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Assay Detail

CHEMBL904734

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

Binding
Inhibition of EGFR tyrosine kinase expressed in A431 cells
7
Total Activities
7
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

Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship.
Rachid Z, Brahimi F, Qiu Q, Williams C, Hartley JM, Hartley JA, Jean-Claude BJ.
J Med Chem (2007) 50 : 2605 -2608
PubMed 17472358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.67 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225928 1 8.36
CHEMBL225720 1 7.43
CHEMBL225929 1 7.15
CHEMBL343352 1 6.70
CHEMBL225721 1 6.01
CHEMBL225930 1 5.66
CHEMBL388286 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225928 IC50 = 4.4 nM 8.36
CHEMBL225720 IC50 = 37.0 nM 7.43
CHEMBL225929 IC50 = 71.0 nM 7.15
CHEMBL343352 IC50 = 200.0 nM 6.70
CHEMBL225721 IC50 = 970.0 nM 6.01
CHEMBL225930 IC50 = 2200.0 nM 5.66
CHEMBL388286 IC50 = 3960.0 nM 5.40