IBC advertised their seventh annual symposium on G protein-coupled receptors (GPCRs) under the heading 'GPCRs still the best drug targets' and, at the end of the 3-day meeting which took place at the Hilton San Diego Resort (October 14-16 2002), it seemed like an appropriate description. The meeting brought together researchers from a wide range of disciplines, and from both academia and industry, to discuss recent advances in GPCR biology, pharmacology and drug design. This review will cover the main themes that emerged during the meeting, with an emphasis on those areas that impact drug discovery.