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Assay Detail

CHEMBL4307050

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

Binding
Inhibition of VEGFR2 (unknown origin)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.
Chen F, Fang Y, Zhao R, Le J, Zhang B, Huang R, Chen Z, Shao J.
Eur J Med Chem (2019) 179 : 916 -935
PubMed 31306818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.36 10.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105717 CABOZANTINIB 4.0 1 10.46
CHEMBL1289926 AXITINIB 4.0 1 9.74
CHEMBL1289601 LENVATINIB 4.0 1 8.40
CHEMBL1946170 REGORAFENIB 4.0 1 8.38
CHEMBL502835 NINTEDANIB 4.0 1 7.89
CHEMBL477772 PAZOPANIB 4.0 1 7.52
CHEMBL24828 VANDETANIB 4.0 1 7.40
CHEMBL535 SUNITINIB 4.0 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105717 CABOZANTINIB IC50 = 0.035 nM 10.46
CHEMBL1289926 AXITINIB IC50 = 0.18 nM 9.74
CHEMBL1289601 LENVATINIB IC50 = 4.0 nM 8.40
CHEMBL1946170 REGORAFENIB IC50 = 4.2 nM 8.38
CHEMBL502835 NINTEDANIB IC50 = 13.0 nM 7.89
CHEMBL477772 PAZOPANIB IC50 = 30.0 nM 7.52
CHEMBL24828 VANDETANIB IC50 = 40.0 nM 7.40
CHEMBL535 SUNITINIB IC50 = 80.0 nM 7.10