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Assay Detail

CHEMBL4138365

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

Binding
Inhibition of N-terminal GST-fused human VEGFR2 C-terminal fragment expressed in Sf9 insect cells using poly(Glu:Tyr) 4:1 as substrate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells.
Kahraman DC, Hanquet G, Jeanmart L, Lanners S, Šramel P, Boháč A, Cetin-Atalay R.
Medchemcomm (2017) 8 : 81 -87
PubMed 30108693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.83 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1200485 SORAFENIB TOSYLATE 4.0 1 8.07
CHEMBL3109274 1 7.82
CHEMBL4165836 1 7.75
CHEMBL194176 1 7.66
CHEMBL4164979 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1200485 SORAFENIB TOSYLATE IC50 = 8.5 nM 8.07
CHEMBL3109274 IC50 = 15.0 nM 7.82
CHEMBL4165836 IC50 = 18.0 nM 7.75
CHEMBL194176 IC50 = 22.0 nM 7.66
CHEMBL4164979 IC50 = 564000.0 nM -