This satellite meeting provided an insight into the current status and progress with GPCR allosterism and interacting accessory proteins. With one compound on the market (cinacalcet) and several others in clinical development (eg, targeting M1 and mGluR2), it is clear that targeting allosteric sites on GPCRs represents a valid approach to identifying novel drugs. Targeting allosteric sites may confer additional selectivity and permit conformational changes in GPCRs to enable disruption of large protein-protein interactions (eg, CCR5). Despite emerging research on the potential of interacting accessory proteins as drug targets, further research to understand these interactions are required before initiating focused drug discovery programs that specifically target GPCR-interacting proteins.