CCF0058981 (CCF981), 3-chlorophenyl analogue, is a noncovalent SARS-CoV-2 3CLpro (SC2) inhibitor with an IC50 of 68 nM. CCF0058981 inhibits SC1 (SARS-CoV-1 3CLpro) with an IC50 of 19 nM. CCF0058981 has antiviral efficacy and has the potential for COVID-19 research[1].
CCF0058981 (CCF981) has cytopathic effect (CPE) inhibition (EC50=497 nM) and plaque reduction (EC50=558 nM) in vitro viral replication[1]. CCF0058981 has the 50% cytotoxic concentration (CC50) in the CPE antiviral assay of >50 μM[1]. CCF0058981 has a T1/2 of 21.1 min, a CLlnt of 141 mL/min•kg in Human liver microsomes[1].
[1]. Sang Hoon Han, et al. Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL pro). J Med Chem. 2021 Aug 4;acs.jmedchem.1c00598.