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Assay Detail

CHEMBL2186467

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

Binding
Inhibition of VEGFR3
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 3 (CHEMBL1955)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
Musumeci F, Radi M, Brullo C, Schenone S.
J Med Chem (2012) 55 : 10797 -10822
PubMed 23098265 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.36 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289494 TIVOZANIB 4.0 1 9.62
CHEMBL2180604 TAK-593 1.0 1 8.96
CHEMBL1230609 FORETINIB 2.0 1 8.55
CHEMBL491473 CEDIRANIB 3.0 1 8.52
CHEMBL2079588 TELATINIB 2.0 1 8.40
CHEMBL1289601 LENVATINIB 4.0 1 8.28
CHEMBL572881 MOTESANIB 3.0 1 8.22
CHEMBL2180605 1 8.00
CHEMBL101253 VATALANIB 3.0 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289494 TIVOZANIB IC50 = 0.24 nM 9.62
CHEMBL2180604 TAK-593 IC50 = 1.1 nM 8.96
CHEMBL1230609 FORETINIB IC50 = 2.8 nM 8.55
CHEMBL491473 CEDIRANIB IC50 = 3.0 nM 8.52
CHEMBL2079588 TELATINIB IC50 = 4.0 nM 8.40
CHEMBL1289601 LENVATINIB IC50 = 5.2 nM 8.28
CHEMBL572881 MOTESANIB IC50 = 6.0 nM 8.22
CHEMBL2180605 IC50 = 10.0 nM 8.00
CHEMBL101253 VATALANIB IC50 = 195.0 nM 6.71