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Assay Detail

CHEMBL673904

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

Functional
Compound was tested for the inhibition of VEGF-stimulated mitogenesis as determined in human umbilical vein endothelial cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Endothelial cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 14 7.60 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL324489 1 8.40
CHEMBL117052 1 8.40
CHEMBL119552 1 8.40
CHEMBL119276 1 8.40
CHEMBL118569 1 8.10
CHEMBL333297 1 7.77
CHEMBL323838 1 7.57
CHEMBL118832 1 7.52
CHEMBL117983 1 7.51
CHEMBL118748 1 7.39
CHEMBL325003 1 7.28
CHEMBL420528 1 7.01
CHEMBL221736 1 6.74
CHEMBL118440 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL324489 IC50 = 4.0 nM 8.40
CHEMBL117052 IC50 = 4.0 nM 8.40
CHEMBL119552 IC50 = 4.0 nM 8.40
CHEMBL119276 IC50 = 4.0 nM 8.40
CHEMBL118569 IC50 = 8.0 nM 8.10
CHEMBL333297 IC50 = 17.0 nM 7.77
CHEMBL323838 IC50 = 27.0 nM 7.57
CHEMBL118832 IC50 = 30.0 nM 7.52
CHEMBL117983 IC50 = 31.0 nM 7.51
CHEMBL118748 IC50 = 41.0 nM 7.39
CHEMBL325003 IC50 = 53.0 nM 7.28
CHEMBL420528 IC50 = 97.0 nM 7.01
CHEMBL221736 IC50 = 184.0 nM 6.74
CHEMBL118440 IC50 = 1140.0 nM 5.94