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Literature summary for 3.4.22.B80 extracted from

  • Ma, C.; Wang, J.
    Validation and invalidation of SARS-CoV-2 papain-like protease inhibitors (2022), ACS Pharmacol. Transl. Sci., 5, 102-109 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-[(pyrazin-2-yl)methyl]-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium i.e. YM15, cytotoxic Severe acute respiratory syndrome coronavirus 2
2-phenylnaphtho[2,3-d][1,3]oxazole-4,9-dione i.e. SJB2-043, cytotoxic Severe acute respiratory syndrome coronavirus 2
6-Mercaptopurine does not show cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
6-thioguanine does not show cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
cryptotanshinone does not show cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
dihydrotanshinone I does not show cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
additional information all compounds tested either did not show binding or lead to denaturation of PLpro in the thermal shift binding assay. None of the compounds shows cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
tanshinone I does not show cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
tanshinone IIA does not show cellular PLpro inhibition Severe acute respiratory syndrome coronavirus 2
YM155
-
Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome coronavirus 2
-
-
-
Severe acute respiratory syndrome coronavirus 2 BetaCoV/Wuhan/WIV04/2019
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0153
-
pH 7.5, 30°C Severe acute respiratory syndrome coronavirus 2 tanshinone IIA
0.0186
-
pH 7.5, 30°C Severe acute respiratory syndrome coronavirus 2 tanshinone I
0.0202
-
pH 7.5, 30°C Severe acute respiratory syndrome coronavirus 2 YM155
0.033
-
pH 7.5, 30°C Severe acute respiratory syndrome coronavirus 2 dihydrotanshinone I
0.0524
-
pH 7.5, 30°C Severe acute respiratory syndrome coronavirus 2 cryptotanshinone