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Assay Detail

CHEMBL5252776

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

Binding
Inhibition of VEGF-induced human VEGFR2 autophosphorylation expressed in HUVEC cells measured after 2 hrs by chemiluminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Bold G, Schnell C, Furet P, McSheehy P, Brüggen J, Mestan J, Manley PW, Drückes P, Burglin M, Dürler U, Loretan J, Reuter R, Wartmann M, Theuer A, Bauer-Probst B, Martiny-Baron G, Allegrini P, Goepfert A, Wood J, Littlewood-Evans A.
J Med Chem (2016) 59 : 132 -146
PubMed 26629594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.40 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5280119 1 8.64
CHEMBL4104297 1 8.54
CHEMBL5288744 1 8.52
CHEMBL4080062 BFH-772 2.0 1 8.52
CHEMBL5276611 1 8.40
CHEMBL75232 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5280119 IC50 = 2.3 nM 8.64
CHEMBL4104297 IC50 = 2.9 nM 8.54
CHEMBL5288744 IC50 = 3.0 nM 8.52
CHEMBL4080062 BFH-772 IC50 = 3.0 nM 8.52
CHEMBL5276611 IC50 = 4.0 nM 8.40
CHEMBL75232 IC50 = 17.0 nM 7.77