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Assay Detail

CHEMBL820698

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

Binding
Inhibition of VEGF receptor 2 mediated phosphorylation of poly-Glu/Tyr (4:1)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Fraley ME, Arrington KL, Buser CA, Ciecko PA, Coll KE, Fernandes C, Hartman GD, Hoffman WF, Lynch JJ, McFall RC, Rickert K, Singh R, Smith S, Thomas KA, Wong BK.
Bioorg Med Chem Lett (2004) 14 : 351 -355
PubMed 14698157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.98 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333297 1 8.40
CHEMBL119276 1 8.40
CHEMBL324489 1 8.30
CHEMBL117052 1 8.30
CHEMBL119552 1 8.30
CHEMBL325003 1 8.22
CHEMBL118569 1 8.15
CHEMBL221736 1 8.10
CHEMBL118748 1 8.10
CHEMBL117983 1 8.00
CHEMBL118832 1 7.96
CHEMBL420528 1 7.85
CHEMBL323838 1 7.80
CHEMBL118440 1 7.35
CHEMBL327029 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333297 IC50 = 4.0 nM 8.40
CHEMBL119276 IC50 = 4.0 nM 8.40
CHEMBL324489 IC50 = 5.0 nM 8.30
CHEMBL117052 IC50 = 5.0 nM 8.30
CHEMBL119552 IC50 = 5.0 nM 8.30
CHEMBL325003 IC50 = 6.0 nM 8.22
CHEMBL118569 IC50 = 7.0 nM 8.15
CHEMBL221736 IC50 = 8.0 nM 8.10
CHEMBL118748 IC50 = 8.0 nM 8.10
CHEMBL117983 IC50 = 10.0 nM 8.00
CHEMBL118832 IC50 = 11.0 nM 7.96
CHEMBL420528 IC50 = 14.0 nM 7.85
CHEMBL323838 IC50 = 16.0 nM 7.80
CHEMBL118440 IC50 = 45.0 nM 7.35
CHEMBL327029 IC50 = 355.0 nM 6.45