Fig. 2.

Agonistic activity of MTP, TAM, DOX, and BRM toward a GPCR panel. (A) PRESTO-TANGO (Parallel Receptor-ome Expression and Screening via Transcriptional Output-TANGO) screen of four known GPCR-targeted drugs (MTP, TAM, DOX, and BRM). These drugs were screened in 11 different combinations for their constitutive agonistic activity against 315 orphan and poorly annotated GPCRs (University of North Carolina collection). (B) Screening of multiple targets simultaneously in a parallel fashion. (C) Dose-dependent trials. These trials used the same system and 16 drug concentrations ranging from 0.001 nM to 100 µM. BRM dose-dependent values for HTR1A, DRD2, DRD3, and ADRA2C receptors were determined. RLU, relative luminescence unit.