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. 2015 Nov;10(11):1793-6.
doi: 10.1002/cmdc.201500310. Epub 2015 Aug 25.

The Role of Target Binding Kinetics in Drug Discovery

Dong Guo  1 , Laura H Heitman  1 , Adriaan P IJzerman  2
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The Role of Target Binding Kinetics in Drug Discovery

Dong Guo et al. ChemMedChem. 2015 Nov.

Abstract

Traditionally structure-activity/affinity relationships (SAR) have dominated research in medicinal chemistry. However, structure-kinetics relationships (SKR) can be very informative too. In this viewpoint we explore the molecular determinants of binding kinetics and discuss challenges for future binding kinetics studies. A scheme for future kinetics-directed drug design and discovery is also proposed.

Keywords: G protein-coupled receptors; binding kinetics; residence time; structure-affinity relationships; structure-kinetics relationships.

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