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Since its first description in 1999, BRET has been widely applied in chemical biology research and drug discovery. Today, it is regarded as one of the most versatile methods for investigating the dynamics of ligand\u2013protein and protein\u2013protein interactions, both in cell\u2010free systems and living cells. Owing to several advantages, including compatibility with high\u2010throughput screening, suitability for cellular target engagement studies, and the ability to monitor real\u2010time kinetics, BRET\u2010based binding assays have become indispensable tools, particularly in early\u2010stage drug discovery. Consequently, over the past decade these approaches have been extensively used for major drug target classes such as G protein\u2010coupled receptors (GPCRs), kinases, and proteases. Despite the high relevance of ion channels as drug targets\u2014approximately one\u2010fifth of all approved drugs act on them\u2014BRET\u2010based assays have so far played only a limited role in this field. Here, we summarize recent applications of BRET\u2010based methods for ion channels with a particular focus on approaches for studying ligand\u2010ion channel interactions, highlighting current challenges and, more importantly, the significant potential of this technology to advance ion channel\u2013focused drug discovery.<\/jats:p>","DOI":"10.1002\/ardp.70325","type":"journal-article","created":{"date-parts":[[2026,9,3]],"date-time":"2026-09-03T14:20:40Z","timestamp":1788445240000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["BRET\u2010Based Approaches for Ion Channels: Emerging Applications and Future Directions"],"prefix":"10.1002","volume":"359","author":[{"given":"Nadine","family":"Kock","sequence":"first","affiliation":[{"name":"Institute for Pharmaceutical and Medical Chemistry, Faculty of Chemistry and Pharmacy University of M\u00fcnster  M\u00fcnster Germany"},{"name":"GRK 2515, Chemical biology of ion 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