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Assay Detail

CHEMBL819557

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

Binding
Inhibition of Vascular endothelial growth factor receptor in 3T3 cells
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type NIH3T3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 12 6.90 7.40
NT 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13983 1 7.40
CHEMBL268731 1 7.30
CHEMBL13354 1 7.30
CHEMBL13485 SU-11652 1 7.30
CHEMBL13629 1 7.30
CHEMBL13608 TOCERANIB 2.0 1 7.30
CHEMBL13976 1 7.30
CHEMBL535 SUNITINIB 4.0 1 7.30
CHEMBL267293 1 6.30
CHEMBL275117 1 6.30
CHEMBL276711 SEMAXANIB 3.0 1 5.98
CHEMBL274654 ORANTINIB 3.0 1 5.70
CHEMBL430155 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13983 IC50 = 40.0 nM 7.40
CHEMBL268731 IC50 = 50.0 nM 7.30
CHEMBL13354 IC50 = 50.0 nM 7.30
CHEMBL13485 SU-11652 IC50 = 50.0 nM 7.30
CHEMBL13629 IC50 = 50.0 nM 7.30
CHEMBL13608 TOCERANIB IC50 = 50.0 nM 7.30
CHEMBL13976 IC50 = 50.0 nM 7.30
CHEMBL535 SUNITINIB IC50 = 50.0 nM 7.30
CHEMBL267293 IC50 = 500.0 nM 6.30
CHEMBL275117 IC50 = 500.0 nM 6.30
CHEMBL276711 SEMAXANIB IC50 = 1040.0 nM 5.98
CHEMBL274654 ORANTINIB IC50 = 2000.0 nM 5.70
CHEMBL430155 NT - -