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Assay Detail

CHEMBL1022425

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

Binding
Inhibition of VEGFR2 by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
Mahboobi S, Dove S, Sellmer A, Winkler M, Eichhorn E, Pongratz H, Ciossek T, Baer T, Maier T, Beckers T.
J Med Chem (2009) 52 : 2265 -2279
PubMed 19301902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.00 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473826 1 5.82
CHEMBL474863 1 5.36
CHEMBL515109 1 5.32
CHEMBL514511 1 5.21
CHEMBL493315 1 5.17
CHEMBL475796 1 5.11
CHEMBL515258 1 5.07
CHEMBL523684 1 5.07
CHEMBL492956 1 5.06
CHEMBL474046 1 5.05
CHEMBL514351 1 5.04
CHEMBL475820 1 5.01
CHEMBL473825 1 4.96
CHEMBL1080580 1 4.96
CHEMBL474208 1 4.92
CHEMBL521652 1 4.85
CHEMBL474015 1 4.62
CHEMBL941 IMATINIB 4.0 1 4.59
CHEMBL475051 1 4.37
CHEMBL515432 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473826 IC50 = 1500.0 nM 5.82
CHEMBL474863 IC50 = 4400.0 nM 5.36
CHEMBL515109 IC50 = 4800.0 nM 5.32
CHEMBL514511 IC50 = 6100.0 nM 5.21
CHEMBL493315 IC50 = 6700.0 nM 5.17
CHEMBL475796 IC50 = 7800.0 nM 5.11
CHEMBL515258 IC50 = 8600.0 nM 5.07
CHEMBL523684 IC50 = 8600.0 nM 5.07
CHEMBL492956 IC50 = 8700.0 nM 5.06
CHEMBL474046 IC50 = 9000.0 nM 5.05
CHEMBL514351 IC50 = 9200.0 nM 5.04
CHEMBL475820 IC50 = 9800.0 nM 5.01
CHEMBL473825 IC50 = 11000.0 nM 4.96
CHEMBL1080580 IC50 = 11000.0 nM 4.96
CHEMBL474208 IC50 = 12000.0 nM 4.92
CHEMBL521652 IC50 = 14000.0 nM 4.85
CHEMBL474015 IC50 = 24000.0 nM 4.62
CHEMBL941 IMATINIB IC50 = 25800.0 nM 4.59
CHEMBL475051 IC50 = 43000.0 nM 4.37
CHEMBL515432 IC50 = 46000.0 nM 4.34