Binding efficacy

The drive to produce stereoisomerically pure drugs is based on the recognition that there are pharmacological differences between drug stereoisomers. These differences are addressed in the third section of this book, which discusses the pharmacokinetic, plasma protein binding, efficacy, toxicity, and biotransformation of stereoisomeric drugs. 

Key Words [ SlGTPyS cannabinoid cannabinoid CBi receptor cell culture intact cells brain membranes radioligand binding efficacy. 

Hit to lead Physicochemical properties (solubility, Log P) PAMPA Plasma protein binding Efficacy species and human liver microsomal stability, CAR and PXR transactivation assay... 

Avantaggiato G, Havenaar R, Visconti A. Evaluation of the intestinal absorption of deoxynivalenol and nivalenol by an in vitro gastrointestinal model, and the binding efficacy of activated carbon and other adsorbent materials. Food Chem Toxicol. 2004 42 817-824. 

In our laboratories, we prepared a systematic array of polymers of varying hydrophobicity and charge. We devised tests to measure the fat binding efficacy of these materials. This included an in vivo animal model using... 

In many cases, one would like to calculate not only the total free energy, but also the entropic and enthalpic contributions thereto. Knowledge of these components can frequently lead to better understanding of the underlying reasons for molecular preferences, e.g., differences in the binding efficacies of related ligands. Obviously, we can attempt to determine AH between two endpoint A states 0 and 1 as the directly calculated difference in their potential energies ... 

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