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Assay Detail

CHEMBL677205

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Binding
Inhibition of Epidermal growth factor receptor from 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

Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.
Rewcastle GW, Denny WA, Bridges AJ, Zhou H, Cody DR, McMichael A, Fry DW.
J Med Chem (1995) 38 : 3482 -3487
PubMed 7658435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.75 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420624 1 10.00
CHEMBL93032 1 9.77
CHEMBL102726 1 6.50
CHEMBL116308 1 6.45
CHEMBL289787 1 6.01
CHEMBL117696 1 -
CHEMBL117988 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420624 IC50 = 0.1 nM 10.00
CHEMBL93032 IC50 = 0.17 nM 9.77
CHEMBL102726 IC50 = 320.0 nM 6.50
CHEMBL116308 IC50 = 355.0 nM 6.45
CHEMBL289787 IC50 = 974.0 nM 6.01
CHEMBL117696 IC50 > 10000.0 nM -
CHEMBL117988 IC50 > 10000.0 nM -