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Assay Detail

CHEMBL677212

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

Binding
Inhibition of epidermal growth factor receptor (EGF-R)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Sun L, Liang C, Shirazian S, Zhou Y, Miller T, Cui J, Fukuda JY, Chu JY, Nematalla A, Wang X, Chen H, Sistla A, Luu TC, Tang F, Wei J, Tang C.
J Med Chem (2003) 46 : 1116 -1119
PubMed 12646019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.00 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13629 1 5.00
CHEMBL274654 ORANTINIB 3.0 1 -
CHEMBL268731 1 -
CHEMBL430155 1 -
CHEMBL13354 1 -
CHEMBL13485 SU-11652 1 -
CHEMBL276711 SEMAXANIB 3.0 1 -
CHEMBL267293 1 -
CHEMBL13608 TOCERANIB 2.0 1 -
CHEMBL13983 1 -
CHEMBL13976 1 -
CHEMBL275117 1 -
CHEMBL535 SUNITINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13629 IC50 = 10000.0 nM 5.00
CHEMBL274654 ORANTINIB IC50 > 20000.0 nM -
CHEMBL268731 IC50 > 20000.0 nM -
CHEMBL430155 IC50 > 20000.0 nM -
CHEMBL13354 IC50 > 20000.0 nM -
CHEMBL13485 SU-11652 IC50 > 20000.0 nM -
CHEMBL276711 SEMAXANIB IC50 > 100000.0 nM -
CHEMBL267293 IC50 > 20000.0 nM -
CHEMBL13608 TOCERANIB IC50 > 20000.0 nM -
CHEMBL13983 IC50 = - nM -
CHEMBL13976 IC50 > 20000.0 nM -
CHEMBL275117 IC50 > 20000.0 nM -
CHEMBL535 SUNITINIB IC50 > 20000.0 nM -