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Assay Detail

CHEMBL4819966

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

Binding
Inhibition of recombinant human His-tagged VEGFR2 expressed in Baculovirus expression system using ADP-Glo as substrate measured after 30 mins in presence of ATP by ADP-Glo kinase assay
29
Total Activities
29
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

Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold.
Wang DP, Liu KL, Li XY, Lu GQ, Xue WH, Qian XH, Mohamed O K, Meng FH.
Eur J Med Chem (2021) 211 : 113083 -113083
PubMed 33340911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 4.21 4.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4874971 1 4.58
CHEMBL4866291 1 4.43
CHEMBL4864168 1 4.35
CHEMBL4863263 1 4.14
CHEMBL535 SUNITINIB 4.0 1 4.08
CHEMBL4857454 1 4.05
CHEMBL4856891 1 4.03
CHEMBL4847439 1 4.00
CHEMBL4848005 1 -
CHEMBL4872149 1 -
CHEMBL4856794 1 -
CHEMBL4850246 1 -
CHEMBL4877343 1 -
CHEMBL4869269 1 -
CHEMBL4864073 1 -
CHEMBL4872013 1 -
CHEMBL4878024 1 -
CHEMBL4878880 1 -
CHEMBL4877074 1 -
CHEMBL4853198 1 -
CHEMBL4856663 1 -
CHEMBL4854778 1 -
CHEMBL4871475 1 -
CHEMBL4847210 1 -
CHEMBL4866203 1 -
CHEMBL4866727 1 -
CHEMBL4846157 1 -
CHEMBL4873974 1 -
CHEMBL4876341 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4874971 IC50 = 26380.0 nM 4.58
CHEMBL4866291 IC50 = 36900.0 nM 4.43
CHEMBL4864168 IC50 = 44670.0 nM 4.35
CHEMBL4863263 IC50 = 71550.0 nM 4.14
CHEMBL535 SUNITINIB IC50 = 83200.0 nM 4.08
CHEMBL4857454 IC50 = 89160.0 nM 4.05
CHEMBL4856891 IC50 = 93110.0 nM 4.03
CHEMBL4847439 IC50 = 99670.0 nM 4.00
CHEMBL4848005 IC50 > 200000.0 nM -
CHEMBL4872149 IC50 = 162810.0 nM -
CHEMBL4856794 IC50 = 115420.0 nM -
CHEMBL4850246 IC50 > 200000.0 nM -
CHEMBL4877343 IC50 = 198540.0 nM -
CHEMBL4869269 IC50 > 200000.0 nM -
CHEMBL4864073 IC50 = 108360.0 nM -
CHEMBL4872013 IC50 = 178910.0 nM -
CHEMBL4878024 IC50 > 200000.0 nM -
CHEMBL4878880 IC50 = 169420.0 nM -
CHEMBL4877074 IC50 = 171120.0 nM -
CHEMBL4853198 IC50 = 192510.0 nM -
CHEMBL4856663 IC50 = 119930.0 nM -
CHEMBL4854778 IC50 = 186440.0 nM -
CHEMBL4871475 IC50 = 170180.0 nM -
CHEMBL4847210 IC50 = 187240.0 nM -
CHEMBL4866203 IC50 = 193410.0 nM -
CHEMBL4866727 IC50 = 190070.0 nM -
CHEMBL4846157 IC50 = 168890.0 nM -
CHEMBL4873974 IC50 = 110600.0 nM -
CHEMBL4876341 IC50 = 139500.0 nM -