Jianjun Cheng group’s research is focused on the medicinal chemistry and drug discovery targeting human G protein-coupled receptors (GPCRs). GPCRs play important roles in many (patho) physiological conditions and they are targeted by more than 30% of known small molecule drugs. We focus on important validated and emerging GPCR drug targets and design novel ligands of these receptors in the aim of discovering novel drug candidates with therapeutic advantages as well as useful chemical tools for the biological study of GPCRs. Besides conventional GPCR agonists/antagonists and positive/negative allosteric modulators,biased ligands of GPCRs is one of our most important researchdirections. Biased ligands will  nd their applications in novel drugdiscovery targeting cannonical GPCRs as well as in providing chemical tools in studying biased signaling of GPCRs.