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Literature summary extracted from

  • Zimmermann, P.J.; Brehm, C.; Buhr, W.; Palmer, A.M.; Volz, J.; Simon, W.A.
    Novel imidazo[1,2-a]pyrazine derivatives as potent reversible inhibitors of the gastric H+/K+-ATPase (2008), Bioorg. Med. Chem., 16, 536-541.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.2.2.19 (8-[(2-ethyl-6-methylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyrazin-6-yl)methanol
-
 Sus scrofa
7.2.2.19 2-aminopyrazine
-
 Sus scrofa
7.2.2.19 8-[(2-ethyl-6-methylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide
-
 Sus scrofa
7.2.2.19 8-[(2-ethyl-6-methylbenzyl)amino]-N,2,3-trimethylimidazo[1,2-a]pyrazine-6-carboxamide
-
 Sus scrofa
7.2.2.19 8-[(2-ethyl-6-methylbenzyl)amino]-N,N,2,3-tetramethylimidazo[1,2-a]pyrazine-6-carboxamide
-
 Sus scrofa
7.2.2.19 8-[(2-ethyl-6-methylbenzyl)amino]-N-(2-hydroxyethyl)-2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide
-
 Sus scrofa
7.2.2.19 8-[(2-ethyl-6-methylbenzyl)amino]-N-(2-methoxyethyl)-2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide
-
 Sus scrofa
7.2.2.19 additional information development of 6-substituted imidazo[1,2-a]pyrazines inhibitors of the gastric H+/K+-ATPase, no inhibition by 8-[(2-ethyl-6-methylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide Sus scrofa
7.2.2.19 N-(2-ethyl-6-methylbenzyl)-2,3-dimethyl-6-(pyrrolidin-1-ylcarbonyl)imidazo[1,2-a]pyrazin-8-amine
-
 Sus scrofa
7.2.2.19 N-(2-ethyl-6-methylbenzyl)-6-(methoxymethyl)-2,3-dimethylimidazo[1,2-a]pyrazin-8-amine
-
 Sus scrofa
7.2.2.19 SCH 32651
-
 Sus scrofa

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
7.2.2.19 membrane
-
 Sus scrofa 16020
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
7.2.2.19 K+ stimulates Sus scrofa
7.2.2.19 Mg2+ required Sus scrofa

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.2.2.19 ATP + H2O + H+/in + K+/out Sus scrofa
-
 ADP + phosphate + H+/out + K+/in
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
7.2.2.19 Sus scrofa
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.2.2.19 stomach mucosa Sus scrofa
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.2.2.19 ATP + H2O + H+/in + K+/out
-
 Sus scrofa ADP + phosphate + H+/out + K+/in
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.2.2.19 gastric H+/K+-ATPase
-
 Sus scrofa
7.2.2.19 H+/K+-ATPase
-
 Sus scrofa

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.2.2.19 22
-
 assay at room temperature Sus scrofa

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2.2.19 7.4
-
 assay at Sus scrofa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
7.2.2.19 0.005
-
 pH 7.4, 22°C Sus scrofa 8-[(2-ethyl-6-methylbenzyl)amino]-N-(2-hydroxyethyl)-2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide
7.2.2.19 0.0055
-
 pH 7.4, 22°C Sus scrofa 8-[(2-ethyl-6-methylbenzyl)amino]-N,2,3-trimethylimidazo[1,2-a]pyrazine-6-carboxamide
7.2.2.19 0.0055
-
 pH 7.4, 22°C Sus scrofa N-(2-ethyl-6-methylbenzyl)-6-(methoxymethyl)-2,3-dimethylimidazo[1,2-a]pyrazin-8-amine
7.2.2.19 0.0059
-
 pH 7.4, 22°C Sus scrofa SCH 32651
7.2.2.19 0.0059
-
 pH 7.4, 22°C Sus scrofa (8-[(2-ethyl-6-methylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyrazin-6-yl)methanol
7.2.2.19 0.006
-
 pH 7.4, 22°C Sus scrofa 8-[(2-ethyl-6-methylbenzyl)amino]-N-(2-methoxyethyl)-2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide
7.2.2.19 0.0064
-
 pH 7.4, 22°C Sus scrofa 8-[(2-ethyl-6-methylbenzyl)amino]-N,N,2,3-tetramethylimidazo[1,2-a]pyrazine-6-carboxamide
7.2.2.19 0.0069
-
 pH 7.4, 22°C Sus scrofa N-(2-ethyl-6-methylbenzyl)-2,3-dimethyl-6-(pyrrolidin-1-ylcarbonyl)imidazo[1,2-a]pyrazin-8-amine