| Assay Method Information | |
| | Inhibition Assay |
| Description: | Measurement of PDE7 inhibition was carried out using a commercial phosphodiesterase activity measurement kit.Some of the compounds of the present invention (including those synthesised in Example 1) were evaluated. For this purpose, said compounds were incubated (in a range of concentrations from 0.1 nM to 100 μM) in the presence of 0.02 U/well of PDE7A1 and 0.05 μCi of [3H] cAMP, for 20 minutes at 30° C. in the assay buffer supplied with the kit (total volume per well=100 μL). Once this time had elapsed, 50 μL of a 20 mg/mL suspension of SPA glass silicate microspheres were added and kept in agitation at ambient temperature for 60 minutes. After allowing the plate to rest for 20 minutes, the radioactivity was tested in a scintillation detector. All the assays included two points in the absence of PDE7A1 (blank/negative control) and two points with PDE7A1 in the absence of inhibitors (positive control). |
| Affinity data for this assay | |
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