We work towards achieving a molecular level understanding of G protein-coupled receptors (GPCRs). We aim to (1) discover molecules that can be used to probe the mechanisms of these receptors in various pathophysiological state and (2) to streamline the development of those molecules as therapeutic agents. We design and synthesize templates based on small molecules, peptides and peptidomimetics. The synthetic strategies involve multi-step organic synthesis, microwave techniques and solid-phase peptide synthesis using automated, semi-automated, and manual synthesizers. The lead optimization and structure-activity studies generally use focused-library design or high throughput screening approach.