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Research ArticleArticle

Concentration dependency of the unbound partition coefficient Kpuu and its application to correct for exposure related discrepancies between biochemical and cellular potency of KAT6A inhibitors

Cornelius Trünkle, Christian Lechner, Daniel Korr, Léa Bouché, Naomi Barak, Amaury Fernández-Montalván, Roderich D Süssmuth and Andreas Reichel
Drug Metabolism and Disposition May 1, 2020, dmd.120.090563; DOI: https://doi.org/10.1124/dmd.120.090563
Cornelius Trünkle
1 Technische Universität Berlin;
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  • For correspondence: andreas.reichel@bayer.com cornelius.truenkle@googlemail.com
Christian Lechner
2 Bayer AG;
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Daniel Korr
2 Bayer AG;
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Léa Bouché
2 Bayer AG;
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Naomi Barak
2 Bayer AG;
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Amaury Fernández-Montalván
3 Servier
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  • ORCID record for Amaury Fernández-Montalván
Roderich D Süssmuth
1 Technische Universität Berlin;
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Andreas Reichel
2 Bayer AG;
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  • For correspondence: andreas.reichel@bayer.com cornelius.truenkle@googlemail.com

Data Supplement

  • Supplemental Figures -

    Supplementary Figure 1 -  Chemical structure of previously published KAT6A inhibitors WM-8014 (A) and WM-1119 (B) that were included in this study.

    Supplementary Figure 2 - Concentration dependent cellular accumulation ratio (Kp) in
    ZR75-1 cells for all investigated KAT6A inhibitors in this study (A-L).

    Supplementary Figure 3 - Concentration dependent Kpuu,cyto determined with the saturation method and observed in vitro potency against ZR75-1 cells for all KAT6A inhibitors in this study (A-L).

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