Drug discovery on membrane proteins is still a difficult task, despite the recognized importance of membrane proteins as drug targets. Here, we present an overview of NMR methods available for structure-based drug design on membrane proteins. NMR spectroscopy is capable of identifying potential binders in screening and defining their relative binding constants, binding stoichiometry, conformation in the binding pocket and the relative binding orientation for binders of different series. Examples are given in the review highlighting the potential of NMR spectroscopy for future progress in drug discovery on membrane proteins.
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