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Assay Detail

CHEMBL829593

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

Binding
Inhibitory concentration against human vascular endothelial growth factor receptor 2
13
Total Activities
13
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

Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
Miyazaki Y, Matsunaga S, Tang J, Maeda Y, Nakano M, Philippe RJ, Shibahara M, Liu W, Sato H, Wang L, Nolte RT.
Bioorg Med Chem Lett (2005) 15 : 2203 -2207
PubMed 15837294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.88 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194911 1 8.52
CHEMBL196841 1 7.44
CHEMBL193752 1 7.24
CHEMBL194149 1 7.21
CHEMBL194150 1 7.19
CHEMBL363389 1 6.75
CHEMBL195567 1 6.73
CHEMBL194057 1 6.46
CHEMBL196021 1 5.95
CHEMBL196022 GW642125X 1 5.26
CHEMBL373073 GW642138X 1 -
CHEMBL362915 1 -
CHEMBL383603 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194911 IC50 = 3.0 nM 8.52
CHEMBL196841 IC50 = 36.0 nM 7.44
CHEMBL193752 IC50 = 58.0 nM 7.24
CHEMBL194149 IC50 = 62.0 nM 7.21
CHEMBL194150 IC50 = 65.0 nM 7.19
CHEMBL363389 IC50 = 180.0 nM 6.75
CHEMBL195567 IC50 = 186.0 nM 6.73
CHEMBL194057 IC50 = 350.0 nM 6.46
CHEMBL196021 IC50 = 1120.0 nM 5.95
CHEMBL196022 GW642125X IC50 = 5500.0 nM 5.26
CHEMBL373073 GW642138X IC50 > 17000.0 nM -
CHEMBL362915 IC50 > 20000.0 nM -
CHEMBL383603 IC50 - nM -