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Assay Detail

CHEMBL3993999

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

Binding
Inhibition of recombinant human GST-tagged VEGFR3 cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assay
2
Total Activities
2
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 3 (CHEMBL1955)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors.
Qin M, Yan S, Wang L, Zhang H, Tian Y, Zhao Y, Gong P.
Bioorg Med Chem (2017) 25 : 1778 -1786
PubMed 28190652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.27 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502835 NINTEDANIB 4.0 1 8.52
CHEMBL4069394 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502835 NINTEDANIB IC50 = 3.0 nM 8.52
CHEMBL4069394 IC50 = 9.6 nM 8.02