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The development of USP1 allosteric inhibitors has progressed rapidly owing to their high selectivity and potency. However, the lack of appropriate chemical tools for developing a binding screen for this site has hampered the discovery of novel ligands. Herein, we developed the first allosteric fluoroprobe and fluorescence polarization (FP) assay for direct validation of USP1 allosteric inhibitors. The FP assay based on allosteric tracer\n                    <jats:bold>6\u20102<\/jats:bold>\n                    enabled the differentiation of known allosteric and catalytic site inhibitors, providing a robust and scalable tool for high\u2010throughput screening. In addition, a novel class of potent tetrahydroisoquinoline USP1 inhibitors was identified, and the representative compound\n                    <jats:bold>14a<\/jats:bold>\n                    possessed superior enzymatic and cellular activity compared with the clinical candidate\n                    <jats:bold>KSQ\u20104279,<\/jats:bold>\n                    with potent in vivo anti\u2010DLBCL efficacy and good druggability. Collectively, this study provides a valuable fluoroprobe, FP assay platform, and lead compounds targeting USP1 for further structural optimization and antitumor mechanism studies.\n                  <\/jats:p>","DOI":"10.1002\/advs.75350","type":"journal-article","created":{"date-parts":[[2026,4,22]],"date-time":"2026-04-22T13:46:56Z","timestamp":1776865616000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors"],"prefix":"10.1002","volume":"13","author":[{"given":"Jiawei","family":"Cheng","sequence":"first","affiliation":[{"name":"Key Laboratory of Structure\u2010Based Drug Design and Discovery, Ministry of Education Shenyang Pharmaceutical University  Shenyang China"},{"name":"State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica Chinese Academy of Sciences  Shanghai 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Institute of Materia Medica Chinese Academy of Sciences  Zhongshan China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Weijuan","family":"Kan","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica Chinese Academy of Sciences  Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yubo","family":"Zhou","sequence":"additional","affiliation":[{"name":"Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica Chinese Academy of Sciences  Zhongshan China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chunpu","family":"Li","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica Chinese Academy of Sciences  Shanghai China"},{"name":"School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced Study, UCAS  Hangzhou China"},{"name":"University of Chinese 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