Potency data for probe JNJ-42396302 and control JNJ-40573663
In vitro potency
| Target name | Target information | Species | Assay description | JNJ-42396302 | JNJ-40573663 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PDE10A | Recombinant human protein expressed in Sf9 cells (using baculovirus expression system) | Homo sapiens | SPA with human PDE10A : [3H]cAMP substrate | Ki = 13 nM | ||
| PDE10A | Recombinant rat protein expressed in Sf9 cells (using baculovirus expression system) | Rattus sp. | SPA with rat PDE10A : [3H]cAMP substrate | Ki = 19 nM | ||
| PDE10A | Recombinant mouse protein expressed in Sf9 cells (using baculovirus expression system) | Mus musculus | SPA with mouse PDE10A : [3H]cAMP substrate | Ki = 11 nM | ||
| PDE10A | Recombinant human protein expressed in Sf9 cells (using baculovirus expression system) | Homo sapiens | In vitro assay with human PDE10A | IC50 > 10 µM |
In cell potency
| Target name | Target information | Species | Assay description | Compound conc. | JNJ-42396302 | JNJ-40573663 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| PDE10A | HEK293 cells stably transfected with mouse PDE10A1 and transiently cotransfected with pCRE-Luc plasmid | Mus musculus | Luciferase activity assay at 1 mikroM: The activity of the luciferase is measured using a luminescent substrate. | 1 µM | Increase in cAMP = 2.3 fold | ||
| PDE10A | HEK293 cells stably transfected with mouse PDE10A1 and transiently cotransfected with pCRE-Luc plasmid | Mus musculus | Luciferase activity assay at 10 mikroM: The activity of the luciferase is measured using a luminescent substrate. | 10 µM | Increase in cAMP = 10 fold |