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Assay Detail

CHEMBL4231194

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

Binding
Inhibition of recombinant human VEGFR2 using peptide as substrate by fluorimetric analysis
10
Total Activities
10
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

Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.
La Pietra V, Sartini S, Botta L, Antonelli A, Ferrari SM, Fallahi P, Moriconi A, Coviello V, Quattrini L, Ke YY, Hsing-Pang H, Da Settimo F, Novellino E, La Motta C, Marinelli L.
Eur J Med Chem (2018) 150 : 491 -505
PubMed 29549836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.81 5.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47173 1 5.95
CHEMBL50 QUERCETIN 3.0 1 5.78
CHEMBL4238771 1 5.11
CHEMBL172517 1 5.02
CHEMBL4241633 1 4.75
CHEMBL273103 1 4.67
CHEMBL1704021 1 4.33
CHEMBL1488812 1 4.29
CHEMBL4239930 1 4.17
CHEMBL4237913 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47173 IC50 = 1130.0 nM 5.95
CHEMBL50 QUERCETIN IC50 = 1660.0 nM 5.78
CHEMBL4238771 IC50 = 7730.0 nM 5.11
CHEMBL172517 IC50 = 9610.0 nM 5.02
CHEMBL4241633 IC50 = 17800.0 nM 4.75
CHEMBL273103 IC50 = 21600.0 nM 4.67
CHEMBL1704021 IC50 = 47000.0 nM 4.33
CHEMBL1488812 IC50 = 51600.0 nM 4.29
CHEMBL4239930 IC50 = 67000.0 nM 4.17
CHEMBL4237913 IC50 = 92700.0 nM 4.03