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 membrane proteins that modulate physiology
across human tissues in response to extracellular signals. GPCR-mediated signalling can …

Among the valuable saturated bicyclic structures incorporated in newly developed bio-active
compounds, bicyclo [2.1. 1] hexanes are playing an increasingly important role, while being …

We present the direct and stereoretentive deuteration of primary amines using Ru-bMepi
(bMepi= 1, 3-(6′-methyl-2′-pyridylimino) isoindolate) complexes and D2O. High …

Agonist bias occurs when different ligands produce distinct signalling outputs when acting at
the same receptor. However, its physiological relevance is not always clear. Using primary …

Drugs targeting adenosine receptors (AR) can provide treatment for diseases. We report the
identification of 7-(phenylamino)-pyrazolo [3, 4-c] pyridines L2–L10, A15, and A17 as low …

Introduction Escalating costs and inherent uncertainties associated with drug discovery
invite initiatives to improve its efficiency and de-risk campaigns for inventing better …

The complex pharmacology of G-protein-coupled receptors (GPCRs) is defined by their multi-
state conformational dynamics. Single-molecule Förster Resonance Energy Transfer …

The development of therapeutic agonists for G protein-coupled receptors (GPCRs) is
hampered by the propensity of GPCRs to couple to multiple intracellular signalling …

The adenosine A3 receptor (A3R) belongs to a family of four adenosine receptor (AR)
subtypes which all play distinct roles throughout the body. A3R antagonists have been …