Assay Method Information

Assay Name:  HTRF Assay
Description:  The effect of the compounds of the invention on the activity of the enzyme PDE3 was evaluated by the company CEREP (Le bois I'Ev que, 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.
Affinity data for this assay
 

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