CHEMBL93754 IC50 = 1124.0 nM 5.95
CHEMBL92882 IC50 = 1132.0 nM 5.95