High Throughput Lead Optimization In Drug Discovery
DOWNLOAD
Download High Throughput Lead Optimization In Drug Discovery PDF/ePub or read online books in Mobi eBooks. Click Download or Read Online button to get High Throughput Lead Optimization In Drug Discovery book now. This website allows unlimited access to, at the time of writing, more than 1.5 million titles, including hundreds of thousands of titles in various foreign languages. If the content not found or just blank you must refresh this page
High Throughput Lead Optimization In Drug Discovery
DOWNLOAD
Author : Tushar Kshirsagar
language : en
Publisher: CRC Press
Release Date : 2008-03-04
High Throughput Lead Optimization In Drug Discovery written by Tushar Kshirsagar and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-03-04 with Medical categories.
A Single Source on Parallel Synthesis for Lead Optimization The end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high qualit
Lead Seeking Approaches
DOWNLOAD
Author : Matthew M. Hayward
language : en
Publisher: Springer Science & Business Media
Release Date : 2010-03-12
Lead Seeking Approaches written by Matthew M. Hayward and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-03-12 with Science categories.
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].
Industrialization Of Drug Discovery
DOWNLOAD
Author : Ph.D., Jeffrey S. Handen
language : en
Publisher: CRC Press
Release Date : 2005-05-26
Industrialization Of Drug Discovery written by Ph.D., Jeffrey S. Handen and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2005-05-26 with Medical categories.
The drug discovery and development process is getting longer, more expensive, and no better. The industry suffers from the same clinical attrition and safety-related market withdrawal rates today as it did 20 years ago. Industrialization of Drug Discovery: From Target Selection Through Lead Optimization scrutinizes these problems in detail, contras
High Throughput Screening In Drug Discovery
DOWNLOAD
Author : Jörg Hüser
language : en
Publisher: John Wiley & Sons
Release Date : 2006-12-13
High Throughput Screening In Drug Discovery written by Jörg Hüser and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2006-12-13 with Science categories.
Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharma and biotech industries working on small molecule screening.
Lead Generation
DOWNLOAD
Author : Jörg Holenz
language : en
Publisher: John Wiley & Sons
Release Date : 2016-03-16
Lead Generation written by Jörg Holenz and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-03-16 with Medical categories.
In this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This is the first book to combine both standard and innovative approaches in comparable breadth and depth, including several recent successful lead generation case studies published here for the first time. Beginning with a general discussion of the underlying principles and strategies, individual lead generation approaches are described in detail, highlighting their strengths and weaknesses, along with all relevant bordering disciplines like e.g. target identification and validation, predictive methods, molecular recognition or lead quality matrices. Novel lead generation approaches for challenging targets like DNA-encoded library screening or chemical biology approaches are treated here side by side with established methods as high throughput and affinity screening, knowledge- or fragment-based lead generation, and collaborative approaches. Within the entire book, a very strong focus is given to highlight the application of the presented methods, so that the reader will be able to learn from real life examples. The final part of the book presents several lead generation case studies taken from different therapeutic fields, including diabetes, cardiovascular and respiratory diseases, neuroscience, infection and tropical diseases. The result is a prime knowledge resource for medicinal chemists and for every scientist involved in lead generation.
Pharmaceutical Profiling In Drug Discovery For Lead Selection
DOWNLOAD
Author : Ronald Borchardt
language : en
Publisher: Springer Science & Business Media
Release Date : 2005-12-05
Pharmaceutical Profiling In Drug Discovery For Lead Selection written by Ronald Borchardt and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2005-12-05 with Medical categories.
This volume focuses on how to increase the efficiency of drug discovery and development. It is written by experienced discovery scientists from diverse disciplines, including chemistry, drug metabolism, and development sciences. The volume details in silico, in vitro, and in vivo tools for prediction, measurement, and application of compound properties to select and improve potential drug candidates.
Lead Generation Approaches In Drug Discovery
DOWNLOAD
Author : Zoran Rankovic
language : en
Publisher: John Wiley & Sons
Release Date : 2010-04-07
Lead Generation Approaches In Drug Discovery written by Zoran Rankovic and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-04-07 with Medical categories.
