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Assay Detail

CHEMBL3766503

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

Binding
Inhibition of recombinant N-terminal 6His-tagged VEGFR-2 (unknown origin) using FL-Peptide 22 as substrate after 90 mins by mobility shift assay
3
Total Activities
3
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

Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
Zhang J, Jiang X, Jiang Y, Guo M, Zhang S, Li J, He J, Liu J, Wang J, Ouyang L.
Eur J Med Chem (2016) 108 : 495 -504
PubMed 26717201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.47 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 7.75
CHEMBL3764045 TAS-115 1.0 1 7.52
CHEMBL1336 SORAFENIB 4.0 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB IC50 = 18.0 nM 7.75
CHEMBL3764045 TAS-115 IC50 = 30.0 nM 7.52
CHEMBL1336 SORAFENIB IC50 = 72.0 nM 7.14