G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one of
the prime targets for marketed drugs. While traditional drug discovery programs have …

G protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology;
about one-third of all marketed drugs target members of this family. GPCR allosteric ligands …

G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

G-protein-coupled receptors (GPCRs) are the largest class of signaling receptors that are
most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at …

Traditionally, optimizing lead molecule interactions with the orthosteric site has been viewed
as the best means for attaining selectivity at G protein-coupled receptors (GPCRs), but …

Terms such as “nondruggable GPCRs” describe a unique group of GPCRs having strong
biological hypothesis validation, but for which medicinal chemistry efforts based on …

Designing covalent allosteric modulators brings new opportunities to the field of drug
discovery towards G-protein-coupled receptors (GPCRs). Targeting an allosteric binding …

Allosteric ligands bind to G protein-coupled receptors (GPCRs; also known as seven-
transmembrane receptors) at sites that are distinct from the sites to which endogenous …

G protein-coupled receptors (GPCRs) are one of the most important classes of proteins in
the genome, not only because of their tremendous molecular diversity but because they are …

In recent years, the concept of allosteric modulation of G-protein-coupled receptors (GPCRs)
has matured and now represents an increasingly viable approach to drug discovery. This is …