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Higher Contrast in 1H-Observed NMR Ligand Screening with the PEARLScreen Experiment
Higher Contrast in 1H-Observed NMR Ligand Screening with the PEARLScreen Experiment
For initial hit identification in fragment-based drug design, NMR is one of the preferred methods, with the well-established ligand screening experiments T1?, waterLOGSY and STD. Here, we present a new, perfect echo-based experiment with superior binding sensitivity, the PEARLScreen. The sensitivity enhancement is based on longer relaxation delays as well as active exchange broadening, enabled by the perfect echo scheme. This allowed a reduction of the protein concentration by up to one order of... More... |
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