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Literature summary for 5.4.99.9 extracted from

  • Carlson, E.E.; May, J.F.; Kiessling, L.L.
    Chemical probes of UDP-galactopyranose mutase (2006), Chem. Biol., 13, 825-837.
    View publication on PubMed

Application

Application Comment Organism
analysis high-throughput fluorescence polarization assay for indentification of inhibitors of enzyme and homologues Klebsiella pneumoniae

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli, His-tagged protein Klebsiella pneumoniae

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-2-(2-chloro-4-hydroxy-5-nitrobenzylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one comparison with inhibition of Mycobacterium tuberculosis enzyme; dissociation constant 0.0053 mM, comparison with inhibition of Klebsiella pneumoniae enzyme Klebsiella pneumoniae
(4E)-4-(4-chloro-3-nitrobenzylidene)-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione comparison with inhibition of Mycobacterium tuberculosis enzyme; dissociation constant 0.0049 mM, comparison with inhibition of Klebsiella pneumoniae enzyme Klebsiella pneumoniae
2-(([2-(4-bromophenyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]carbonyl)amino)benzoic acid comparison with inhibition of Mycobacterium tuberculosis enzyme Klebsiella pneumoniae
2-[(5E)-5-(3-bromobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid comparison with inhibition of Mycobacterium tuberculosis enzyme; dissociation constant 0.0094 mM, comparison with inhibition of Klebsiella pneumoniae enzyme Klebsiella pneumoniae
2-[(5E)-5-(4-bromobenzylidene)-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid dissociation constant 0.0093 mM, comparison with inhibition of Klebsiella pneumoniae enzyme Klebsiella pneumoniae

Organism

Organism UniProt Comment Textmining
Klebsiella pneumoniae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-D-galactofuranose
-
Klebsiella pneumoniae UDP-D-galactopyranose
-
r
UDP-D-galactopyranose
-
Klebsiella pneumoniae UDP-D-galactofuranose
-
r

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0016
-
pH 7.0, 37°C Klebsiella pneumoniae 2-[(5E)-5-(3-bromobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
0.004
-
pH 7.0, 37°C Klebsiella pneumoniae (4E)-4-(4-chloro-3-nitrobenzylidene)-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione
0.004
-
pH 7.0, 37°C Klebsiella pneumoniae (2Z)-2-(2-chloro-4-hydroxy-5-nitrobenzylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
0.0046
-
pH 7.0, 37°C Klebsiella pneumoniae 2-(([2-(4-bromophenyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]carbonyl)amino)benzoic acid
0.035
-
pH 7.0, 37°C Klebsiella pneumoniae (2Z)-2-(2-chloro-4-hydroxy-5-nitrobenzylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
0.041
-
pH 7.0, 37°C Klebsiella pneumoniae (4E)-4-(4-chloro-3-nitrobenzylidene)-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione
0.065
-
pH 7.0, 37°C Klebsiella pneumoniae 2-[(5E)-5-(3-bromobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid