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. 2024 Jan 19;14:1739. doi: 10.1038/s41598-023-50964-x

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© The Author(s) 2024

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 licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence 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 licence, visit http://creativecommons.org/licenses/by/4.0/.

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Impact of compound binding kinetics on biochemical EZH2 inhibition and comparison of kinetic-, thermodynamic- and conventional ligand efficiency parameters. (a) Representative enzyme inhibition curves for EZH2^+/+ by two reference inhibitors +/− compound and protein pre-incubation. (b) Effects of increasing compound and protein pre-incubation times on the inhibition of different PRC complexes by the compounds analyzed in this study. The color code represents maximum differences in pIC₅₀ values +/− compound and protein pre-incubation, using the no pre-incubation pIC₅₀ value as reference. The PRC complexes evaluated are indicated on the top. (c) Radar plots representing the ligand efficiencies of the compounds analyzed in this study calculated based on their biochemical inhibition (top left), TR-FRET equilibrium binding affinities at 25 °C (top right), residence times derived from TR-FRET kinetic binding (kPCA) assays at 25 °C (bottom left) and enthalpies from TR-FRET equilibrium binding affinities at multiple temperatures (bottom right).