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Assay Detail

CHEMBL867220

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

Binding
Inhibitory activity against VEGFR-1 using 2 uM ATP by HTRF assay
42
Total Activities
42
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 1 (CHEMBL1868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.
Kiselyov AS, Semenova M, Semenov VV, Piatnitski E.
Bioorg Med Chem Lett (2006) 16 : 1726 -1730
PubMed 16364640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.38 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24828 VANDETANIB 4.0 1 7.00
CHEMBL101253 VATALANIB 3.0 1 6.85
CHEMBL382855 1 6.85
CHEMBL202011 1 6.80
CHEMBL153843 1 6.77
CHEMBL425587 1 6.75
CHEMBL203003 1 6.66
CHEMBL204548 1 6.66
CHEMBL205984 1 6.58
CHEMBL206279 1 6.52
CHEMBL206348 1 6.47
CHEMBL377081 1 6.47
CHEMBL203167 1 6.44
CHEMBL437889 1 6.39
CHEMBL204099 1 6.36
CHEMBL206403 1 6.31
CHEMBL203243 1 6.27
CHEMBL202643 1 6.24
CHEMBL380932 1 6.21
CHEMBL206185 1 6.16
CHEMBL202805 1 6.13
CHEMBL203965 1 6.12
CHEMBL382584 1 6.11
CHEMBL203063 1 6.02
CHEMBL205413 1 5.94
CHEMBL382478 1 5.94
CHEMBL205610 1 5.90
CHEMBL380503 1 5.60
CHEMBL379888 1 -
CHEMBL382256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24828 VANDETANIB IC50 = 100.0 nM 7.00
CHEMBL101253 VATALANIB IC50 = 140.0 nM 6.85
CHEMBL382855 IC50 = 140.0 nM 6.85
CHEMBL202011 IC50 = 160.0 nM 6.80
CHEMBL153843 IC50 = 170.0 nM 6.77
CHEMBL425587 IC50 = 180.0 nM 6.75
CHEMBL203003 IC50 = 220.0 nM 6.66
CHEMBL204548 IC50 = 220.0 nM 6.66
CHEMBL205984 IC50 = 260.0 nM 6.58
CHEMBL206279 IC50 = 300.0 nM 6.52
CHEMBL206348 IC50 = 340.0 nM 6.47
CHEMBL377081 IC50 = 340.0 nM 6.47
CHEMBL203167 IC50 = 360.0 nM 6.44
CHEMBL437889 IC50 = 410.0 nM 6.39
CHEMBL204099 IC50 = 440.0 nM 6.36
CHEMBL206403 IC50 = 490.0 nM 6.31
CHEMBL203243 IC50 = 540.0 nM 6.27
CHEMBL202643 IC50 = 570.0 nM 6.24
CHEMBL380932 IC50 = 610.0 nM 6.21
CHEMBL206185 IC50 = 690.0 nM 6.16
CHEMBL202805 IC50 = 740.0 nM 6.13
CHEMBL203965 IC50 = 760.0 nM 6.12
CHEMBL382584 IC50 = 770.0 nM 6.11
CHEMBL203063 IC50 = 950.0 nM 6.02
CHEMBL205413 IC50 = 1160.0 nM 5.94
CHEMBL382478 IC50 = 1140.0 nM 5.94
CHEMBL205610 IC50 = 1250.0 nM 5.90
CHEMBL380503 IC50 = 2530.0 nM 5.60
CHEMBL203429 IC50 > 10000.0 nM -
CHEMBL377952 IC50 > 10000.0 nM -
CHEMBL205401 IC50 > 10000.0 nM -
CHEMBL206215 IC50 > 10000.0 nM -
CHEMBL202682 IC50 > 10000.0 nM -
CHEMBL205876 IC50 > 10000.0 nM -
CHEMBL206567 IC50 > 10000.0 nM -
CHEMBL381786 IC50 > 10000.0 nM -
CHEMBL206388 IC50 > 10000.0 nM -
CHEMBL203110 IC50 - -
CHEMBL382596 IC50 - -
CHEMBL205138 IC50 - -
CHEMBL382256 IC50 > 10000.0 nM -
CHEMBL379888 IC50 > 10000.0 nM -