Ranking of High‐Affinity Ligands by NMR Spectroscopy
Xiaolu Zhang, Andrea Sänger, René Hemmig, Wolfgang Jahnke · Angewandte Chemie International Edition · 2009
Let the protein choose its ligand, and use NMR spectroscopy to see which one it has chosen (see scheme). This principle enables the most precise determination of relative binding affinities of two ligands to a protein receptor and for the first time allows the affinities of tightly binding ligands to be determined by NMR spectroscopy. This approach is a valuable tool for the lead-optimization process.