Finding substances that alter the activity of GPCRs to increase or decrease signal transduction cascades in different cell types and tissues is one method used in current drug discovery. As a result of this approach, new medications have been created to treat a wide range of illnesses, such as mental health issues, HIV/AIDS, cardiovascular disease, some types of cancer, and Type 2 diabetic mellitus (T2DM). These achievements support the further investigation of GPCRs as disease targets and offer important insights that should aid in the development of new therapeutic drugs. This paper examines the state of GPCR drug discovery today, focusing on initiatives to create novel compounds for the treatment of obesity and type 2 diabetes. We examine past attempts to develop GPCR-based medications to treat metabolic diseases in order to identify the contributing variables that led to their success and failure in this attempt