Concepedia

Target Engagement Optimization

Target Engagement Optimization is a methodological framework within potency optimization that systematically enhances the interaction specificity and binding affinity of a therapeutic agent toward its intended biological target while minimizing off-target effects.

52

Publications

2.3K

Citations

857

Authors

157

Institutions

Publications per year

2017–2026

44

Parents

Publications

52

Determining target engagement in living systems

Gabriel M. Simon, Micah J. Niphakis, Benjamin F. Cravatt · Nature Chemical Biology · 2013 · 250 citations · Full text

, , +3

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Ganesha Rai, Kyle R. Brimacombe, Bryan T. Mott et al. · Journal of Medicinal Chemistry · 2017 · 154 citations · Full text

, , +17

1,4,9-Triazaspiro[5.5]undecan-2-one Derivatives as Potent and Selective METTL3 Inhibitors

A. Dolbois, R.K. Bedi, Elena Bochenkova et al. · Journal of Medicinal Chemistry · 2021 · 146 citations · Full text

, , +14

Transcranial optical imaging reveals a pathway for optimizing the delivery of immunotherapeutics to the brain

Benjamin A. Plog, Humberto Mestre, Genaro E. Olveda et al. · JCI Insight · 2018 · 105 citations · Full text

, , +17

Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies

Bernard Barlaam, Robert Casella, Justin Cidado et al. · Journal of Medicinal Chemistry · 2020 · 104 citations · Full text

, , +15

1–5 of 52

Authors

857

  1. BF
    Benjamin F. Cravatt

    Scripps Research Institute, United States

    3 publications · 338 citations

    3

    h-index

  2. HL
    Hank La

    Charles River Laboratories (United Kingdom), United Kingdom

    2 publications · 56 citations

    2

    h-index

  3. JW
    Jon Winter-Holt

    AstraZeneca (United Kingdom), United Kingdom

    2 publications · 66 citations

    2

    h-index

  4. LW
    Liangwei Wu

    AstraZeneca (United Kingdom), United Kingdom

    2 publications · 129 citations

    2

    h-index

  5. TK
    Thomas Kornecook

    Amgen (United States), United States

    2 publications · 90 citations

    2

    h-index

1–5 of 857

Institutions

157

  1. AstraZeneca (United Kingdom)

    Cambridge, United Kingdom

    5 h-index

    82 publications

    3.4K citations

  2. AstraZeneca (United States)

    Wilmington, United States

    4 h-index

    42 publications

    2.9K citations

  3. University of Pennsylvania

    Philadelphia, United States

    4 h-index

    6 publications

    298 citations

  4. Scripps Research Institute

    San Diego, United States

    3 h-index

    11 publications

    854 citations

  5. Amgen (United States)

    Thousand Oaks, United States

    2 h-index

    74 publications

    3.7K citations

  6. GlaxoSmithKline (United Kingdom)

    London, United Kingdom

    2 h-index

    23 publications

    1.4K citations

  7. National Center for Advancing Translational Sciences

    Rockville, United States

    2 h-index

    37 publications

    3.8K citations

  8. Pfizer (United States)

    New York, United States

    2 h-index

    9 publications

    496 citations

1–8 of 157

Venues

  1. Journal of Medicinal Chemistry

    23 publications · 1.2K citations

    19

    h-index

  2. ChemBioChem

    2 publications · 48 citations

    2

    h-index

  3. International Journal of Eating Disorders

    2 publications · 32 citations

    2

    h-index

  4. Bioorganic & Medicinal Chemistry Letters

    2 publications · 51 citations

    2

    h-index

  5. Molecular Cancer Therapeutics

    MCT · 2 publications · 37 citations

    2

    h-index

1–5