Cloned (Comment) | Organism |
---|---|
expressed in HEK-293S GnT1 cells | Sus scrofa |
Protein Variants | Comment | Organism |
---|---|---|
D136A | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
D136F | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
D136I | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
D136L | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
D137A | the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, BYK99 and BYK73) | Sus scrofa |
D137F | the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
D137I | the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, and BYK99) | Sus scrofa |
D137L | the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
D138I | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
L139A | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
L139F | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
L139I | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
L141A | the mutant has low ATPase activity | Sus scrofa |
L141F | the mutant has low ATPase activity | Sus scrofa |
L141I | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
N138A | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
N138F | the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
N138L | the mutant shows strongly increased sensitivity against imidazo[1,2-a]pyridine inhibitors (BYK99 and BYK73) | Sus scrofa |
Y140A | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
Y140F | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
Y140I | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
Y140L | the mutant shows wild type-like sensitivity against imidazo[1,2-a]pyridine inhibitors (SCH28080, SCH-Me-, SCH-CN-, BYK99 and BYK73) | Sus scrofa |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | - |
Sus scrofa | |
(7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | high-affinity K+-competitive inhibitor | Sus scrofa | |
8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine | - |
Sus scrofa | |
BYK73 | i.e. (7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | Sus scrofa | |
BYK99 | i.e. (7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol, high-affinity K+-competitive inhibitor | Sus scrofa | |
SCH-CN- | i.e. 8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine | Sus scrofa | |
SCH-Me- | i.e. [8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile | Sus scrofa | |
SCH28080 | i.e. 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile | Sus scrofa | |
[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile | - |
Sus scrofa | |
[8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile | - |
Sus scrofa |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + H2O + H+[side 1] + K+[side 2] | Sus scrofa | - |
ADP + phosphate + H+[side 2] + K+[side 1] | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Sus scrofa | P19156 and P18434 | subunits alpha and beta | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
stomach | - |
Sus scrofa | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + H2O + H+[side 1] + K+[side 2] | - |
Sus scrofa | ADP + phosphate + H+[side 2] + K+[side 1] | - |
? |
Synonyms | Comment | Organism |
---|---|---|
H+,K+-ATPase | - |
Sus scrofa |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000058 | - |
8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.0000058 | - |
BYK99 | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.00015 | - |
SCH28080 | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.0015 | - |
(7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.0032 | - |
[8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.0032 | - |
SCH-CN- | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.0049 | - |
(7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.0049 | - |
BYK73 | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.011 | - |
[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | |
0.011 | - |
SCH-Me- | wild type enzyme, at pH 7.6 and 37°C | Sus scrofa |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000077 | - |
wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | (7R,8R,9R)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | |
0.0011 | - |
at pH 7.6 and 37°C | Sus scrofa | SCH28080 | |
0.011 | - |
wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | [8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile | |
0.029 | - |
wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | (7R,8R,9R)-2,3,10-trimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridine-7,8-diol | |
0.054 | - |
wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | [8-(benzyloxy)imidazo[1,2-a]pyridin-3-yl]acetonitrile | |
0.11 | - |
wild type enzyme, at pH 7.6 and 37°C | Sus scrofa | 8-(benzyloxy)-2-methylimidazo[1,2-a]pyridine |