Drug Discovery Technology Review: Emerging Tools and Modalities in 2022Q1

DILI is a leading cause of acute liver failure, accounting for half of these cases and often resulting in drug withdrawals. Understanding and managing DILI risk as a medicinal chemist involves exploring the intricate interplay among properties and structural features. In this article, we provide a medicinal chemist's perspective on the current understanding of DILI mechanisms, highlight cutting-edge assay developments for a holistic assessment, and discuss strategies for predicting DILI risks.

Drug Hunter has sifted through news articles, press releases, financial disclosures, SEC filings, and more to bring you a roundup of 2023’s biggest mergers and acquisitions (M&A) in the drug discovery world. Following our open-access industry overview, in part 2 of this 4-part series we bring you the small molecule-focused deals, ranked 11-20 by value. Covering a range of targets and modalities, this article gives Drug Hunter members in-depth background and analysis of the hottest science opening checkbooks in 2023.

There has been substantial interest in the development of screening methods capable of surveying a wider sample of chemical space and larger numbers of compounds. Over the past two decades, DEL technology has evolved into a broadly utilized and validated platform in drug discovery, yielding diverse hits for a wide range of biologically relevant targets. Read the full review for a historical and technical overview of DEL technology, including how libraries are prepared and screened, a comparison to other HTS methods, and examples of successful applications in drug discovery.

This article highlights million-dollar molecules that were recently in the news with related patent applications that give clues to their structures and properties. This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, brain-penetrant HER2 and ROCK2 inhibitors, and MDM2 degraders.

Peptidic GLP-1R agonists have received significant media coverage over the past year for their astounding efficacy in several indications. While most of the recent fanfare has been related to their role in weight loss, GLP-1R agonists have been a mainstay of the type 2 diabetes treatment landscape for the past 2 decades. GLP-1R agonists have also recently shown efficacy in reducing heart disease risk and treating certain chronic kidney diseases. Here’s a recap of the March 14th, 2024, Flash Talk, from Oliver Philps.