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. 2023 Feb 8;14:686. doi: 10.1038/s41467-023-36246-0

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© The Author(s) 2023

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 6 — a–c Structures and VCPIP1 biochemical inhibitory activity of WH-9943-103C analogs. Data for hit WH-9943-103C are duplicated from earlier figures for ease of comparison. d DUB-ABPP data for the WH-103C focused library. Compounds with VCPIP1 biochemical IC₅₀ values below 250 nM (V02, V08, V12) were screened in ABPP at 10 μM, less potent compounds were screened at 50 μM. e, f SAR analysis suggested a combination of functionalities on V12 and V02 (yellow highlights) to yield CAS-12290-201. Binding kinetics and DUB-ABPP (10 and 1 µM) demonstrated that CAS-12290-201 to be a potent and selective inhibitor of the understudied DUB VCPIP1, error bars show the 95% confidence interval for parameters as fitted by GraphPad Prism 9.0.1.