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.

Fragment Screening 162

Fragment Screening Drugs 162

Drug Target Review

APRIL 7, 2025

The challenge of GPCR drug discovery G protein-coupled receptors (GPCRs) are one of the most desirable and challenging target classes in drug discovery, as their mutation can lead to a wide range of diseases such as cancer, cardiovascular disorders and neurological conditions.

Fragment Screening 52

Fragment Screening Drugs Biophysical Assays Small Molecule 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.

Fragment Screening 147

Fragment Screening Compound Screening Small Molecule Drugs 147