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Assay Detail

CHEMBL673451

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

Binding
Inhibition of epidermal growth factor receptor (EGFR) autophosphorylation in A431 cells
9
Total Activities
9
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. 13. Structure-activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Thompson AM, Murray DK, Elliott WL, Fry DW, Nelson JA, Showalter HD, Roberts BJ, Vincent PW, Denny WA.
J Med Chem (1997) 40 : 3915 -3925
PubMed 9397172 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.10 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL126623 1 8.09
CHEMBL53428 1 7.85
CHEMBL54400 1 7.80
CHEMBL128987 1 7.44
CHEMBL52076 1 6.96
CHEMBL126372 1 6.64
CHEMBL127086 1 4.94
CHEMBL128467 1 -
CHEMBL339416 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL126623 IC50 = 8.1 nM 8.09
CHEMBL53428 IC50 = 14.0 nM 7.85
CHEMBL54400 IC50 = 16.0 nM 7.80
CHEMBL128987 IC50 = 36.0 nM 7.44
CHEMBL52076 IC50 = 110.0 nM 6.96
CHEMBL126372 IC50 = 227.0 nM 6.64
CHEMBL127086 IC50 = 11400.0 nM 4.94
CHEMBL128467 IC50 > 1000.0 nM -
CHEMBL339416 IC50 > 1000.0 nM -