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Assay Detail

CHEMBL3887044

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

Binding
HTRF Assay: The effect of the compounds of the invention on the activity of the enzyme PDE3 was evaluated by the company CEREP (Le bois I'Evêque, 86600 Celle I'Evescault, France; http://www.cerep.fr) in accordance with its standard protocol (see Bender, A. T., Beavo, J. A. Pharmacol Rev. 2006, 58, 488-520: the enzyme PDE3A in recombinant form is expressed in Sf9 cells, the substrate is cAMP and the residual AMPc is measured by HTRF. The reference inhibitor in the test is milrinone, whose IC50 is 270 nM. The residual activity % are related to the control without inhibitor). The results are expressed either as the concentration which induces inhibition by 50% (IC50) or as a percentage inhibition measured at a set concentration of the compound.
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Aurora kinase A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Anti-cancer compound and pharmaceutical composition containing the same
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.05 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4112853 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4112853 IC50 = 900.0 nM 6.05