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Assay Detail

CHEMBL4021257

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ADMET
Inhibition of VEGFR-2 (unknown origin) by HTRF method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.
Zhao Y, Zhang J, Zhuang R, He R, Xi J, Pan X, Shao Y, Pan J, Sun J, Cai Z, Liu S, Huang W, Lv X.
Bioorg Med Chem (2017) 25 : 3195 -3205
PubMed 28412159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.10 10.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105717 CABOZANTINIB 4.0 1 10.07
CHEMBL388978 STAUROSPORINE 1 8.32
CHEMBL4104302 1 7.26
CHEMBL460702 BMS-777607 2.0 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105717 CABOZANTINIB IC50 = 0.086 nM 10.07
CHEMBL388978 STAUROSPORINE IC50 = 4.8 nM 8.32
CHEMBL4104302 IC50 = 55.0 nM 7.26
CHEMBL460702 BMS-777607 IC50 = 180.0 nM 6.75