Covalent Modifiers

MARCH 19, 2024

Flaherty Journal of Medicinal Chemistry 2024 DOI: 10.1021/acs.jmedchem.3c01661 Herein, we describe a covalent fragment screen that identified the chloroacetohydrazide scaffold as a covalent UCHL1 inhibitor. Jones, Adan Pinto-Fernandez, Iolanda Vendrell, Hao Chen, Christine S. Muli, Aaron D. Krabill, Benedikt M.

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Fragment Screening Disease Treatment 195

Drug Target Review

APRIL 7, 2025

PoLiPa detergent-free stabilisation of membrane proteins enables the application of fragment-based screening to GPCRs, expanding the methods possible targets and opening the potential to develop novel therapeutics agents as a result. Available at: [link] (Accessed: 23 September 2024). References Sun D, et al. Jones EM, et al.

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Fragment Screening Drugs Small Molecule Biophysical Assays 52

Covalent Modifiers

DECEMBER 3, 2024

Marto SLAS Discovery, 2024 [link] Target-based screening of covalent fragment libraries with mass spectrometry has emerged as a powerful strategy to identify chemical starting points for small molecule inhibitors or find new binding pockets on proteins of interest. Buhrlage, Jarrod A.

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Fragment Screening Compound Screening Small Molecule Drugs 147

Covalent Modifiers

DECEMBER 27, 2024

2024 , e202419736 [link] Protein kinases are important drug targets, yet specific inhibitors have been developed for only a fraction of the more than 500 human kinases. Previously, covalent fragment screens yielded potent and selective compounds for individual kinases such as ERK1/2 but have not been applied to the broader kinome.

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Fragment Screening Drugs 162