Fig. 5: 212-148 is a bispecific compound that blocks both viral entry pathways.
From: Structure-based discovery of dual pathway inhibitors for SARS-CoV-2 entry
a Structure of 212-148. b, c Enzyme inhibition data for 212-148, IC50 values and data points are shown as mean ± SD for four biological independent replicates. (d–f) Antiviral efficacy of 212-148. d Huh-7 cells pre-treated with 212-148 at different concentrations for 1 h and then infected with Omicron BA.2, BA.2.12.1 or BA.4 & BA.5 SARS-CoV-2-S pseudotyped virus (650 TCID50/well). Chemiluminescence signals were detected twenty-four hours after the incubation of cells. e Calu-3 cells pre-treated with 212-148 at different concentrations for 1 h and then infected with clinical SARS-CoV-2 isolates delta strain or omicron strain BA.2 (MOI = 1). Twenty-four hours after inoculation, the supernatants were collected and virus titers were determined as TCID50/mL. f A summary of the results for the antiviral experiments, including the CC50 values of 212-148 in the specific types of cells (Supplementary Fig. 6); n, the number of biological independent replicates. g The catalytic pocket of TMPRSS2 in complex with 212-148. h The catalytic pocket of CTSB in complex with 212-148.
