Skip to main content
SpringerLink
Log in
Book cover
  • Book
  • © 2010

Lead-Seeking Approaches

Editors:

  1. Matthew M. Hayward

    1. Dept. Neuroscience Chemistry, Pfizer Global Research & Development, Groton CT, USA

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  2. J. A. Bikker
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  3. J. W. Ellingboe
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  4. K. D. Freeman-Cook
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  5. A. M. Gilbert
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  6. R. K. Harrison
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  7. D. W. Kung
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  8. C. A. Lipinski
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  9. J. E. Morin
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  10. L. S. Narasimhan
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  11. J. W. Paslay
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  12. M. Pellecchia
    View editor publications

    You can also search for this editor in PubMed   Google Scholar

Part of the book series: Topics in Medicinal Chemistry (TMC, volume 5)

Sections

Buy it now

eBook USD 129.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book USD 169.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book USD 169.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Other ways to access

This is a preview of subscription content, log in via an institution to check for access.

Table of contents (6 chapters)

  1. Front Matter

    Pages i-xiii
    PDF

  3. High Throughput Screening in the Twenty-First Century

    • Jeff W. Paslay, John E. Morin, Richard K. Harrison
    Pages 25-83

  4. Lead Discovery Using Virtual Screening

    • Jack Andrew Bikker, Lakshmi S. Narasimhan
    Pages 85-124

  5. NMR Spectroscopy in Fragment Based Drug Design

    • Maurizio Pellecchia
    Pages 125-139

  7. Lead Identification

    • John W. Ellingboe, Adam M. Gilbert
    Pages 175-212

  8. Back Matter

    Pages 213-217
    PDF
Back to top

About this book

High quality leads provide the foundation for the discovery of successful clinical development candidates, and therefore the identi?cation of leads is an essential part of drug discovery. The process for the identi?cation of leads generally starts with the screening of a compound collection, either an HTS of a relatively large compound collection (hundreds of thousands to one million plus compounds) or a more focused screen of a smaller set of compounds that have been preselected for the target of interest. Virtual screening methods such as structure-based or pharmacophore-based searches can complement or replace one of the above approaches. Once hits are identi?ed from one or more of these screening methods, they need to be thoroughly characterized in order to con?rm activity and identify areas in need of optimization. Finally, once fully characterized hits are identi?ed, preliminary optimization through synthetic modi?cation is carried out to generate leads. Parallel optimization of all properties, including biological, physicochemical, and ADME is the most ef?cient approach to the identi?cation of leads. Hit characterization is described in the previous chapter. The focus of this chapter is on hit optimization and the identi?- tion of leads. After a general overview of these processes, examples taken from the literature since 2001 will be used to illustrate speci?c points. There are also a number of excellent reviews covering the lead identi?cation process [1–6].
Back to top

Keywords

Back to top

Editors and Affiliations

  • Dept. Neuroscience Chemistry, Pfizer Global Research & Development, Groton CT, USA

    Matthew M. Hayward

Back to top

Bibliographic Information

  • Book Title: Lead-Seeking Approaches

  • Editors: Matthew M. Hayward, 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

  • Series Title: Topics in Medicinal Chemistry

  • DOI: https://doi.org/10.1007/978-3-642-01075-0

  • Publisher: Springer Berlin, Heidelberg

  • eBook Packages: Chemistry and Materials Science, Chemistry and Material Science (R0)

  • Copyright Information: Springer-Verlag Berlin Heidelberg 2010

  • Hardcover ISBN: 978-3-642-01074-3Published: 27 October 2009

  • Softcover ISBN: 978-3-642-26106-0Published: 14 March 2012

  • eBook ISBN: 978-3-642-01075-0Published: 12 March 2010

  • Series ISSN: 1862-2461

  • Series E-ISSN: 1862-247X

  • Edition Number: 1

  • Number of Pages: XIII, 217

  • Number of Illustrations: 26 b/w illustrations, 10 illustrations in colour

  • Topics: Medicinal Chemistry, Neurosciences, Organic Chemistry

Back to top

Publish with us

Policies and ethics

Back to top
Access via your institution

Buy it now

eBook USD 129.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book USD 169.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book USD 169.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Other ways to access

Search

Navigation