The cannabinoid CB 2 receptor (CB 2 R) represents a promising therapeutic target for various
forms of tissue injury and inflammatory diseases. Although numerous compounds have …

The function of G protein-coupled receptors (GPCRs) can be modulated by a number of
endogenous allosteric molecules. In this study, we used molecular dynamics, radioligand …

Recently we identified a sodium ion binding pocket in a high-resolution structure of the human
adenosine A 2A receptor. In the present study we explored this binding site through site-…

We report the synthesis and evaluation of previously unreported 4-amino-6-aryl-5-cyano-2-thiopyrimidines
as selective human adenosine A 1 receptor (hA 1 AR) agonists with tunable …

Classical drug design and development rely mostly on affinity‐ or potency‐driven structure–activity
relationships (SAR). Thus far, a given compound’s binding kinetics have been largely …

There is a growing interest in understanding the binding kinetics of compounds that bind to
G protein-coupled receptors prior to progressing a lead compound into clinical trials. The …

Scintillation proximity assay (SPA) is a radio-isotopic technology format used to measure a
wide range of biological interactions, including drug-target binding affinity studies. The assay …

We expanded on a series of pyrido[2,1-f]purine-2,4-dione derivatives as human adenosine
A 3 receptor (hA 3 R) antagonists to determine their kinetic profiles and affinities. Many …

The human adenosine A 3 (hA 3 ) receptor has been suggested as a viable drug target in
inflammatory diseases and in cancer. So far, a number of selective hA 3 receptor agonists (eg …

While equilibrium binding affinities and in vitro functional antagonism of CB1 receptor
antagonists have been studied in detail, little is known on the kinetics of their receptor interaction. …