生物活性 | |||
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描述 | The papain-like protease (PLpro) is a viable target for the development of antivirals against coronavirus-caused severe acute respiratory syndrome (SARS-CoV). GRL0617 is a potent competitive inhibitor of PLpro with a Ki value of 0.49 ± 0.08μM. The IC50 value of GRL0617 for PLpro activity in vitro is 0.6 ± 0.1μM. The antiviral EC50 value of GRL0617 against SARS-CoV is 14.5 ± 0.8μM. GRL0617 is unlikely to inhibit other human ubiquitin-specific proteases, such as HAUSP, USP18, UCH-L1, UCH-L3, and papain-like protease (IC50 > 100μM)[1]. The in vitro IC50 value of GRL0617 against SARS-CoV-2 PLpro is 2.1 ± 0.2μM[2]. | ||
作用机制 | GRL0617 binds within the S3 and S4 subsites of PLpro. The interaction between them is stabilized through a pair of hydrogen bonds and a series of hydrophobic interactions[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.29mL 0.66mL 0.33mL |
16.43mL 3.29mL 1.64mL |
32.85mL 6.57mL 3.29mL |
参考文献 |
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