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Assay Detail

CHEMBL1686403

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

Binding
Inhibition of human recombinant His-tagged VEGFR2 assessed as infrared absorption by ELISA assay in presence of 20 uM ATP
4
Total Activities
4
Compounds Tested
2
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

Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization.
Kawakami JK, Martinez Y, Sasaki B, Harris M, Kurata WE, Lau AF.
Bioorg Med Chem Lett (2011) 21 : 1371 -1375
PubMed 21306896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.51 8.70
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1558704 1 8.70
CHEMBL92461 1 7.72
CHEMBL147138 1 6.10
CHEMBL1277526 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1558704 IC50 = 2.0 nM 8.70
CHEMBL92461 IC50 = 19.0 nM 7.72
CHEMBL147138 IC50 = 800.0 nM 6.10
CHEMBL1277526 Inhibition - % -