Development of GS-441524 Derivatives as Potent SARS-CoV-2 Mac1 Inhibitors via a Direct-to-Biology Approach
Kewen Peng, Suryadeep Chakraborty, Shamar D. Wallace, Jéssica Caroline Gomes Noll, Jialin Shang, Xuan Lu, Annette Choi, gary whittaker, J. Christopher Fromme, Hening Lin
The paper develops potent SARS-CoV-2 Mac1 inhibitors through a direct-to-biology approach, improving the potency of GS-441524 to KP-S54 with IC50 values of 44 nM and 91 nM against SARS-CoV-2 and MERS-CoV Mac1, respectively.
European Journal of Medicinal Chemistry · Aug 28, 2026Peer-reviewedPharmacology & Toxicology