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Literature summary for 3.4.21.105 extracted from

  • Wolf, E.V.; Zeissler, A.; Vosyka, O.; Zeiler, E.; Sieber, S.; Verhelst, S.H.
    A new class of rhomboid protease inhibitors discovered by activity-based fluorescence polarization (2013), PLoS ONE, 8, e72307.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.105

Application

Application Comment Organism
analysis screening assay using fluorescence polarization activity-based protein profiling Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
7-amino-3-butoxy-4-chloro-1H-isochromen-1-one
-
 Escherichia coli
7-amino-4-chloro-3-(2-phenylethoxy)-1H-isochromen-1-one
-
 Escherichia coli
7-amino-4-chloro-3-[(5-phenylpentyl)oxy]-1H-isochromen-1-one
-
 Escherichia coli
additional information identification of beta-lactone inhititors that form covalent and irreversible complexes with the active site serine of GlpG. The presence of alkyne handles on the beta-lactones also allows activity-based labeling Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli P09391
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0004
-
 pH 7.3, 37°C Escherichia coli 7-amino-3-butoxy-4-chloro-1H-isochromen-1-one
0.00075
-
 pH 7.3, 37°C Escherichia coli 7-amino-4-chloro-3-[(5-phenylpentyl)oxy]-1H-isochromen-1-one
0.0011
-
 pH 7.3, 37°C Escherichia coli 7-amino-4-chloro-3-(2-phenylethoxy)-1H-isochromen-1-one