Lead-Seeking Approaches
Christopher A. Lipinski: Overview of Hit to Lead: The Medicinal Chemist’s Role from HTS Retest to Lead Optimization Hand Off Jeff W. Paslay • John E. Morin • Richard K. Harrison: High Throughput Screening in the Twenty - First Century Jack Andrew Bik
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Volume Editor Matthew M. Hayward
Lead-Seeking Approaches
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5 Topics in Medicinal Chemistry
Editorial Board: P. R. Bernstein · A. Buschauer · G. J. Georg · J. A. Lowe · H. U. Stilz
Lead-Seeking Approaches Volume Editor: Matthew M. Hayward
With contributions by J. A. Bikker J. W. Ellingboe K. D. Freeman-Cook A. M. Gilbert R. K. Harrison D. W. Kung C. A. Lipinski J. E. Morin L. S. Narasimhan J. W. Paslay M. Pellecchia
Editor Dr. Matthew M. Hayward Pfizer Global Research & Development Dept. Neuroscience Chemistry Eastern Point Rd. Groton CT 06340 MS 8220/4339 USA [email protected]
ISSN 1862-2461 e-ISSN 1862-247X ISBN 978-3-642-01074-3 e-ISBN 978-3-642-01075-0 DOI 10.1007/978-3-642-01075-0 Springer Heidelberg Dordrecht London New York Library of Congress Control Number: 2009935068 # Springer-Verlag Berlin Heidelberg 2010 This work is subject to copyright. All rights are reserved, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfilm or in any other way, and storage in data banks. Duplication of this publication or parts thereof is permitted only under the provisions of the German Copyright Law of September 9, 1965, in its current version, and permission for use must always be obtained from Springer. Violations are liable to prosecution under the German Copyright Law. The use of general descriptive names, registered names, trademarks, etc. in this publication does not imply, even in the absence of a specific statement, that such names are exempt from the relevant protective laws and regulations and therefore free for general use. Cover design: Ku¨nkelLopka GmbH, Heidelberg, Germany Typesetting and Production: SPi Publisher Services Printed on acid-free paper Springer is part of Springer ScienceþBusiness Media (www.springer.com)
Volume Editors Dr. Matthew M. Hayward Pfizer Global Research & Development Dept. Neuroscience Chemistry Eastern Point Rd. Groton CT 06340 MS 8220/4339 USA [email protected]
Editorial Board Dr. Peter R. Bernstein
John A. Lowe
AstraZeneca Pharmaceuticals 1800 Concord Pike Fairfax Research Center B313 PO Box 15437 Wilmington, DE 19850-5437 USA
[email protected]
Prof. Dr. Armin Buschauer
Dr. Hans Ulrich Stilz Aventis Pharma Deutschland GmbH Geb. G 838 65926 Frankfurt a.M. Germany
Institute of Pharmacy University of Regensburg Universita¨tsstr. 31 93053 Regensburg Germany
Prof. Dr. Gunda J. Georg University of Minnesota Department of Medical Chemistry 8-101A Weaver Densford Hall Minneapolis, MN 55455 USA
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