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Assay Detail

CHEMBL3857915

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

Binding
Inhibition of TIE-2 (unknown origin)
2
Total Activities
2
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

The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
Talele TT.
J Med Chem (2016) 59 : 8712 -8756
PubMed 27299736 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.97 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545365 ALTIRATINIB 2.0 1 8.10
CHEMBL2105717 CABOZANTINIB 4.0 1 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545365 ALTIRATINIB IC50 = 8.0 nM 8.10
CHEMBL2105717 CABOZANTINIB IC50 = 14.3 nM 7.84