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Assay Detail

CHEMBL1067992

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Binding
Inhibition of recombinant GST-fused VEGFR2 expressed in baculovirus infected Sf9 cells by DELFIA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.
Gaudette F, Raeppel S, Nguyen H, Beaulieu N, Beaulieu C, Dupont I, Macleod AR, Besterman JM, Vaisburg A.
Bioorg Med Chem Lett (2010) 20 : 848 -852
PubMed 20071170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.24 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL465130 1 8.00
CHEMBL602703 1 8.00
CHEMBL464510 1 7.70
CHEMBL591924 1 7.70
CHEMBL602704 1 7.70
CHEMBL602905 1 7.70
CHEMBL600604 1 7.52
CHEMBL612137 1 7.40
CHEMBL600632 1 6.68
CHEMBL600603 1 6.44
CHEMBL600398 1 6.07
CHEMBL603082 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL465130 IC50 = 10.0 nM 8.00
CHEMBL602703 IC50 = 10.0 nM 8.00
CHEMBL464510 IC50 = 20.0 nM 7.70
CHEMBL591924 IC50 = 20.0 nM 7.70
CHEMBL602704 IC50 = 20.0 nM 7.70
CHEMBL602905 IC50 = 20.0 nM 7.70
CHEMBL600604 IC50 = 30.0 nM 7.52
CHEMBL612137 IC50 = 40.0 nM 7.40
CHEMBL600632 IC50 = 210.0 nM 6.68
CHEMBL600603 IC50 = 360.0 nM 6.44
CHEMBL600398 IC50 = 860.0 nM 6.07
CHEMBL603082 IC50 = 1200.0 nM 5.92