Integration of palladium-catalyzed C–N coupling into self-encoded libraries for accelerated hit discovery

Edith van der Nol, Zhenshuo Luo, Qing Qing Gao, Nils Alexander Haupt, Sebastian Böcker and Sebastian Pomplun

RSC Chem. Biol., 2026, 7, 630
DOI: 10.1039/D5CB00303B

Expanding the reaction toolbox for nanoscale direct-to-biology PROTAC synthesis and biological evaluation

Rebecca Stevens, Harry J. Shrives, Jenni Cryan, Diana Klimaszewska, Peter Stacey, Glenn A. Burley, John D. Harling, David J. Battersby and Afjal H. Miah

RSC Med. Chem., 2025, 16, 1141
DOI: 10.1039/D4MD00760C

High-throughput discovery and characterisation of pentafluorobenzene sulfonamide modifiers of Aurora A kinase

Julian Chesti, Jennifer A. Miles, Lawrence J. Collins, Hamish A. McCallum, Martina Foglizzo, Mohd Syed Ahangar, Elton Zeqiraj, Richard Bayliss, Stuart L. Warriner, Megan H. Wright and Adam Nelson

RSC Chem. Biol., 2026, 7, 862
DOI: 10.1039/D5CB00290G

Covalent fragment screening to inhibit the E3 ligase activity of bacterial NEL enzymes SspH1 and SspH2

Cassandra R. Kennedy, Katherine A. McPhie, Aini Vuorinen, Jane Dudley-Fraser, Diego Esposito, Sarah Maslen, William J. McCarthy, Jonathan Pettinger, J. Mark Skehel, Jacob Bush, David House and Katrin Rittinger

RSC Chem. Biol., 2026, 7, 153
DOI: 10.1039/D5CB00177C

Covalent-reversible peptide-based protease inhibitors. Design, synthesis, and clinical success stories

Anthony Feral, Anthony R. Martin, Alexandre Desfoux, Muriel Amblard and Lubomir L. Vezenkov

Amino Acids, 2023, 55, 1775
DOI: 10.1007/s00726-023-03286-1

Covalent hits and where to find them

Simon C.C. Lucas, J. Henry Blackwell, Sarah H. Hewitt, Hannah Semple, Benjamin C. Whitehurst and Hua Xu

SLAS Discovery, 2024, 29, 100142
DOI: 10.1016/j.slasd.2024.01.003

Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening

Harry Wilders, George Biggs, Sam M. Rowe, Emma E. Cawood, Ioannis G. Riziotis, Alan R. Rendina, Emma K. Grant, Jonathan Pettinger, David J. Fallon, Mark Skehel, David House, Nicholas C. O. Tomkinson and Jacob T. Bush

Angewandte Chemie, 2025, 137
DOI: 10.1002/ange.202418314

Fragment-to-Lead Medicinal Chemistry Publications in 2023

Rhian S. Holvey, Daniel A. Erlanson, Iwan J. P. de Esch, Barbara Farkaš, Wolfgang Jahnke, Tsuyoshi Nishiyama and Andrew J. Woodhead

J. Med. Chem., 2025, 68, 986
DOI: 10.1021/acs.jmedchem.4c02593

Modular Rh‐Catalyzed Synthesis and Biological Profiling of Diverse Pentafluorobenzenesulfonamide Reactive Fragments

Julian Chesti, Jennifer A. Miles, George J. Wade, Scott Grossman, George W. Preston, Richard Bayliss, Stuart L. Warriner, Megan H. Wright and Adam Nelson

Chemistry A European J, 2026
DOI: 10.1002/chem.202600009

Direct‐to‐Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery

Ariane F. Hübner and Fabian Barthels

ChemMedChem, 2026, 21
DOI: 10.1002/cmdc.202501080

Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening

Harry Wilders, George Biggs, Sam M. Rowe, Emma E. Cawood, Ioannis G. Riziotis, Alan R. Rendina, Emma K. Grant, Jonathan Pettinger, David J. Fallon, Mark Skehel, David House, Nicholas C. O. Tomkinson and Jacob T. Bush

Angew Chem Int Ed, 2025, 64
DOI: 10.1002/anie.202418314

Covalent fragment approaches targeting non-cysteine residues

Noémi Csorba, Péter Ábrányi-Balogh and György M. Keserű

Trends in Pharmacological Sciences, 2023, 44, 802
DOI: 10.1016/j.tips.2023.08.014

Collaborative GSK–University of Strathclyde doctoral research and training programmes: Transforming approaches to industry–academia engagement

Laura C. Paterson, Philip G. Humphreys, Henry A. Kelly and William J. Kerr

Drug Discovery Today, 2024, 29, 104162
DOI: 10.1016/j.drudis.2024.104162

Covalent Inhibitors - An Overview of Design Process, Challenges and Future Directions

Simon Mugisa and Manikanta Murahari

COC, 2025, 29, 1424
DOI: 10.2174/0113852728361926250123092017

Oxadiazolines as Photoreleasable Labels for Drug Target Identification

Corentin Bon, Benedikt Goretzki, Marie Flamme, Claude Shelton, Holly Davis, Fabio Lima, Francisco Garcia, Scott Brittain and Cara E. Brocklehurst

J. Am. Chem. Soc., 2024, 146, 26759
DOI: 10.1021/jacs.4c06936

Formation of Nitrile Imine in the Ground and Excited States from Photolysis of 2-N-Methylpyrrole-5-formylamino-tetrazole

Lei Zhao, Ye-Guang Fang, Bin-Bin Xie, Qiu Fang, Haobin Wang and Wei-Hai Fang

J. Phys. Chem. Lett., 2025, 16, 10149
DOI: 10.1021/acs.jpclett.5c02521