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Protein crystallography is a more sensitive technique than the conventional bioassays used in HTS and can typically identify the binding of much weaker ligands (in the mM affinities compared with the µM range in bioassays).

Thus x-ray crystallography boasts an illustrious career. Protein crystallography has progressed from a discipline driven by technology to a field driven by biological, physiological, or pharmaceutical questions. The recent structure determinations of ribosomes and their subunits 25–27 show that even vast multimolecular complexes are amenable to crystallographic analysis, and have provided detailed information as to the workings of, e.g., antibiotics. 28

X-ray Crystallography - Chemistry LibreTexts

X-ray crystallography - Wikipedia

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