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Assay Detail

CHEMBL2186468

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

Binding
Inhibition of VEGFR2
15
Total Activities
15
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 2 (CHEMBL279)
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 15 8.15 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289494 TIVOZANIB 4.0 1 9.80
CHEMBL2180604 TAK-593 1.0 1 9.02
CHEMBL491473 CEDIRANIB 3.0 1 9.00
CHEMBL572881 MOTESANIB 3.0 1 8.52
CHEMBL1289601 LENVATINIB 4.0 1 8.40
CHEMBL2180602 TAFETINIB 1.0 1 8.30
CHEMBL2079588 TELATINIB 2.0 1 8.22
CHEMBL1230609 FORETINIB 2.0 1 8.17
CHEMBL1614710 OSI-930 1.0 1 8.05
CHEMBL253969 OSI-632 2.0 1 7.96
CHEMBL2180605 1 7.60
CHEMBL2180603 1 7.50
CHEMBL101253 VATALANIB 3.0 1 7.37
CHEMBL352308 1 7.16
CHEMBL587723 AEE-788 2.0 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289494 TIVOZANIB IC50 = 0.16 nM 9.80
CHEMBL2180604 TAK-593 IC50 = 0.95 nM 9.02
CHEMBL491473 CEDIRANIB IC50 = 1.0 nM 9.00
CHEMBL572881 MOTESANIB IC50 = 3.0 nM 8.52
CHEMBL1289601 LENVATINIB IC50 = 4.0 nM 8.40
CHEMBL2180602 TAFETINIB IC50 = 5.0 nM 8.30
CHEMBL2079588 TELATINIB IC50 = 6.0 nM 8.22
CHEMBL1230609 FORETINIB IC50 = 6.8 nM 8.17
CHEMBL1614710 OSI-930 IC50 = 9.0 nM 8.05
CHEMBL253969 OSI-632 IC50 = 11.0 nM 7.96
CHEMBL2180605 IC50 = 25.0 nM 7.60
CHEMBL2180603 IC50 = 32.0 nM 7.50
CHEMBL101253 VATALANIB IC50 = 43.0 nM 7.37
CHEMBL352308 IC50 = 69.0 nM 7.16
CHEMBL587723 AEE-788 IC50 = 77.0 nM 7.11