Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL677215

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

Binding
Inhibition of Epidermal growth factor receptor autophosphorylation in A431 human epidermoid carcinoma cells
13
Total Activities
13
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. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor.
Rewcastle GW, Palmer BD, Thompson AM, Bridges AJ, Cody DR, Zhou H, Fry DW, McMichael A, Denny WA.
J Med Chem (1996) 39 : 1823 -1835
PubMed 8627606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.22 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53062 1 7.92
CHEMBL53428 1 7.85
CHEMBL53753 1 7.82
CHEMBL54400 1 7.80
CHEMBL51853 1 7.80
CHEMBL53156 1 7.70
CHEMBL53711 1 7.68
CHEMBL53796 1 7.50
CHEMBL300217 1 7.28
CHEMBL52076 1 6.96
CHEMBL298637 1 6.26
CHEMBL300083 1 5.68
CHEMBL50245 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53062 IC50 = 12.0 nM 7.92
CHEMBL53428 IC50 = 14.0 nM 7.85
CHEMBL53753 IC50 = 15.0 nM 7.82
CHEMBL54400 IC50 = 16.0 nM 7.80
CHEMBL51853 IC50 = 16.0 nM 7.80
CHEMBL53156 IC50 = 20.0 nM 7.70
CHEMBL53711 IC50 = 21.0 nM 7.68
CHEMBL53796 IC50 = 32.0 nM 7.50
CHEMBL300217 IC50 = 53.0 nM 7.28
CHEMBL52076 IC50 = 110.0 nM 6.96
CHEMBL298637 IC50 = 552.0 nM 6.26
CHEMBL300083 IC50 = 2085.0 nM 5.68
CHEMBL50245 IC50 = 2300.0 nM 5.64