Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli BL21 (DE3) pLysS cells | Mycobacterium tuberculosis |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(-(5-nitrothiazol-2-yl)piperidin-4-yl)-3-phenylthiourea | - |
Mycobacterium tuberculosis | |
1-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)-3-phenylurea | - |
Mycobacterium tuberculosis | |
1-(4-acetylphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-acetylphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-chlorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-chlorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-chlorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-chlorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-fluorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-fluorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-fluorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-fluorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-methoxybenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-methoxybenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-methoxyphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-methoxyphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-nitrophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-nitrophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(4-tolyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-(4-tolyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
1-(5-nitrothiazol-2-yl)-N-phenylpiperidin-4-amine | - |
Mycobacterium tuberculosis | |
1-benzyl-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | - |
Mycobacterium tuberculosis | |
1-benzyl-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | - |
Mycobacterium tuberculosis | |
4-chloro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | - |
Mycobacterium tuberculosis | |
4-chloro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | - |
Mycobacterium tuberculosis | |
4-fluoro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | - |
Mycobacterium tuberculosis | |
4-fluoro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | - |
Mycobacterium tuberculosis | |
4-methoxy-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | - |
Mycobacterium tuberculosis | |
4-methoxy-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | - |
Mycobacterium tuberculosis | |
6-(3,4-dimethylphenyl)-3-[[4-[3-(4-methylpiperazin-1-yl)propoxy]phenyl]amino]pyrazine-2-carboxamide | - |
Mycobacterium tuberculosis | |
additional information | not inhibited by Isoniazid, rifampicin, and afloxacin | Mycobacterium tuberculosis | |
N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)-1-phenylmethanesulfonamide | - |
Mycobacterium tuberculosis | |
N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)-2-phenylacetamide | - |
Mycobacterium tuberculosis | |
N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | - |
Mycobacterium tuberculosis | |
N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | - |
Mycobacterium tuberculosis | |
N-(4-chlorobenzyl)-1-(5-nitrothiazol-2-yl)piperidin-4-amine | - |
Mycobacterium tuberculosis | |
N-(4-fluorobenzyl)-1-(5-nitrothiazol-2-yl)piperidin-4-amine | - |
Mycobacterium tuberculosis | |
N-(4-methoxybenzyl)-1-(5-nitrothiazol-2-yl)piperidin-4-amine | - |
Mycobacterium tuberculosis | |
N-benzyl-1-(5-nitrothiazol-2-yl)piperidin-4-amine | - |
Mycobacterium tuberculosis | |
novobiocin | potent inhibitor | Mycobacterium tuberculosis |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | 0.016 mM used in assay conditions | Mycobacterium tuberculosis |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mycobacterium tuberculosis | - |
- |
- |
Mycobacterium tuberculosis H37Rv | - |
- |
- |
Purification (Comment) | Organism |
---|---|
Ni-NTA column chromatography | Mycobacterium tuberculosis |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + relaxed pBR322 DNA | - |
Mycobacterium tuberculosis | ADP + phosphate + supercoiled pBR322 DNA | - |
? | |
ATP + relaxed pBR322 DNA | - |
Mycobacterium tuberculosis H37Rv | ADP + phosphate + supercoiled pBR322 DNA | - |
? |
Synonyms | Comment | Organism |
---|---|---|
DNA gyrase B | - |
Mycobacterium tuberculosis |
DNA gyrB | - |
Mycobacterium tuberculosis |
GyrB | - |
Mycobacterium tuberculosis |
gyrB ATPase | - |
Mycobacterium tuberculosis |
type II topoisomerase | - |
Mycobacterium tuberculosis |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0001496 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(4-fluorobenzyl)-1-(5-nitrothiazol-2-yl)piperidin-4-amine | |
0.00018 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | novobiocin | |
0.00023 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | |
0.00105 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | |
0.0015 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-fluorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.0015 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-methoxybenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.00173 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)-2-phenylacetamide | |
0.00175 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)-3-phenylurea | |
0.002136 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-benzyl-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0026 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-fluorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0026 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 4-chloro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | |
0.0035 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 4-chloro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | |
0.00356 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-methoxyphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0036 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-fluorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.004538 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-methoxyphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.00531 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 4-methoxy-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | |
0.0054 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 4-fluoro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | |
0.00585 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-tolyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0064 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-chlorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0065 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 4-methoxy-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzamide | |
0.00733 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(5-nitrothiazol-2-yl)-N-phenylpiperidin-4-amine | |
0.0075 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-benzyl-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.0076 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-methoxybenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.00807 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-fluorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.008707 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-chlorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.00925 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-benzyl-1-(5-nitrothiazol-2-yl)piperidin-4-amine | |
0.0098 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(-(5-nitrothiazol-2-yl)piperidin-4-yl)-3-phenylthiourea | |
0.0098 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-chlorophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0117 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 4-fluoro-N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)benzenesulfonamide | |
0.01305 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-chlorobenzyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.0157 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-acetylphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.01742 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(4-methoxybenzyl)-1-(5-nitrothiazol-2-yl)piperidin-4-amine | |
0.01785 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-tolyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.0199 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(4-chlorobenzyl)-1-(5-nitrothiazol-2-yl)piperidin-4-amine | |
0.02151 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-nitrophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.02331 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-acetylphenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)thiourea | |
0.0239 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | 1-(4-nitrophenyl)-3-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)urea | |
0.0529 | - |
at pH 7.9 and 37°C | Mycobacterium tuberculosis | N-(1-(5-nitrothiazol-2-yl)piperidin-4-yl)-1-phenylmethanesulfonamide |