Cloned (Comment) | Organism |
---|---|
expression of isozyme GSTA1-1 in Escherichia coli strain BL21 (DE3) | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-methyl-2-[((2-nitrobenzyl)sulfonyl)]-1H-pyrrole | 44.3% inhibition at 0.1 mM | Homo sapiens | |
1-methyl-2-[(2-nitrobenzyl)sulfanyl]-1H-pyrrole | - |
Homo sapiens | |
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-((1E)-[4-(trifluoromethyl)phenyl]methylene)aniline | 68.4% inhibition at 0.1 mM | Homo sapiens | |
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(4-nitrophenyl)methylene]aniline | 90.0% inhibition at 0.1 mM | Homo sapiens | |
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(phenyl)methylene]aniline | 30.2% inhibition at 0.1 mM | Homo sapiens | |
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-1H-pyrrol-2-ylmethylene]aniline | 36.0% inhibition at 0.1 mM | Homo sapiens | |
2-[(1-methyl-1H-pyrrol-2-ylsulfonyl)methyl]aniline | 28.0% inhibition at 0.1 mM | Homo sapiens | |
bromosulfophthalein | - |
Homo sapiens | |
additional information | synthesis, screening, and potencies of 2-(pyrrolesulfonylmethyl)-N-arylimines as inhibitors of human glutathione transferase A1-1, in silico molecular docking analysis and molecular modeling, overview | Homo sapiens | |
N-((1E)-[4-(dimethylamino)phenyl]methylene)-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline | 78.9% inhibition at 0.1 mM | Homo sapiens | |
N-[(1E)-(2-chlorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline | 88.8% inhibition at 0.1 mM | Homo sapiens | |
N-[(1E)-(4-chlorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline | 60.4% inhibition at 0.1 mM | Homo sapiens | |
N-[(1E)-(4-fluorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline | 37.1% inhibition at 0.1 mM | Homo sapiens | |
N-[(1E)-(5-bromo-2-methoxyphenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline | 646% inhibition at 0.1 mM | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isozyme GSTA1-1 | - |
Purification (Comment) | Organism |
---|---|
recombinant isozyme GSTA1-1 from Escherichia coli strain BL21 (DE3) by glutathione affinity chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
1-chloro-2,4-dinitrobenzene + glutathione | - |
Homo sapiens | 2,4-dinitrophenyl-glutathione + HCl | - |
? |
Synonyms | Comment | Organism |
---|---|---|
GSTA1-1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics of 2-(pyrrolesulfonylmethyl)-N-arylimines versus substrate 1-chloro-2,4-dinitrobenzene on GSTA1-1, overview | Homo sapiens | |
0.071 | - |
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(4-nitrophenyl)methylene]aniline | pH 6.5, 25°C | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
physiological function | overexpression of human GSTA1-1 in tumor cells is part of multi drug resistance mechanisms | Homo sapiens |