| Assay Method Information | |
| | Glosensor cAMP assay |
| Description: | In Vitro Evaluation of GPR52 Activation. Newly synthesized compounds were evaluated in a twelve-point concentration-response for GPR52 agonist activity using the Glosensor cAMP assay in HEK293 cells transiently expressing human GPR52. Transient expression of GPR52 resulted in a dramatic increase in basal cAMP levels (>100 fold over empty vector, FIG. 6 ), indicating that GPR52 displays high constitutive activity for the cAMP pathway. As summarized in Tables 1-4, the EC50 (nM) indicates the potency of these novel GPR52 agonists, while the efficacy (Emax) indicates the maximal activity to increase cAMP. The previously reported GPR52 agonist compound 4 was used as the reference compound to highlight SAR comparisons. |
| Affinity data for this assay | |
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