Lead generation methods, strategies, and case studies - Holenz, Jörg 1968- (Wiley-VCH, 2016)
Introduction to Lead Generation. Introduction: Learnings from the Past : Characteristics of Successful Leads / Mike Hann -- Modern Lead Generation Strategies / Jörg Holenz, Dean G Brown -- The Importance of Target Identification for Generating Successful Leads. "Ligandability" of Drug Targets: Assessment of Chemical Tractability via Experimental and Approaches / Udo Bauer, Alexander L Breeze -- Chemistry-Driven Target Identification / Iván Cornella-Taracido, Ryan Hicks, Ola Engkvist, J Adam Hendricks, Ronald Tomlinson, M Paola Castaldi -- Hit Generation Methods. Lead Generation Based on Compound Collection Screening / Dirk Weigelt, Ismet Dorange -- Fragment-Based Lead Generation / Ivan V Efremov, Daniel A Erlanson -- Rational Hit Generation / Bernd Wellenzohn, Alexander Weber -- Competitive Intelligence-based Lead Generation and Fast Follower Approaches / Yu Jiang, Ziping Liu, Jörg Holenz, Hua Yang
Selective Optimization of Side Activities: An Alternative and Promising Strategy for Lead Generation / Norbert Handler, Andrea Wolkerstorfer, Helmut Buschmann -- Lead Generation for Challenging Targets / Jinqiao Wan, Dengfeng Dou, Hongmei Song, Xian-Hui Wu Xuemin Cheng, Jin Li -- Collaborative Approaches to Lead Generation / Fabrizio Giordanetto, Anna Karawajczyk, Graham Showell -- Converting Hits to Successful Leads. A Medicinal Chemistry Perspective on the Hit-to-Lead Phase in the Current Era of Drug Discovery / Dean G Brown -- Molecular Recognition and Its Importance for Fragment-Based Lead Generation and Hit-to-Lead / Thorsten Nowak -- Affinity-Based Screening Methodologies and Their Application in the Hit-to-Lead Phase / Stefan Geschwindner -- Predictive Methods in Lead Generation / Matthew D Segall, Peter Hunt -- Lead Quality / J Willem M Nissink, Sebastien Degorce, Ken Page
Hypothesis-driven Lead Optimization. The Strategies and Politics of Successful Design, Make, Test, and Analyze (DMTA) Cycles in Lead Generation / Steven S Wesolowski, Dean G Brown -- Recent Lead Generation Success Stories. Lead Generation Paved the Way for the Discovery of a Novel H Inverse Agonist Clinical Candidate / Christophe Genicot, Laurent Provins -- Vorapaxar: From Lead Identification to FDA Approval / Samuel Chackalamannil, Mariappan Chelliah -- Lead Generation Approaches Delivering Inhaled [beta]-Adrenoreceptor Agonist Drug Candidates / Michael Stocks, Lilian Alcaraz -- GPR81 HTS Case Study / Eric Wellner, Ola Fjellström -- Development of Influenza Virus Sialidase Inhibitors / Mauro Pascolutti, Robin J Thomson, Mark von Itzstein
The Discovery of Cathepsin A Inhibitors: A Project-Adapted Fragment Approach Based on HTS Results / Sven Ruf, Christian Buning, Herman Schreuder, Wolfgang Linz, Dominik Linz, Hartmut Rütten, Georg Horstick, Markus Kohlmann, Katja Kroll, Klaus Wirth, Thorsten Sadowski -- Lead Structure Discovery for Neglected Diseases: Product Development Partnerships Driving Drug Discovery / Jeremy N Burrows, Takushi Kaneko -- A Fragmentation Enumeration Approach to Generating Novel Drug Leads / Pravin S Iyer, Manoranjan Panda. - Includes bibliographical references and index