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Research ArticleArticle

Concentration Dependence 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 July 2020, 48 (7) 553-562; DOI: https://doi.org/10.1124/dmd.120.090563
Cornelius Trünkle
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Christian Lechner
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Daniel Korr
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Léa Bouché
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Naomi Barak
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Amaury Fernández-Montalván
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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  • ORCID record for Amaury Fernández-Montalván
Roderich D Süssmuth
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Andreas Reichel
Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
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Article Information

vol. 48 no. 7 553-562
DOI 
https://doi.org/10.1124/dmd.120.090563
PubMed 
32357973

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0090-9556
Online ISSN 
1521-009X
History 
  • Received January 31, 2020
  • Accepted April 7, 2020
  • Published online June 4, 2020.

Article Versions

  • Earlier version (May 1, 2020 - 02:20).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2020 by The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Cornelius Trünkle,
  2. Christian Lechner,
  3. Daniel Korr,
  4. Léa Bouché,
  5. Naomi Barak,
  6. Amaury Fernández-Montalván,
  7. Roderich D Süssmuth, and
  8. Andreas Reichel
  1. Bayer AG, Pharma R&D, Translational Sciences, Research Pharmacokinetics, Berlin, Germany (C.T., C.L., A.R.); Bayer AG, Pharma R&D, Therapeutic Compound Research, Berlin, Germany (D.K.); Bayer AG, Pharma R&D, Small Molecule Innovation, Berlin, Germany (L.B., N.B., A.F.-M) and Technische Universität Berlin, Institut für Chemie, Berlin, Germany (C.T., R.D.S.)
  1. Address correspondence to:
    Dr. Andreas Reichel, Bayer AG, Pharma R&D, Research Pharmacokinetics, Bldg. S109, 612, 13342 Berlin, Germany. E-mail: andreas.reichel{at}bayer.com
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Drug Metabolism and Disposition: 48 (7)
Drug Metabolism and Disposition
Vol. 48, Issue 7
1 Jul 2020
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Research ArticleArticle

Concentration Dependence of Kpuu

Cornelius Trünkle, Christian Lechner, Daniel Korr, Léa Bouché, Naomi Barak, Amaury Fernández-Montalván, Roderich D Süssmuth and Andreas Reichel
Drug Metabolism and Disposition July 1, 2020, 48 (7) 553-562; DOI: https://doi.org/10.1124/dmd.120.090563

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Research ArticleArticle

Concentration Dependence of Kpuu

Cornelius Trünkle, Christian Lechner, Daniel Korr, Léa Bouché, Naomi Barak, Amaury Fernández-Montalván, Roderich D Süssmuth and Andreas Reichel
Drug Metabolism and Disposition July 1, 2020, 48 (7) 553-562; DOI: https://doi.org/10.1124/dmd.120.090563
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