Drug like Properties Concepts Structure Design and Methods

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. * Serves as an essential working handbook aimed at scientists and students in medicinal chemistry * Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies * Discusses improvements in pharmacokinetics from a practical chemist's standpoint

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  • Author : Li Di
  • Publisher : Elsevier
  • Pages : 552 pages
  • ISBN : 0080557619
  • Rating : 4/5 from 21 reviews
CLICK HERE TO GET THIS BOOKDrug like Properties Concepts Structure Design and Methods

Drug-like Properties: Concepts, Structure Design and Methods

Drug-like Properties: Concepts, Structure Design and Methods
  • Author : Li Di,Edward H Kerns
  • Publisher : Elsevier
  • Release : 26 July 2010
GET THIS BOOKDrug-like Properties: Concepts, Structure Design and Methods

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be

Drug-like Properties

Drug-like Properties
  • Author : Edward Harvel Kerns,Li Di
  • Publisher : Unknown Publisher
  • Release : 21 May 2022
GET THIS BOOKDrug-like Properties

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be

Optimizing the "Drug-Like" Properties of Leads in Drug Discovery

Optimizing the
  • Author : Ronald Borchardt,Edward Kerns,Michael Hageman,Dhrien Thakker,James Stevens
  • Publisher : Springer Science & Business Media
  • Release : 31 December 2007
GET THIS BOOKOptimizing the "Drug-Like" Properties of Leads in Drug Discovery

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.

Discovering and Developing Molecules with Optimal Drug-Like Properties

Discovering and Developing Molecules with Optimal Drug-Like Properties
  • Author : Allen C Templeton,Stephen R. Byrn,Roy J Haskell,Thomas E. Prisinzano
  • Publisher : Springer
  • Release : 31 October 2014
GET THIS BOOKDiscovering and Developing Molecules with Optimal Drug-Like Properties

This authoritative volume provides a contemporary view on the latest research in molecules with optimal drug-like properties. It is a valuable source to access current best practices as well as new research techniques and strategies. Written by leading scientists in their fields, the text consists of fourteen chapters with an underlying theme of early collaborative opportunities between pharmaceutical and discovery sciences. The book explores the practical realities of performing physical pharmaceutical and biopharmaceutical research in the context of drug discovery

Drug-Like Properties

Drug-Like Properties
  • Author : Li Di,Edward H Kerns
  • Publisher : Academic Press
  • Release : 17 December 2015
GET THIS BOOKDrug-Like Properties

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This

Drug Design Strategies

Drug Design Strategies
  • Author : David J. Livingstone,Andrew M. Davis
  • Publisher : Royal Society of Chemistry
  • Release : 01 November 2011
GET THIS BOOKDrug Design Strategies

Shows how different parts of the drug discovery process have developed, with particular emphasis on quantitative aspects and possible future progress.

Structure-based Design of Drugs and Other Bioactive Molecules

Structure-based Design of Drugs and Other Bioactive Molecules
  • Author : Arun K. Ghosh,Sandra Gemma
  • Publisher : John Wiley & Sons
  • Release : 11 August 2014
GET THIS BOOKStructure-based Design of Drugs and Other Bioactive Molecules

Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use

Metabolism, Pharmacokinetics and Toxicity of Functional Groups

Metabolism, Pharmacokinetics and Toxicity of Functional Groups
  • Author : Dennis A Smith
  • Publisher : Royal Society of Chemistry
  • Release : 09 April 2010
GET THIS BOOKMetabolism, Pharmacokinetics and Toxicity of Functional Groups

Until now, the area of drug metabolism and pharmacokinetics has been lacking in texts written for the Medicinal Chemist. This outstanding book, aimed at postgraduate medicinal chemists and those working in industry, fills this gap in the literature. Written by medicinal chemists and ADMET scientists with a combined experience of around 300 years, this aid to discovering drugs addresses the absorption, distribution, metabolism, excretion and toxicity (ADMET) issues associated with drugs. The book starts by describing drug targets and their structural

Textbook of Drug Design and Discovery, Third Edition

Textbook of Drug Design and Discovery, Third Edition
  • Author : Tommy Liljefors,Povl Krogsgaard-Larsen,Ulf Madsen
  • Publisher : CRC Press
  • Release : 25 July 2002
GET THIS BOOKTextbook of Drug Design and Discovery, Third Edition

Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for

ADMET for Medicinal Chemists

ADMET for Medicinal Chemists
  • Author : Katya Tsaioun,Steven A. Kates
  • Publisher : John Wiley & Sons
  • Release : 15 February 2011
GET THIS BOOKADMET for Medicinal Chemists

This book guides medicinal chemists in how to implement early ADMET testing in their workflow in order to improve both the speed and efficiency of their efforts. Although many pharmaceutical companies have dedicated groups directly interfacing with drug discovery, the scientific principles and strategies are practiced in a variety of different ways. This book answers the need to regularize the drug discovery interface; it defines and reviews the field of ADME for medicinal chemists. In addition, the scientific principles and

The Practice of Medicinal Chemistry

The Practice of Medicinal Chemistry
  • Author : Camille Georges Wermuth,David Aldous,Pierre Raboisson,Didier Rognan
  • Publisher : Elsevier
  • Release : 01 July 2015
GET THIS BOOKThe Practice of Medicinal Chemistry

The Practice of Medicinal Chemistry, Fourth Edition provides a practical and comprehensive overview of the daily issues facing pharmaceutical researchers and chemists. In addition to its thorough treatment of basic medicinal chemistry principles, this updated edition has been revised to provide new and expanded coverage of the latest technologies and approaches in drug discovery. With topics like high content screening, scoring, docking, binding free energy calculations, polypharmacology, QSAR, chemical collections and databases, and much more, this book is the go-to

Advances in Nucleic Acid Therapeutics

Advances in Nucleic Acid Therapeutics
  • Author : Sudhir Agrawal,Michael J Gait
  • Publisher : Royal Society of Chemistry
  • Release : 08 February 2019
GET THIS BOOKAdvances in Nucleic Acid Therapeutics

The sequencing of the human genome and subsequent elucidation of the molecular pathways that are important in the pathology of disease have provided unprecedented opportunities for the development of new therapeutics. Nucleic acid-based drugs have emerged in recent years to yield extremely promising candidates for drug therapy to a wide range of diseases. Advances in Nucleic Acid Therapeutics is a comprehensive review of the latest advances in the field, covering the background of the development of nucleic acids for therapeutic

Drug Metabolism and Pharmacokinetics Quick Guide

Drug Metabolism and Pharmacokinetics Quick Guide
  • Author : Siamak Cyrus Khojasteh,Harvey Wong,Cornelis E.C.A. Hop
  • Publisher : Springer Science & Business Media
  • Release : 07 April 2011
GET THIS BOOKDrug Metabolism and Pharmacokinetics Quick Guide

Drug Metabolism and Pharmacokinetics Quick Guide covers a number of aspects of drug assessment at drug discovery and development stages, topics such as pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations. It covers key concepts, with useful tables on physiological parameters (eg. blood flow to organs in x-species, expression and localization of enzymes and transporters), chemical structure, nomenclature, and moieties leading to bioactivation (with examples). Overall it includes a number of key

Modern Approaches in Drug Discovery

Modern Approaches in Drug Discovery
  • Author : Anonim
  • Publisher : Academic Press
  • Release : 31 October 2018
GET THIS BOOKModern Approaches in Drug Discovery

Modern Approaches in Drug Discovery, Volume 611, the latest release in the Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting chapters on topics such as Target Identification and Validation, Cell Painting/High Content Imaging, Target ID using chemical probes, Mining the microbiome for targets, Data driven approaches for diversity and drug-likeness, Affinity-based screening, Fragment screening (X-ray), Array-based approaches, Hit-to-lead: assessment and improvement of drug-like properties, Hit assessment and prioritization, Lead Optimization: fine tuning

Drug Discovery

Drug Discovery
  • Author : Jie Jack Li,E. J. Corey
  • Publisher : John Wiley & Sons
  • Release : 03 April 2013
GET THIS BOOKDrug Discovery

Sets forth the history, state of the science, and future directions of drug discovery Edited by Jie Jack Li and Nobel laureate E. J. Corey, two leading pioneers in drug discovery and medicinal chemistry, this book synthesizes great moments in history, the current state of the science, and future directions of drug discovery into one expertly written and organized work. Exploring all major therapeutic areas, the book introduces readers to all facets and phases of drug discovery, including target selection,