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20 nM SARS-CoV-2 Protease Inhibitors
20 nM SARS-CoV-2 Protease Inhibitors
Structure-based design of Mpro Antagonists
- Potent (IC50 sub-20nM) series of small molecule, non-peptidic, non-covalent, inhibitors of the SARS- CoV-2 main protease (Mpro) (Table 1).
- OCR8038 inhibitors have 0.2 μM activity in infected cells, while remdesivir is 1.0 μM
- Weak binding non-antiviral approved drug (Table 1/Cmpd 1) optimized for Mpro inhibition (Table 1/Cmpds 18 - 25).
- High-resolution co-crystal structures of complexes (Figure 1).
- Demonstrated anti-viral properties in vitro (Table 2).
- Synergy with remdesivir (Figure2)
- Drug-like properties & commercially viable synthetic routes