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Assay Detail

CHEMBL4623161

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

Binding
Inhibition of GST-tagged human recombinant VEGFR1 cytoplasmic domain (781 to 1338 residues) expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by 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 1 (CHEMBL1868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.
Qin M, Tian Y, Han X, Cao Q, Zheng S, Liu C, Wu X, Liu L, Meng Y, Wang X, Zhang H, Hou Y.
Bioorg Med Chem (2020) 28 : 115486 -115486
PubMed 32305182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.58 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502835 NINTEDANIB 4.0 1 7.64
CHEMBL4644718 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502835 NINTEDANIB IC50 = 23.0 nM 7.64
CHEMBL4644718 IC50 = 31.0 nM 7.51