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Researchers at the Memorial Sloan Kettering Cancer Center in New York are preparing the first test in humans of a new type of diagnostic that combines a radioisotope and antibody via bioorthogonal ‘click’ chemistry. The trial is expected to be a proof of principle of the clinical potential of bioorthogonal chemistry—reactions that can be performed in living systems without interfering with the surrounding biology. Over the past two decades, this type of chemistry has been increasingly used by bio-inorganic and medicinal chemists, most notably in the development of targeted medicines, such as antibody-drug conjugates (ADCs). But the Sloan Kettering trial will be first test of such reactions inside human participants.