Specific radiation damage to halogenated inhibitors and ligands in protein–ligand crystal structures
Matthew J. Rodrigues, Marc Cabry, Gavin W. Collie, Michael W. Carter et autres
Protein–inhibitor crystal structures aid medicinal chemists in efficiently improving the potency and selectivity of small-molecule inhibitors. It is estimated that a quarter of lead molecules in drug discovery projects are halogenated. Protein–inhibitor crystal structures have shed light on the role of halogen …
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