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.