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Assay Detail

CHEMBL679548

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Binding
Inhibition of tyrosine kinase activity of Epidermal growth factor receptor from human A431 cells
10
Total Activities
10
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 Expert

Target

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

Publication

Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Rewcastle GW, Palmer BD, Bridges AJ, Showalter HD, Sun L, Nelson J, McMichael A, Kraker AJ, Fry DW, Denny WA.
J Med Chem (1996) 39 : 918 -928
PubMed 8632415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.30 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29197 1 10.60
CHEMBL366580 1 9.47
CHEMBL39337 1 9.36
CHEMBL176891 1 8.88
CHEMBL172652 1 8.39
CHEMBL93051 1 7.82
CHEMBL175101 1 7.66
CHEMBL427298 1 6.69
CHEMBL96627 1 5.86
CHEMBL93346 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29197 IC50 = 0.025 nM 10.60
CHEMBL366580 IC50 = 0.34 nM 9.47
CHEMBL39337 IC50 = 0.44 nM 9.36
CHEMBL176891 IC50 = 1.32 nM 8.88
CHEMBL172652 IC50 = 4.1 nM 8.39
CHEMBL93051 IC50 = 15.0 nM 7.82
CHEMBL175101 IC50 = 22.0 nM 7.66
CHEMBL427298 IC50 = 203.0 nM 6.69
CHEMBL96627 IC50 = 1370.0 nM 5.86
CHEMBL93346 IC50 > 10000.0 nM -