Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

  • Paul V. Fish
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • Panagis Filippakopoulos
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Gerwyn Bish
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • Paul E. Brennan
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Mark E. Bunnage
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • Andrew S. Cook
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • Oleg Federov
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Brian S. Gerstenberger
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Eastern Pont Road, Groton, Connecticut 06340, United States
  • Hannah Jones
    Pfizer Worldwide R&D, 35/200 Cambridgepark Drive, Cambridge, Massachusetts 02140, United States
  • Stefan Knapp
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Brian Marsden
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Karl Nocka
    Pfizer Worldwide R&D, 35/200 Cambridgepark Drive, Cambridge, Massachusetts 02140, United States
  • Dafydd R. Owen
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • Martin Philpott
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Sarah Picaud
    Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom
  • Michael J. Primiano
    Pfizer Worldwide R&D, 35/200 Cambridgepark Drive, Cambridge, Massachusetts 02140, United States
  • Michael J. Ralph
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • Nunzio Sciammetta
    Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom
  • John D. Trzupek
    Pfizer Worldwide R&D, 35/200 Cambridgepark Drive, Cambridge, Massachusetts 02140, United States

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