The article provides an in-depth analysis of the current trends in G protein-coupled receptor (GPCR) drug discovery, focusing on molecule types, drug targets, and therapeutic indications. It highlights that 481 drugs (approximately 34% of all FDA-approved drugs) act at 107 unique GPCR targets, with 320 agents currently in clinical trials. The study reveals a shift towards diabetes, obesity, and Alzheimer's disease as major disease indications, while other central nervous system disorders remain highly represented. The article also discusses the increasing focus on novel GPCR targets, particularly in genetic and immune system disorders, and the growing number of biological drugs, allosteric modulators, and biased agonists. Additionally, it explores the impact of GPCR structures on drug discovery, the emergence of biased signaling as a novel mechanism for achieving functional selectivity, and the potential of orphan receptors as new therapeutic targets. The authors provide an interactive online resource (gpcrdb.org) to analyze and infer trends in GPCR drug discovery, emphasizing the broad therapeutic potential of GPCRs in addressing various diseases.The article provides an in-depth analysis of the current trends in G protein-coupled receptor (GPCR) drug discovery, focusing on molecule types, drug targets, and therapeutic indications. It highlights that 481 drugs (approximately 34% of all FDA-approved drugs) act at 107 unique GPCR targets, with 320 agents currently in clinical trials. The study reveals a shift towards diabetes, obesity, and Alzheimer's disease as major disease indications, while other central nervous system disorders remain highly represented. The article also discusses the increasing focus on novel GPCR targets, particularly in genetic and immune system disorders, and the growing number of biological drugs, allosteric modulators, and biased agonists. Additionally, it explores the impact of GPCR structures on drug discovery, the emergence of biased signaling as a novel mechanism for achieving functional selectivity, and the potential of orphan receptors as new therapeutic targets. The authors provide an interactive online resource (gpcrdb.org) to analyze and infer trends in GPCR drug discovery, emphasizing the broad therapeutic potential of GPCRs in addressing various diseases.