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Assay Detail

CHEMBL3587278

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

Binding
Inhibition of VEGFR-2 (unknown origin) after 1 hr by ADP-Glo assay
28
Total Activities
28
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

Discovery of biphenyl-aryl ureas as novel VEGFR-2 inhibitors. Part 4: exploration of diverse hinge-binding fragments.
Su P, Wang J, Shi Y, Pan X, Shao R, Zhang J.
Bioorg Med Chem (2015) 23 : 3228 -3236
PubMed 25982075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.48 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586072 1 9.85
CHEMBL3586071 1 9.82
CHEMBL3586057 1 9.66
CHEMBL3586049 1 9.44
CHEMBL1336 SORAFENIB 4.0 1 9.32
CHEMBL3586056 1 8.66
CHEMBL3586051 1 8.34
CHEMBL3586065 1 7.88
CHEMBL3586052 1 7.20
CHEMBL3586070 1 7.00
CHEMBL3586058 1 6.14
CHEMBL3586050 1 -
CHEMBL3586053 1 -
CHEMBL3586054 1 -
CHEMBL3586055 1 -
CHEMBL3586059 1 -
CHEMBL3586060 1 -
CHEMBL3586061 1 -
CHEMBL3586063 1 -
CHEMBL3586064 1 -
CHEMBL3586066 1 -
CHEMBL3586062 1 -
CHEMBL3586067 1 -
CHEMBL3586068 1 -
CHEMBL3586075 1 -
CHEMBL3586069 1 -
CHEMBL3586074 1 -
CHEMBL3586073 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586072 IC50 = 0.14 nM 9.85
CHEMBL3586071 IC50 = 0.15 nM 9.82
CHEMBL3586057 IC50 = 0.22 nM 9.66
CHEMBL3586049 IC50 = 0.36 nM 9.44
CHEMBL1336 SORAFENIB IC50 = 0.48 nM 9.32
CHEMBL3586056 IC50 = 2.19 nM 8.66
CHEMBL3586051 IC50 = 4.6 nM 8.34
CHEMBL3586065 IC50 = 13.26 nM 7.88
CHEMBL3586052 IC50 = 63.08 nM 7.20
CHEMBL3586070 IC50 = 99.58 nM 7.00
CHEMBL3586058 IC50 = 722.38 nM 6.14
CHEMBL3586050 IC50 > 200.0 nM -
CHEMBL3586053 IC50 - -
CHEMBL3586054 IC50 > 200.0 nM -
CHEMBL3586055 IC50 - -
CHEMBL3586059 IC50 - -
CHEMBL3586060 IC50 > 1000.0 nM -
CHEMBL3586061 IC50 > 1000.0 nM -
CHEMBL3586063 IC50 > 1000.0 nM -
CHEMBL3586064 IC50 - -
CHEMBL3586066 IC50 > 1000.0 nM -
CHEMBL3586062 IC50 - -
CHEMBL3586067 IC50 - -
CHEMBL3586068 IC50 - -
CHEMBL3586075 IC50 - -
CHEMBL3586069 IC50 > 1000.0 nM -
CHEMBL3586074 IC50 - -
CHEMBL3586073 IC50 - -