Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.5.1.18 extracted from

  • Xie, Y.; Tummala, P.; Oakley, A.J.; Deora, G.S.; Nakano, Y.; Rooke, M.; Cuellar, M.E.; Strasser, J.M.; Dahlin, J.L.; Walters, M.A.; Casarotto, M.G.; Board, P.G.; Baell, J.B.
    Development of benzenesulfonamide derivatives as potent glutathione transferase omega-1 inhibitors (2020), J. Med. Chem., 63, 2894-2914 .
    View publication on PubMed
Search for more literature for 2.5.1.18

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapor diffusion method, using 1.7-2.2 M (NH4)2SO4, 0.2 M sodium potassium tartrate, 0.75 mM ZnSO4, 17 mM citric acid Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)methanesulfonyl fluoride
-
 Homo sapiens
(E)-2-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)ethene-1-sulfonyl fluoride
-
 Homo sapiens
(E)-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)but-2-enamide
-
 Homo sapiens
2-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)ethane-1-sulfonyl fluoride
-
 Homo sapiens
2-chloro-5-((cyanomethyl)amino)-N,N-dimethylbenzenesulfonamide
-
 Homo sapiens
2-chloro-N,N-dimethyl-5 -(oxiran-2-ylmethyl) -benzenesulfonamide
-
 Homo sapiens
2-chloro-N,N-dimethyl-5-(oxiran-2-yl)benzenesulfonamide
-
 Homo sapiens
2-chloro-N-(2-(N,N-dimethylsulfamoyl)-[1,1'-biphenyl]-4-yl)-acetamide
-
 Homo sapiens
2-chloro-N-(3-(morpholinosulfonyl)-4-(trifluoromethyl)phenyl)-acetamide
-
 Homo sapiens
2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethoxy)-phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethyl)-phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-iodophenyl)-acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(morpholinosulfonyl)phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-propanamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-((tetrahydrofuran-2-yl)methyl)-sulfamoyl)phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(2-hydroxyethyl)-N-methylsulfamoyl)phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(2-hydroxyethyl)sulfamoyl)phenyl)-acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(2-methoxyethyl)-N-methylsulfamoyl)phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(2-methoxyethyl)sulfamoyl)phenyl)-acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(3-methoxypropyl)-N-methylsulfamoyl)phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(3-methoxypropyl)sulfamoyl)phenyl)-acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-(tetrahydrofuran-3-yl)sulfamoyl)-phenyl)acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-isopropylsulfamoyl)phenyl)-acetamide
-
 Homo sapiens
2-chloro-N-(4-chloro-3-(N-methylsulfamoyl)phenyl)acetamide
-
 Homo sapiens
2-chloro-N-[4-chloro-3-(N,N-dimethylsulfamoyl)phenyl]acetamide i.e. C1-27 Homo sapiens
3-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)propane-1-sulfonyl fluoride
-
 Homo sapiens
3-chloro-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-propenamide
-
 Homo sapiens
N-(4-bromo-3-(N,N-dimethylsulfamoyl)phenyl)-2-chloroacetamide
-
 Homo sapiens
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-cyanoacetamide
-
 Homo sapiens
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-fluoroacetamide
-
 Homo sapiens
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-oxopropanamide
-
 Homo sapiens
N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)acrylamide
-
 Homo sapiens
N1-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)oxalamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-(4-nitrophenacyl)-glutathione
-
 Homo sapiens 4-nitroacetophenone + glutathione
-
 ?

