C
Claire Mackie
Researcher at Janssen Pharmaceutica
Publications - 58
Citations - 2543
Claire Mackie is an academic researcher from Janssen Pharmaceutica. The author has contributed to research in topics: In vivo & Allosteric modulator. The author has an hindex of 23, co-authored 57 publications receiving 2302 citations. Previous affiliations of Claire Mackie include Janssen-Cilag & Johnson & Johnson Pharmaceutical Research and Development.
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Journal ArticleDOI
MetaSite: understanding metabolism in human cytochromes from the perspective of the chemist.
Gabriele Cruciani,Emanuele Carosati,Benoit Christian Albert Ghislain De Boeck,Kantharaj Ethirajulu,Claire Mackie,Trevor Howe,Riccardo Vianello +6 more
TL;DR: A new method is presented that provides the cytochrome involved and the site of metabolism for any human cy tochrome P450 (CYP) mediated reaction acting on new substrates, and can be applied automatically to all the cy tochromes for which 3D structure is known.
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Prediction of human pharmacokinetics using physiologically based modeling: a retrospective analysis of 26 clinically tested drugs.
Stefan S De Buck,Vikash K. Sinha,Luca A. Fenu,Marjoleen J.M.A Nijsen,Claire Mackie,Ron Gilissen +5 more
TL;DR: The physiologically based pharmacokinetics (PBPK) model, which combined methods Vd2 and CL2 yielded the most accurate predictions of in vivo terminal half-life (69% within 2-fold), demonstrates that PBPK models can lead to reasonable predictions of human pharmacokinetic predictions.
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In vivo, in vitro and in silico methods for small molecule transfer across the BBB
TL;DR: This review gives a comprehensive overview of different approaches currently considered in drug discovery to circumvent the lack of small molecule transfer through the BBB, together with their inherent advantages and disadvantages.
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Anxiolytic- and antidepressant-like profile of a new CRF1 receptor antagonist, R278995/CRA0450.
Shigeyuki Chaki,Atsuro Nakazato,Ludo Edmond Josephine Kennis,Masato Nakamura,Claire Mackie,Masayuki Sugiura,Petra Vinken,David Ashton,Xavier Langlois,Thomas Steckler +9 more
TL;DR: Results indicate that R278995/CRA0450 is an orally active CRF (1) and sigma(1) receptor antagonist with potent anxiolytic-like and antidepressant-like activities.
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Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents
Jerri M. Rook,Zixiu Xiang,Xiaohui Lv,Ayan Ghoshal,Jonathan W. Dickerson,Thomas M. Bridges,Kari A. Johnson,Daniel J. Foster,Karen J. Gregory,Karen J. Gregory,Paige N. Vinson,Analisa D. Thompson,Nellie Byun,Rebekah L. Collier,Michael Bubser,Michael T. Nedelcovych,Robert W. Gould,Shaun R. Stauffer,J. Scott Daniels,Colleen M. Niswender,Hilde Lavreysen,Claire Mackie,Susana Conde-Ceide,Jesús Alcázar,José Manuel Bartolomé-Nebreda,Gregor James Macdonald,John Talpos,Thomas Steckler,Carrie K. Jones,Craig W. Lindsley,P. Jeffrey Conn +30 more
TL;DR: Interestingly, VU0409551 produced robust antipsychotic-like and cognition-enhancing activity in animal models and suggest that modulation of NMDAR currents is not critical for in-vivo efficacy, providing surprising new mechanistic insights into the actions of mGlu5 PAMs.