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. 2018 May 1;8:6846. doi: 10.1038/s41598-018-25158-5

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© The Author(s) 2018

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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In vitro profiling of FXR modulation by 4. (A) At 20 µM, 4 significantly enhances transactivation efficacy of FXR agonists 1–3 in a full-length FXR reporter gene assay. (B) Dose-response curves of FXR agonist 1 and compound 4 in presence of a fixed concentration of the respective other agent confirms increased maximum relative transactivation without marked changes in EC₅₀-values. The maximum relative transactivation exceeds the sum of the single compounds’ maximum relative transactivation suggesting synergy. (C) 4 does not activate FXR’s heterodimer partner RXR. (D) 4 is a potent inhibitor of the kinases Abl, c-Kit and PDGF-Rα but does not markedly inhibit kinases that interact with FXR. (E) 4 does not modulate the membrane bile acid receptor TGR5. *p < 0.05, **p < 0.01, ***p < 0.001.