Table of Contents:
  • 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.