Synonyms

Synonyms Comment Organism
glutathione transferase omega-1
-
 Homo sapiens
GSTO1-1
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00044
-
 2-chloro-N-[4-chloro-3-(N,N-dimethylsulfamoyl)phenyl]acetamide at pH 8.0 and 37°C Homo sapiens
0.00061
-
 2-chloro-N-(3-(morpholinosulfonyl)-4-(trifluoromethyl)phenyl)-acetamide at pH 8.0 and 37°C Homo sapiens
0.0012
-
 2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethyl)-phenyl)acetamide at pH 8.0 and 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00003
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(2-methoxyethyl)sulfamoyl)phenyl)-acetamide
0.00006
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethyl)-phenyl)acetamide
0.00007
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-isopropylsulfamoyl)phenyl)-acetamide
0.00008
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(2-methoxyethyl)-N-methylsulfamoyl)phenyl)acetamide
0.00011
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(3-methoxypropyl)sulfamoyl)phenyl)-acetamide
0.00013
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-iodophenyl)-acetamide
0.00013
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-[4-chloro-3-(N,N-dimethylsulfamoyl)phenyl]acetamide
0.00015
-
 at pH 8.0 and 37°C Homo sapiens N-(4-bromo-3-(N,N-dimethylsulfamoyl)phenyl)-2-chloroacetamide
0.00016
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(morpholinosulfonyl)phenyl)acetamide
0.00016
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(3-methoxypropyl)-N-methylsulfamoyl)phenyl)acetamide
0.00018
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(2-hydroxyethyl)-N-methylsulfamoyl)phenyl)acetamide
0.0002
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-((tetrahydrofuran-2-yl)methyl)-sulfamoyl)phenyl)acetamide
0.00021
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(3-(N,N-dimethylsulfamoyl)-4-(trifluoromethoxy)-phenyl)acetamide
0.00025
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(3-(morpholinosulfonyl)-4-(trifluoromethyl)phenyl)-acetamide
0.00034
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(tetrahydrofuran-3-yl)sulfamoyl)-phenyl)acetamide
0.00058
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-methylsulfamoyl)phenyl)acetamide
0.0007
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N-(2-hydroxyethyl)sulfamoyl)phenyl)-acetamide
0.00071
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(2-(N,N-dimethylsulfamoyl)-[1,1'-biphenyl]-4-yl)-acetamide
0.0008
-
 at pH 8.0 and 37°C Homo sapiens (4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)methanesulfonyl fluoride
0.0012
-
 at pH 8.0 and 37°C Homo sapiens 2-chloro-N,N-dimethyl-5-(oxiran-2-yl)benzenesulfonamide
0.0032
-
 at pH 8.0 and 37°C Homo sapiens 3-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)propane-1-sulfonyl fluoride
0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 37°C Homo sapiens (E)-2-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)ethene-1-sulfonyl fluoride
0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 37°C Homo sapiens 2-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)ethane-1-sulfonyl fluoride
0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 37°C Homo sapiens 2-chloro-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-propanamide
0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 37°C Homo sapiens 3-chloro-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-propenamide
0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 37°C Homo sapiens N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-oxopropanamide
0.1
-
 IC50 above 0.1 mM, at pH 8.0 and 37°C Homo sapiens (E)-N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)but-2-enamide
0.1
-
 IC50 above 0.1 mM, at pH 8.0 and 37°C Homo sapiens 2-chloro-5-((cyanomethyl)amino)-N,N-dimethylbenzenesulfonamide
0.1
-
 IC50 above 0.1 mM, at pH 8.0 and 37°C Homo sapiens 2-chloro-N,N-dimethyl-5 -(oxiran-2-ylmethyl) -benzenesulfonamide
0.1
-
 IC50 above 0.1 mM, at pH 8.0 and 37°C Homo sapiens N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-cyanoacetamide
0.1
-
 IC50 above 0.1 mM, at pH 8.0 and 37°C Homo sapiens N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)-2-fluoroacetamide
1
-
 IC50 above 1.0 mM, at pH 8.0 and 37°C Homo sapiens N-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)acrylamide
1
-
 IC50 above 1.0 mM, at pH 8.0 and 37°C Homo sapiens N1-(4-chloro-3-(N,N-dimethylsulfamoyl)phenyl)oxalamide