Fragment-to-Lead Medicinal Chemistry Publications in 2024: A Tenth Annual Perspective

David G. Twigg; Kenta Arai; Michelle R. Arkin; Daniel A. Erlanson; Iwan J.P. de Esch; Barbara Farkaš; Stephen W. Fesik; Wolfgang Jahnke; Christopher N. Johnson; Martin Schroeder

doi:10.1021/acs.jmedchem.5c02894

Fragment-to-Lead Medicinal Chemistry Publications in 2024: A Tenth Annual Perspective

David G. Twigg
, Kenta Arai
, Michelle R. Arkin
, Daniel A. Erlanson
, Iwan J.P. de Esch
, Barbara Farkaš
, Stephen W. Fesik
, Wolfgang Jahnke
, Christopher N. Johnson
, Martin Schroeder

Research output: Contribution to Journal › Review article › Academic › peer-review

Abstract

Fragment-based drug discovery (FBDD) has led to dozens of clinical compounds, including eight approved drugs. For the past decade, we have published an annual review of successful fragment-to-lead (F2L) medicinal chemistry programs. This Perspective marks the tenth in the series. We analyze the 18 F2L case studies from 2024 and put them in the context of the larger set of 233 examples dating back to 2015. We hope that the lessons herein will both inform and inspire researchers to discover the next generation of drugs.

Original language	English
Pages (from-to)	24830-24847
Number of pages	18
Journal	Journal of medicinal chemistry
Volume	68
Issue number	23
Early online date	25 Nov 2025
DOIs	https://doi.org/10.1021/acs.jmedchem.5c02894
Publication status	Published - 11 Dec 2025

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title = "Fragment-to-Lead Medicinal Chemistry Publications in 2024: A Tenth Annual Perspective",

abstract = "Fragment-based drug discovery (FBDD) has led to dozens of clinical compounds, including eight approved drugs. For the past decade, we have published an annual review of successful fragment-to-lead (F2L) medicinal chemistry programs. This Perspective marks the tenth in the series. We analyze the 18 F2L case studies from 2024 and put them in the context of the larger set of 233 examples dating back to 2015. We hope that the lessons herein will both inform and inspire researchers to discover the next generation of drugs.",

author = "Twigg, \{David G.\} and Kenta Arai and Arkin, \{Michelle R.\} and Erlanson, \{Daniel A.\} and \{de Esch\}, \{Iwan J.P.\} and Barbara Farka{\v s} and Fesik, \{Stephen W.\} and Wolfgang Jahnke and Johnson, \{Christopher N.\} and Martin Schroeder",

year = "2025",

month = dec,

day = "11",

doi = "10.1021/acs.jmedchem.5c02894",

language = "English",

volume = "68",

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TY - JOUR

T1 - Fragment-to-Lead Medicinal Chemistry Publications in 2024

T2 - A Tenth Annual Perspective

AU - Twigg, David G.

AU - Arai, Kenta

AU - Arkin, Michelle R.

AU - Erlanson, Daniel A.

AU - de Esch, Iwan J.P.

AU - Farkaš, Barbara

AU - Fesik, Stephen W.

AU - Jahnke, Wolfgang

AU - Johnson, Christopher N.

AU - Schroeder, Martin

PY - 2025/12/11

Y1 - 2025/12/11

N2 - Fragment-based drug discovery (FBDD) has led to dozens of clinical compounds, including eight approved drugs. For the past decade, we have published an annual review of successful fragment-to-lead (F2L) medicinal chemistry programs. This Perspective marks the tenth in the series. We analyze the 18 F2L case studies from 2024 and put them in the context of the larger set of 233 examples dating back to 2015. We hope that the lessons herein will both inform and inspire researchers to discover the next generation of drugs.

AB - Fragment-based drug discovery (FBDD) has led to dozens of clinical compounds, including eight approved drugs. For the past decade, we have published an annual review of successful fragment-to-lead (F2L) medicinal chemistry programs. This Perspective marks the tenth in the series. We analyze the 18 F2L case studies from 2024 and put them in the context of the larger set of 233 examples dating back to 2015. We hope that the lessons herein will both inform and inspire researchers to discover the next generation of drugs.

UR - https://www.scopus.com/pages/publications/105024726488

UR - https://www.scopus.com/pages/publications/105024726488#tab=citedBy

U2 - 10.1021/acs.jmedchem.5c02894

DO - 10.1021/acs.jmedchem.5c02894

M3 - Review article

C2 - 41290421

AN - SCOPUS:105024726488

SN - 0022-2623

VL - 68

SP - 24830

EP - 24847

JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 23

ER -

Fragment-to-Lead Medicinal Chemistry Publications in 2024: A Tenth Annual Perspective

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