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Label-free chemical probes
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JQ1 (1) is a potent and selective BET bromodomain inhibitor; (S)-(+)-JQ1 is the active enantiomer and the (R)-(−)-JQ1 is the negative control.128
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Labelled chemical probes
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Reporter tag, no linker
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[3H] Spiperone (2) is a high-affinity radioligand for the dopamine receptors, commonly used in radioligand binding assays and compound screening.132,133
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Reactive group and reporter tag, no linker
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Photoaffinity probe with radioisotope reporter tag of the 3,5-diaryl-oxadiazole based lead MX-126374 to study selective apoptosis in malignant cells.134
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Reporter tag with linker
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GB2-Cy3 (4) is a fluorescently-labelled glucose bioprobe for applicationsin high-throughput phenotypic screening to find therapeutic compounds for the treatment of cancer and diabetes.135
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Reactive group and reporter tag with linker
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PCI-33380 (5) is an activity-based fluorescent probe of the anti-cancer drug ibrutinib. The depicted probe was used to measure occupancy levels in cells and tissue, and permitted the prediction of efficacious dosage of the drug for patients in clinical trials.136
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Reactive group and reportertag with click handle
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The clickable activity-based probe (6) of the anti-cancer drug ibrutinib was used to study in-cell proteome selectivity in human cancer cells. The probe was designed to have minimal effect on the reactivity of the Michael acceptor, which subsequently was optimized to improve the selectivity profile of next generation analogues.137
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