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Assay Detail

CHEMBL690866

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Functional
Inhibition of VEGFstimulated HUVEC cell proliferation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HUVEC
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Vascular endothelial growth factor receptor (CHEMBL2095227)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.
Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO, Kendrew J, Lambert-van der Brempt C.
J Med Chem (1999) 42 : 5369 -5389
PubMed 10639280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL347086 1 8.40
CHEMBL150187 1 7.70
CHEMBL357815 1 7.40
CHEMBL281872 ZD-4190 FREE BASE 1.0 1 7.30
CHEMBL358672 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL347086 IC50 = 4.0 nM 8.40
CHEMBL150187 IC50 = 20.0 nM 7.70
CHEMBL357815 IC50 = 40.0 nM 7.40
CHEMBL281872 ZD-4190 FREE BASE IC50 = 50.0 nM 7.30
CHEMBL358672 IC50 = 600.0 nM 6.22