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Assay Detail

CHEMBL4330409

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

Binding
Inhibition of TIE2 (unknown origin) after 4 hrs by ADP-Glo reagent based luminescent assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiopoietin-1 receptor (CHEMBL4128)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel anti-angiogenesis agents. Part 10: Multi-target inhibitors of VEGFR-2, Tie-2 and EphB4 incorporated with 1,2,3-triazol.
Pan X, Liang L, Si R, Wang J, Zhang Q, Zhou H, Zhang L, Zhang J.
Eur J Med Chem (2019) 163 : 1 -9
PubMed 30503935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.74 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4449700 1 9.59
CHEMBL4447552 1 9.55
CHEMBL4528844 1 9.52
CHEMBL4452256 1 9.44
CHEMBL1336 SORAFENIB 4.0 1 9.41
CHEMBL4570075 1 9.35
CHEMBL4441465 1 9.14
CHEMBL4556134 1 7.62
CHEMBL4454065 1 7.21
CHEMBL4456856 1 6.58
CHEMBL4556899 1 -
CHEMBL4473253 1 -
CHEMBL4470400 1 -
CHEMBL4519953 1 -
CHEMBL4449321 1 -
CHEMBL4443204 1 -
CHEMBL4440813 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4449700 IC50 = 0.26 nM 9.59
CHEMBL4447552 IC50 = 0.28 nM 9.55
CHEMBL4528844 IC50 = 0.3 nM 9.52
CHEMBL4452256 IC50 = 0.36 nM 9.44
CHEMBL1336 SORAFENIB IC50 = 0.39 nM 9.41
CHEMBL4570075 IC50 = 0.45 nM 9.35
CHEMBL4441465 IC50 = 0.73 nM 9.14
CHEMBL4556134 IC50 = 24.19 nM 7.62
CHEMBL4454065 IC50 = 61.26 nM 7.21
CHEMBL4456856 IC50 = 265.72 nM 6.58
CHEMBL4556899 IC50 > 1000.0 nM -
CHEMBL4473253 IC50 - -
CHEMBL4470400 IC50 > 1000.0 nM -
CHEMBL4519953 IC50 > 1000.0 nM -
CHEMBL4449321 IC50 > 1000.0 nM -
CHEMBL4443204 IC50 - -
CHEMBL4440813 IC50 - -