G protein-coupled receptors (GPCRs) are capable of downstream signaling through distinct
noncanonical pathways such as β-arrestins in addition to the canonical G protein-dependent …

Functionally selective G protein-coupled receptor (GPCR) ligands, which differentially
modulate canonical and noncanonical signaling, are extremely useful for elucidating key …

The high affinity dopamine D4 receptor ligand APH199 and derivatives thereof exhibit bias
toward the Gi signaling pathway over β-arrestin recruitment compared to quinpirole. Based …

Noncatechol heterocycles have recently been discovered as potent and selective G protein
biased dopamine 1 receptor (D1R) agonists with superior pharmacokinetic properties. To …

The discovery of functionally biased and physiologically beneficial ligands directed toward G-
protein coupled receptors (GPCRs) has provided the impetus to design dopamine D2 …

The forward (kon) and reverse (koff) rate constants of drug–target interactions have
important implications for therapeutic efficacy. Hence, time-resolved assays capable of …

Biased ligands (also known as functionally selective ligands) of G protein-coupled receptors
are valuable tools for dissecting the roles of G protein-dependent and independent signaling …

Biased agonism at GPCRs highlights the potential for the discovery and design of pathway-
selective ligands and may confer therapeutic advantages to ligands targeting the dopamine …

Functionally selective ligands stabilize conformations of G protein-coupled receptors
(GPCRs) that induce a preference for signaling via a subset of the intracellular pathways …

Dopamine receptors are important G protein-coupled receptors (GPCRs) with therapeutic
opportunities for treating Parkinson's Disease (PD) motor and cognitive deficits. Biased D1 …