G protein-coupled receptors (GPCRs) are one of the largest families of drug targets. This Review analyses drug discovery trends for GPCRs, covering compounds, targets and indications that have reached regulatory approval or that are being investigated in clinical trials, and also highlights the potential of untapped target–disease associations and pathway-biased signalling.
- Javier Sánchez Lorente
- Aleksandr V. Sokolov
- David E. Gloriam
