Discovery of a Potent, Selective, and Brain-Penetrant Checkpoint Kinase 1 Inhibitor, BEN-28010, for the Treatment of Glioblastoma.

Michael J Rawling¹, Arpita Ray-Sinha², Michael Bestwick¹, Michael K Carter², Sandeep K Chahal³, Anthony J Chalmers³, David J Elsey², Amanda Giddings², Jennie Gold¹, Scott H Henderson¹, Calum MacGregor², Andrew Malcolm¹, Fernando Ortega¹, Anne Phelan¹, Edward D Savory¹, Alejandro C Schwartz¹, Neil G Stevenson¹, Emma L Turner¹, Márton Vass², Jamie A Wright¹, Christine Watson¹

¹BenevolentAI, Minerva Building, Babraham Research Campus, Cambridge CB22 3AT, U.K.

²BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K.

³School of Cancer Sciences, University of Glasgow, Glasgow G61 1QH, U.K.

PubMed DOI

Abstract

Glioblastoma (GBM) patients face a dire prognosis and alternative therapeutic options are desperately needed. Inhibition of checkpoint kinase 1 (CHK1) represents a potential therapeutic strategy for GBM through regulation of the DNA damage response (DDR) pathway, but no suitable brain-penetrant CHK1 inhibitors have been reported to date. In this study, we disclose the discovery and optimization of…

Create a free account to keep reading

Free members get 10 full research views every month across publications, clinical trials, FDA clearances, adverse events, and NIH grants. No credit card required.

Create Free Account Sign In

Want unlimited research access? See Pro plans

Data Accuracy Notice: Research intelligence on Health AI Central is aggregated from public sources (PubMed, ClinicalTrials.gov, FDA, NIH, CMS, and others) and refreshed nightly. Classifications and derived metrics are produced by automated methods described in our Methodology. We recommend verifying critical data points against the primary sources before making decisions.