An integrated overview of modern approaches to lead discovery Lead generation is increasingly seen as a distinct and success-determining phase of the drug discovery process. Over recent years, there have been major advances in the understanding of what constitutes a good lead compound and how to improve the chances of finding such a compound. Written by leading scientists and established opinion leaders from industry and academia, this book provides an authoritative overview of the field, as well as the theory, practice, and scope, of the principal Lead Generation Approaches in Drug Discovery, including: The evolution of the lead discovery process, key concepts, current challenges, and future directions Strategies and technologies driving the high-throughput screening (HTS) approach to lead discovery, including the shifting paradigms in the design of compound collections and best practice in the hit confirmation process Knowledge-based in silico or "virtual" screening Theory and practice of the fragment-based approach to lead discovery The opportunities and challenges presented by multi-target drug discovery (MTDD) De novo design of lead compounds and new approaches to estimating the synthetic accessibility of de novo–designed molecules The impact of natural products on drug discovery, and potential of natural product–like compounds for exploring regions of biologically relevant chemical space Using early screening of hits and leads for metabolic, pharmacokinetic, and toxicological liabilities to reduce attrition during the later phases of drug discovery The utility of parallel synthesis and purification in lead discovery With each topic supported by numerous case studies, this is indispensable reading for researchers in industry and academia who wish to keep up to date with the latest strategies and approaches in drug discovery.
Chemoinformatics In Drug Discovery
DOWNLOAD
Author : Tudor I. Oprea
language : en
Publisher: John Wiley & Sons
Release Date : 2006-03-06
Chemoinformatics In Drug Discovery written by Tudor I. Oprea and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2006-03-06 with Science categories.
This handbook provides the first-ever inside view of today's integrated approach to rational drug design. Chemoinformatics experts from large pharmaceutical companies, as well as from chemoinformatics service providers and from academia demonstrate what can be achieved today by harnessing the power of computational methods for the drug discovery process. With the user rather than the developer of chemoinformatics software in mind, this book describes the successful application of computational tools to real-life problems and presents solution strategies to commonly encountered problems. It shows how almost every step of the drug discovery pipeline can be optimized and accelerated by using chemoinformatics tools -- from the management of compound databases to targeted combinatorial synthesis, virtual screening and efficient hit-to-lead transition. An invaluable resource for drug developers and medicinal chemists in academia and industry.
Optimization In Drug Discovery
DOWNLOAD
Author : Zhengyin Yan
language : en
Publisher: Humana Press
Release Date : 2004-08-11
Optimization In Drug Discovery written by Zhengyin Yan and has been published by Humana Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2004-08-11 with Medical categories.
Recent analyses of drug attrition rates reveal that a significant number of drug candidates fail in the later stage of clinical development owing to absorption, distribution, metabolism, elimination (ADME), and toxicity issues. Lead optimization in drug discovery, a process attempting to uncover and correct these defects of drug candidates, is highly beneficial in lowering the cost and time to develop therapeutic drugs by reducing drug candidate failures in development. At present, parallel synthesis combining with high-throughput screening has made it easier to generate highly potent compounds (i. e. , hits). However, to be a potential drug, a hit must have drug-like characteristics in addition to potency, which include optimal physicochemical properties, reasonable ph- macokinetic parameters, and good safety profiles. Therefore, research tools must be available in drug discovery to rapidly screen for compounds with favorable drug-like properties, and thus adequate resources can be directed to projects with high potential. Optimization in Drug Discovery: In Vitro Methods is a compilation of detailed experimental protocols necessary for setting up a variety of assays important in compound evaluation. A total of 25 chapters, contributed by many experts in their research areas, cover a wide spectrum of subjects including physicochemical properties, abso- tion, plasma binding, metabolism, drug interactions, and toxicity. A good pharmacokinetic profile has long been recognized as an imp- tant drug-like characteristic. Pharmacokinetic parameters are affected by many properties of drug molecules such as physicochemical nature, abso- tion, metabolic stability, and so on.
Optimizing The Drug Like Properties Of Leads In Drug Discovery
DOWNLOAD
Author : Ronald Borchardt
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-12-31
Optimizing The Drug Like Properties Of Leads In Drug Discovery written by Ronald Borchardt and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-12-31 with Medical categories.
This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.