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Literature summary for 3.4.22.B80 extracted from

  • Liu, N.; Zhang, Y.; Lei, Y.; Wang, R.; Zhan, M.; Liu, J.; An, Y.; Zhou, Y.; Zhan, J.; Yin, F.; Li, Z.
    Design and evaluation of a novel peptide-drug conjugate covalently targeting SARS-CoV-2 papain-like protease (2022), J. Med. Chem., 65, 876-884 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.B80

Inhibitors

Inhibitors Comment Organism Structure
5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide i.e. GRL0617 severe acute respiratory syndrome coronavirus
5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide i.e. GRL0617 Severe acute respiratory syndrome coronavirus 2
5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-C peptide-drug conjugate, in which 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide is linked to a sulfonium-tethered peptide derived from PLpro-specific substrate LRGG. The inhibitor can covalently label PLpro active site C111 and displays anti-ISGylation activities in cellular assays severe acute respiratory syndrome coronavirus
5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-C peptide-drug conjugate, in which 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide is linked to a sulfonium-tethered peptide derived from PLpro-specific substrate LRGG. The inhibitor can covalently label PLpro active site C111 and displays anti-ISGylation activities in cellular assays Severe acute respiratory syndrome coronavirus 2
5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-M peptide-drug conjugate, in which 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide is linked to a sulfonium-tethered peptide derived from PLpro-specific substrate LRGG. The inhibitor can covalently label PLpro active site C111 and displays anti-ISGylation activities in cellular assays severe acute respiratory syndrome coronavirus
5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-M peptide-drug conjugate, in which 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide is linked to a sulfonium-tethered peptide derived from PLpro-specific substrate LRGG. The inhibitor can covalently label PLpro active site C111 and displays anti-ISGylation activities in cellular assays Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
severe acute respiratory syndrome coronavirus
-
-
-
Severe acute respiratory syndrome coronavirus 2 P0DTD1 replicase polyprotein 1ab
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-Leu-Arg-Gly-Gly-ACC + H2O
-
 Severe acute respiratory syndrome coronavirus 2 ?
-
 ?
Ac-Leu-Arg-Gly-Gly-ACC + H2O
-
 severe acute respiratory syndrome coronavirus ?
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00343
-
 pH 7.4, 37°C severe acute respiratory syndrome coronavirus 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-C
0.0074
-
 pH 7.4, 37°C Severe acute respiratory syndrome coronavirus 2 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-C
0.00863
-
 pH 7.4, 37°C Severe acute respiratory syndrome coronavirus 2 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-M
0.0164
-
 pH 7.4, 37°C severe acute respiratory syndrome coronavirus 5-amino-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide pepide conjugate EC-M