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Assay Detail

CHEMBL5152021

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

Binding
Inhibition of recombinant VEGFR2 (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform method
5
Total Activities
5
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

Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.
Saha D, Ryan KR, Lakkaniga NR, Acharya B, Garcia NG, Smith EL, Frett B.
J Med Chem (2021) 64 : 11747 -11773
PubMed 34402300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.22 10.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105717 CABOZANTINIB 4.0 1 10.46
CHEMBL24828 VANDETANIB 4.0 1 8.40
CHEMBL2029988 CEP-32496 2.0 1 7.77
CHEMBL5171764 1 7.46
CHEMBL4559134 SELPERCATINIB 4.0 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105717 CABOZANTINIB IC50 = 0.035 nM 10.46
CHEMBL24828 VANDETANIB IC50 = 4.0 nM 8.40
CHEMBL2029988 CEP-32496 IC50 = 17.0 nM 7.77
CHEMBL5171764 IC50 = 35.0 nM 7.46
CHEMBL4559134 SELPERCATINIB IC50 = 100.0 nM 7.00