Concepedia

Fragment-based Lead Optimization

Fragment-Based Lead Optimization is a ligand efficiency optimization strategy that involves the systematic expansion or elaboration of low-molecular-weight fragment hits into high-affinity lead compounds through structure-guided design and iterative chemical modification.

97

Publications

5.3K

Citations

838

Authors

160

Institutions

Publications per year

2017–2026

32

Parents

Publications

97

Ligand efficiency indices for effective drug discovery

Cele Abad‐Zapatero · Expert Opinion on Drug Discovery · 2007 · 273 citations

, , +17

Ligand efficiency as a guide in fragment hit selection and optimization

Sabine Schultes, Chris de Graaf, Eric Haaksma et al. · Drug Discovery Today Technologies · 2010 · 249 citations · Full text

, , +15

Application of Fragment-Based Lead Generation to the Discovery of Novel, Cyclic Amidine β-Secretase Inhibitors with Nanomolar Potency, Cellular Activity, and High Ligand Efficiency

Philip D. Edwards, Jeffrey S. Albert, Mark Sylvester et al. · Journal of Medicinal Chemistry · 2007 · 211 citations · Full text

, , +17

Topomer CoMFA:  A Design Methodology for Rapid Lead Optimization

Richard D. Cramer · Journal of Medicinal Chemistry · 2003 · 198 citations

, , +17

Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface

Inge Van Molle, Andreas Thomann, Dennis L. Buckley et al. · Chemistry & Biology · 2012 · 193 citations

, , +17

1–5 of 97

Authors

838

  1. RE
    Roderick E. Hubbard

    University of York, United Kingdom

    5 publications · 282 citations

    5

    h-index

  2. IJ
    Iwan J. P. de Esch

    Vrije Universiteit Amsterdam, Netherlands

    5 publications · 500 citations

    5

    h-index

  3. MC
    Miles Congreve

    Heptares Therapeutics (United Kingdom), United Kingdom

    4 publications · 728 citations

    4

    h-index

  4. MF
    Martyn Frederickson

    University of Leeds, United Kingdom

    4 publications · 728 citations

    4

    h-index

  5. CW
    Christopher W. Murray

    Proteus (United Kingdom), United Kingdom

    4 publications · 728 citations

    4

    h-index

1–5 of 838

Institutions

160

  1. Novartis (Switzerland)

    Basel, Switzerland

    6 h-index

    26 publications

    1.3K citations

  2. Novartis Institutes for BioMedical Research

    Basel, Switzerland

    5 h-index

    21 publications

    650 citations

  3. Vrije Universiteit Amsterdam

    Amsterdam, The Netherlands

    5 h-index

    18 publications

    1.8K citations

  4. AstraZeneca (United Kingdom)

    Cambridge, United Kingdom

    5 h-index

    73 publications

    10.7K citations

  5. University of York

    York, United Kingdom

    5 h-index

    6 publications

    306 citations

  6. Granta Design (United Kingdom)

    Cambridge, United Kingdom

    5 h-index

    11 publications

    504 citations

  7. University of Cambridge

    Cambridge, United Kingdom

    4 h-index

    29 publications

    2.3K citations

  8. Inserm

    Paris, France

    4 h-index

    9 publications

    295 citations

1–8 of 160

Venues

  1. Journal of Medicinal Chemistry

    27 publications · 2.3K citations

    25

    h-index

  2. Bioorganic & Medicinal Chemistry Letters

    5 publications · 88 citations

    5

    h-index

  3. Bioorganic & Medicinal Chemistry

    5 publications · 147 citations

    5

    h-index

  4. Journal of Computer-Aided Molecular Design

    5 publications · 148 citations

    5

    h-index

  5. ChemMedChem

    4 publications · 109 citations

    4

    h-index

1–5