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Assay Detail

CHEMBL3830047

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

ADMET
Inhibition of recombinant human VEGFR2 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.
Yan W, Wang X, Dai Y, Zhao B, Yang X, Fan J, Gao Y, Meng F, Wang Y, Luo C, Ai J, Geng M, Duan W.
J Med Chem (2016) 59 : 6690 -6708
PubMed 27348537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.05 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828439 1 8.60
CHEMBL3828009 LY-2874455 1.0 1 8.24
CHEMBL3827178 1 8.12
CHEMBL3827268 1 8.11
CHEMBL3828740 1 8.10
CHEMBL3828122 1 8.05
CHEMBL3827180 1 7.90
CHEMBL212054 1 7.79
CHEMBL3348846 FEXAGRATINIB 2.0 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828439 IC50 = 2.5 nM 8.60
CHEMBL3828009 LY-2874455 IC50 = 5.8 nM 8.24
CHEMBL3827178 IC50 = 7.5 nM 8.12
CHEMBL3827268 IC50 = 7.8 nM 8.11
CHEMBL3828740 IC50 = 8.0 nM 8.10
CHEMBL3828122 IC50 = 9.0 nM 8.05
CHEMBL3827180 IC50 = 12.6 nM 7.90
CHEMBL212054 IC50 = 16.4 nM 7.79
CHEMBL3348846 FEXAGRATINIB IC50 = 27.0 nM 7.57