Publications by authors named "Steven Whitebread"

20Publications

The activities of drug inactive ingredients on biological targets.

Authors:
Joshua Pottel Duncan Armstrong Ling Zou Alexander Fekete Xi-Ping Huang Hayarpi Torosyan Dallas Bednarczyk Steven Whitebread Barun Bhhatarai Guiqing Liang Hong Jin S Nassir Ghaemi Samuel Slocum Katalin V Lukacs John J Irwin Ellen L Berg Kathleen M Giacomini Bryan L Roth Brian K Shoichet Laszlo Urban

Science 2020 07;369(6502):403-413

Preclinical Safety, Novartis Institutes for Biomedical Research, Cambridge, MA 02139, USA.

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July 2020

Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.

Authors:
Folkert Reck Alun Bermingham Johanne Blais Vladimir Capka Taryn Cariaga Anthony Casarez Richard Colvin Charles R Dean Alex Fekete Wanben Gong Ellie Growcott Hongqiu Guo Adriana K Jones Cindy Li Fengxia Li Xiaodong Lin Mika Lindvall Sara Lopez David McKenney Louis Metzger Heinz E Moser Ramadevi Prathapam Dita Rasper Patrick Rudewicz Vijay Sethuraman Xiaoyu Shen Jacob Shaul Robert L Simmons Kyuto Tashiro Dazhi Tang Meiliana Tjandra Nancy Turner Tsuyoshi Uehara Charles Vitt Steven Whitebread Aregahegn Yifru Xu Zang Qingming Zhu

Bioorg Med Chem Lett 2018 02 4;28(4):748-755. Epub 2018 Jan 4.

Novartis Institutes for BioMedical Research, Emeryville, CA, USA.

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February 2018

Reverse translation of adverse event reports paves the way for de-risking preclinical off-targets.

Authors:
Mateusz Maciejewski Eugen Lounkine Steven Whitebread Pierre Farmer William DuMouchel Brian K Shoichet Laszlo Urban

Elife 2017 08 8;6. Epub 2017 Aug 8.

Novartis Institutes for Biomedical Research, Cambridge, United States.

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August 2017

Secondary pharmacology: screening and interpretation of off-target activities - focus on translation.

Authors:
Steven Whitebread Berengere Dumotier Duncan Armstrong Alexander Fekete Shanni Chen Andreas Hartmann Patrick Y Muller Laszlo Urban

Drug Discov Today 2016 08 29;21(8):1232-42. Epub 2016 Apr 29.

Preclinical Safety, Novartis Institutes for Biomedical Research, Cambridge, MA 02139, USA. Electronic address:

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August 2016

Implications of Dynamic Occupancy, Binding Kinetics, and Channel Gating Kinetics for hERG Blocker Safety Assessment and Mitigation.

Authors:
Robert A Pearlstein K Andrew MacCannell Gül Erdemli Sarita Yeola Gabriel Helmlinger Qi-Ying Hu Ramy Farid William Egan Steven Whitebread Clayton Springer Jeremy Beck Hao-Ran Wang Mateusz Maciejewski Laszlo Urban José S Duca

Curr Top Med Chem 2016 ;16(16):1792-818

Novartis Institutes for Bio- Medical Research, Inc., 100 Technology Square, Cambridge, MA 02139, USA.

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February 2017

A screening pattern recognition method finds new and divergent targets for drugs and natural products.

Authors:
Anne Mai Wassermann Eugen Lounkine Laszlo Urban Steven Whitebread Shanni Chen Kevin Hughes Hongqiu Guo Elena Kutlina Alexander Fekete Martin Klumpp Meir Glick

ACS Chem Biol 2014 Jul 2;9(7):1622-31. Epub 2014 Jun 2.

Novartis Institutes for Biomedical Research Inc. , 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

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July 2014

Matched molecular pair analysis: significance and the impact of experimental uncertainty.

Authors:
Christian Kramer Julian E Fuchs Steven Whitebread Peter Gedeck Klaus R Liedl

J Med Chem 2014 May 16;57(9):3786-802. Epub 2014 Apr 16.

Department of Theoretical Chemistry, Faculty for Chemistry and Pharmacy, Center for Molecular Biosciences Innsbruck (CMBI), Leopold-Franzens University Innsbruck , Innrain 80/82, A-6020 Innsbruck, Austria.

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May 2014

Reducing safety-related drug attrition: the use of in vitro pharmacological profiling.

Authors:
Joanne Bowes Andrew J Brown Jacques Hamon Wolfgang Jarolimek Arun Sridhar Gareth Waldron Steven Whitebread

Nat Rev Drug Discov 2012 Dec;11(12):909-22

AstraZeneca R&D, Alderley Park, Cheshire SK10 4TG, UK.

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December 2012

Large-scale prediction and testing of drug activity on side-effect targets.

Authors:
Eugen Lounkine Michael J Keiser Steven Whitebread Dmitri Mikhailov Jacques Hamon Jeremy L Jenkins Paul Lavan Eckhard Weber Allison K Doak Serge Côté Brian K Shoichet Laszlo Urban

Nature 2012 Jun 10;486(7403):361-7. Epub 2012 Jun 10.

Novartis Institutes for Biomedical Research, Cambridge, Massachusetts 02139, USA.

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June 2012

Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.

