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Assay Detail

CHEMBL863825

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

Binding
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.
Kiselyov AS, Semenova M, Semenov VV, Milligan D.
Bioorg Med Chem Lett (2006) 16 : 1913 -1919
PubMed 16460936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.59 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101253 VATALANIB 3.0 1 7.68
CHEMBL205502 1 7.36
CHEMBL202011 1 7.30
CHEMBL380536 1 7.29
CHEMBL205325 1 7.20
CHEMBL377995 1 7.12
CHEMBL381182 1 7.12
CHEMBL153843 1 7.05
CHEMBL382218 1 7.04
CHEMBL204621 1 7.03
CHEMBL206123 1 6.96
CHEMBL382610 1 6.96
CHEMBL383334 1 6.96
CHEMBL205050 1 6.54
CHEMBL383123 1 6.54
CHEMBL204984 1 6.50
CHEMBL207975 1 6.41
CHEMBL207772 1 6.29
CHEMBL205544 1 6.28
CHEMBL383333 1 6.28
CHEMBL382142 1 6.23
CHEMBL383434 1 6.18
CHEMBL208363 1 6.14
CHEMBL205244 1 6.13
CHEMBL381293 1 6.12
CHEMBL205639 1 6.07
CHEMBL381577 1 5.96
CHEMBL24828 VANDETANIB 4.0 1 5.78
CHEMBL204425 1 5.67
CHEMBL205421 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101253 VATALANIB IC50 = 21.0 nM 7.68
CHEMBL205502 IC50 = 44.0 nM 7.36
CHEMBL202011 IC50 = 50.0 nM 7.30
CHEMBL380536 IC50 = 51.0 nM 7.29
CHEMBL205325 IC50 = 63.0 nM 7.20
CHEMBL377995 IC50 = 75.0 nM 7.12
CHEMBL381182 IC50 = 76.0 nM 7.12
CHEMBL153843 IC50 = 90.0 nM 7.05
CHEMBL382218 IC50 = 92.0 nM 7.04
CHEMBL204621 IC50 = 94.0 nM 7.03
CHEMBL383334 IC50 = 110.0 nM 6.96
CHEMBL382610 IC50 = 110.0 nM 6.96
CHEMBL206123 IC50 = 110.0 nM 6.96
CHEMBL205050 IC50 = 290.0 nM 6.54
CHEMBL383123 IC50 = 290.0 nM 6.54
CHEMBL204984 IC50 = 320.0 nM 6.50
CHEMBL207975 IC50 = 390.0 nM 6.41
CHEMBL207772 IC50 = 510.0 nM 6.29
CHEMBL205544 IC50 = 530.0 nM 6.28
CHEMBL383333 IC50 = 520.0 nM 6.28
CHEMBL382142 IC50 = 590.0 nM 6.23
CHEMBL383434 IC50 = 660.0 nM 6.18
CHEMBL208363 IC50 = 720.0 nM 6.14
CHEMBL205244 IC50 = 740.0 nM 6.13
CHEMBL381293 IC50 = 760.0 nM 6.12
CHEMBL205639 IC50 = 860.0 nM 6.07
CHEMBL381577 IC50 = 1110.0 nM 5.96
CHEMBL24828 VANDETANIB IC50 = 1660.0 nM 5.78
CHEMBL204425 IC50 = 2140.0 nM 5.67
CHEMBL205421 IC50 = 2540.0 nM 5.59
CHEMBL206136 IC50 - -
CHEMBL205901 IC50 > 10000.0 nM -
CHEMBL205647 IC50 > 10000.0 nM -
CHEMBL206089 IC50 > 10000.0 nM -
CHEMBL382797 IC50 > 10000.0 nM -
CHEMBL205684 IC50 > 10000.0 nM -
CHEMBL207099 IC50 > 10000.0 nM -
CHEMBL207049 IC50 > 10000.0 nM -
CHEMBL207821 IC50 > 10000.0 nM -
CHEMBL380421 IC50 > 10000.0 nM -
CHEMBL206670 IC50 - -
CHEMBL208229 IC50 - -
CHEMBL205869 IC50 - -
CHEMBL381704 IC50 - -
CHEMBL204846 IC50 - -