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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.
Trünkle, Cornelius; Lechner, Christian; Korr, Daniel; Bouché, Léa; Barak, Naomi; Fernández-Montalván, Amaury; Süssmuth, Roderich D; Reichel, Andreas.
Affiliation
  • Trünkle C; 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 U
  • Lechner C; 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 U
  • Korr D; 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 U
  • Bouché L; 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 U
  • Barak N; 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 U
  • Fernández-Montalván A; 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 U
  • Süssmuth RD; 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 U
  • Reichel A; 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 U
Drug Metab Dispos ; 48(7): 553-562, 2020 07.
Article in En | MEDLINE | ID: mdl-32357973
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Enzyme Inhibitors / Histone Acetyltransferases / Models, Biological Type of study: Prognostic_studies Limits: Humans Language: En Journal: Drug Metab Dispos Journal subject: FARMACOLOGIA Year: 2020 Type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Enzyme Inhibitors / Histone Acetyltransferases / Models, Biological Type of study: Prognostic_studies Limits: Humans Language: En Journal: Drug Metab Dispos Journal subject: FARMACOLOGIA Year: 2020 Type: Article