Authors:
Michael D Shultz Xueying Cao Christine H Chen Young Shin Cho Nicole R Davis Joe Eckman Jianmei Fan Alex Fekete Brant Firestone Julie Flynn Jack Green Joseph D Growney Mats Holmqvist Meier Hsu Daniel Jansson Lei Jiang Paul Kwon Gang Liu Franco Lombardo Qiang Lu Dyuti Majumdar Christopher Meta Lawrence Perez Minying Pu Tim Ramsey Stacy Remiszewski Suzanne Skolnik Martin Traebert Laszlo Urban Vinita Uttamsingh Ping Wang Steven Whitebread Lewis Whitehead Yan Yan-Neale Yung-Mae Yao Liping Zhou Peter Atadja

J Med Chem 2011 Jul 17;54(13):4752-72. Epub 2011 Jun 17.

Novartis Institutes for Biomedical Research, Inc., Cambridge, Massachusetts 02139, United States.

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July 2011

In vitro safety pharmacology profiling: what else beyond hERG?

Authors:
Jacques Hamon Steven Whitebread Valerie Techer-Etienne Helene Le Coq Kamal Azzaoui Laszlo Urban

Future Med Chem 2009 Jul;1(4):645-65

Center for Proteomic Chemistry, Novartis Pharma AG, Forum 1, 4002 Basel, Switzerland.

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July 2009

Gaining insight into off-target mediated effects of drug candidates with a comprehensive systems chemical biology analysis.

Authors:
Josef Scheiber Bin Chen Mariusz Milik Sai Chetan K Sukuru Andreas Bender Dmitri Mikhailov Steven Whitebread Jacques Hamon Kamal Azzaoui Laszlo Urban Meir Glick John W Davies Jeremy L Jenkins

J Chem Inf Model 2009 Feb;49(2):308-17

Lead Discovery Informatics and Preclinical Safety Profiling, CPC, Novartis Institutes for Biomedical Research, 250 Massachussetts Avenue, Cambridge, Massachusetts 02139, USA.

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February 2009

Mapping adverse drug reactions in chemical space.

Authors:
Josef Scheiber Jeremy L Jenkins Sai Chetan K Sukuru Andreas Bender Dmitri Mikhailov Mariusz Milik Kamal Azzaoui Steven Whitebread Jacques Hamon Laszlo Urban Meir Glick John W Davies

J Med Chem 2009 May;52(9):3103-7

Lead Discovery Informatics, CPC, Novartis Institutes for Biomedical Research, 250 Massachussetts Avenue, Cambridge, Massachusetts 02139, USA.

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May 2009

2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.

Authors:
David A Sandham Clive Aldcroft Urs Baettig Lucy Barker David Beer Gurdip Bhalay Zarin Brown Gerald Dubois David Budd Louise Bidlake Emma Campbell Brian Cox Brian Everatt David Harrison Catherine J Leblanc Jodie Manini Rachael Profit Rowan Stringer Katy S Thompson Katharine L Turner Morris F Tweed Christoph Walker Simon J Watson Steven Whitebread Jennifer Willis Gareth Williams Caroline Wilson

Bioorg Med Chem Lett 2007 Aug 13;17(15):4347-50. Epub 2007 May 13.

Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.

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August 2007

Modeling promiscuity based on in vitro safety pharmacology profiling data.

Authors:
Kamal Azzaoui Jacques Hamon Bernard Faller Steven Whitebread Edgar Jacoby Andreas Bender Jeremy L Jenkins Laszlo Urban

ChemMedChem 2007 Jun;2(6):874-80

CPC/LFP/MLI, Novartis Institutes for Biomedical Research, Novartis Pharma AG, Postfach, 4002 Basel, Switzerland.

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June 2007

Analysis of pharmacology data and the prediction of adverse drug reactions and off-target effects from chemical structure.

Authors:
Andreas Bender Josef Scheiber Meir Glick John W Davies Kamal Azzaoui Jacques Hamon Laszlo Urban Steven Whitebread Jeremy L Jenkins

ChemMedChem 2007 Jun;2(6):861-73

Lead Finding Platform, Novartis Institutes for BioMedical Research Inc. 250 Massachusetts Ave., Cambridge, Massachusetts 02139, USA.

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June 2007

High-throughput in vitro profiling assays: lessons learnt from experiences at Novartis.

Authors:
Bernard Faller Jianling Wang Alfred Zimmerlin Leslie Bell Jacques Hamon Steven Whitebread Kamal Azzaoui Dejan Bojanic Laszlo Urban

Expert Opin Drug Metab Toxicol 2006 Dec;2(6):823-33

Novartis Institutes for BioMedical Research, Basel, Switzerland.

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December 2006

ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.

Authors:
Samuel Hintermann Ivo Vranesic Hans Allgeier Armin Brülisauer Daniel Hoyer Michel Lemaire Thomas Moenius Stephan Urwyler Steven Whitebread Fabrizio Gasparini Yves P Auberson

Bioorg Med Chem 2007 Jan 21;15(2):903-14. Epub 2006 Oct 21.

Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland.

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January 2007

Keynote review: in vitro safety pharmacology profiling: an essential tool for successful drug development.

Authors:
Steven Whitebread Jacques Hamon Dejan Bojanic Laszlo Urban

Drug Discov Today 2005 Nov;10(21):1421-33

PreClinical Profiling, Lead Discovery Center, Novartis Institutes for BioMedical Research, Cambridge, MA 02139, USA.

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November 2005

Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.

Authors:
Heinrich Rueeger Marc Gerspacher Peter Buehlmayer Pascal Rigollier Yasuchika Yamaguchi Tibur Schmidlin Steven Whitebread Barbara Nuesslein-Hildesheim Hanspeter Nick Leoluca Cricione

Bioorg Med Chem Lett 2004 May;14(10):2451-7

Novartis Pharma AG, Novartis Institutes for BioMedical Research Basel, CH-4002 Basel, Switzerland.

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May 2004