Literature DB >> 15892684

Components of successful lead generation.

Andrew M Davis1, David J Keeling, John Steele, Nicholas P Tomkinson, Alan C Tinker.   

Abstract

This review aims to give an overview of current good practice in the prosecution of Lead Generation. It will assess experiences across the field as judged from the contents of the limited number of peer-review disclosures to date. It will also rely heavily on the experiences of the authors from many campaigns within this organisation. Its focus will be on the assembly of an appropriate compound collection for application in High Throughput Screening (HTS), the prosecution of HTS, the profiling of HTS output and, lastly the Hit-to-Lead optimisation of selected HTS output. Excluded from the scope are detailed aspects of library design [1], parallel synthesis [2], virtual library applications [3], virtual screening [4] and fragment screening [5] approaches, all of which have been the subject of recent reviews.

Mesh:

Year:  2005        PMID: 15892684     DOI: 10.2174/1568026053828411

Source DB:  PubMed          Journal:  Curr Top Med Chem        ISSN: 1568-0266            Impact factor:   3.295


  9 in total

Review 1.  The influence of the 'organizational factor' on compound quality in drug discovery.

Authors:  Paul D Leeson; Stephen A St-Gallay
Journal:  Nat Rev Drug Discov       Date:  2011-09-30       Impact factor: 84.694

Review 2.  The influence of lead discovery strategies on the properties of drug candidates.

Authors:  György M Keserü; Gergely M Makara
Journal:  Nat Rev Drug Discov       Date:  2009-03       Impact factor: 84.694

Review 3.  Chemical predictive modelling to improve compound quality.

Authors:  John G Cumming; Andrew M Davis; Sorel Muresan; Markus Haeberlein; Hongming Chen
Journal:  Nat Rev Drug Discov       Date:  2013-12       Impact factor: 84.694

Review 4.  Application of NMR and molecular docking in structure-based drug discovery.

Authors:  Jaime L Stark; Robert Powers
Journal:  Top Curr Chem       Date:  2012

5.  Thousands of chemical starting points for antimalarial lead identification.

Authors:  Francisco-Javier Gamo; Laura M Sanz; Jaume Vidal; Cristina de Cozar; Emilio Alvarez; Jose-Luis Lavandera; Dana E Vanderwall; Darren V S Green; Vinod Kumar; Samiul Hasan; James R Brown; Catherine E Peishoff; Lon R Cardon; Jose F Garcia-Bustos
Journal:  Nature       Date:  2010-05-20       Impact factor: 49.962

Review 6.  Probing the links between in vitro potency, ADMET and physicochemical parameters.

Authors:  M Paul Gleeson; Anne Hersey; Dino Montanari; John Overington
Journal:  Nat Rev Drug Discov       Date:  2011-03       Impact factor: 84.694

Review 7.  Probing the probes: fitness factors for small molecule tools.

Authors:  Paul Workman; Ian Collins
Journal:  Chem Biol       Date:  2010-06-25

Review 8.  Connecting synthetic chemistry decisions to cell and genome biology using small-molecule phenotypic profiling.

Authors:  Bridget K Wagner; Paul A Clemons
Journal:  Curr Opin Chem Biol       Date:  2009-10-12       Impact factor: 8.822

9.  Activation of inhibitors by sortase triggers irreversible modification of the active site.

Authors:  Anthony W Maresso; Ruiying Wu; Justin W Kern; Rongguang Zhang; Dorota Janik; Dominique M Missiakas; Mark-Eugene Duban; Andrzej Joachimiak; Olaf Schneewind
Journal:  J Biol Chem       Date:  2007-06-01       Impact factor: 5.157

  9 in total

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