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Literature summary for 7.2.2.19 extracted from

  • Zimmermann, P.J.; Buhr, W.; Brehm, C.; Palmer, A.M.; Feth, M.P.; Senn-Bilfinger, J.; Simon, W.A.
    Novel indanyl-substituted imidazo[1,2-a]pyridines as potent reversible inhibitors of the gastric H+/K+-ATPase (2007), Bioorg. Med. Chem. Lett., 17, 5374-5378.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-N,2,3-trimethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-N-(1-methoxyethyl)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]oxy]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
8-[[(1S,2S)-2-hydroxy-7-methoxy-2,3-dihydro-1H-inden-1-yl]oxy]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
8-[[(1S,2S)-2-hydroxy-7-methyl-2,3-dihydro-1H-inden-1-yl]oxy]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
-
Sus scrofa
AR-HO47108
-
Sus scrofa
additional information development of indanyl-substituted imidazo[1,2-a]pyridines as potent reversible inhibitors of the gastric H+/K+-ATPase, overview Sus scrofa
P-CAB1
-
Sus scrofa

Localization

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
parietal cell
-
Sus scrofa
-
stomach
-
Sus scrofa
-

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0047
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-N-(1-methoxyethyl)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
0.0048
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
0.0053
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-N,2,3-trimethylimidazo[1,2-a]pyridine-6-carboxamide
0.0057
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]oxy]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
0.0057
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-7-methoxy-2,3-dihydro-1H-inden-1-yl]oxy]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
0.0062
-
pH 7.4, 22°C Sus scrofa AR-HO47108
0.0063
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide
0.0069
-
pH 7.4, 22°C Sus scrofa 8-[[(1S,2S)-2-hydroxy-7-methyl-2,3-dihydro-1H-inden-1-yl]oxy]-N,N,2,3-tetramethylimidazo[1,2-a]pyridine-6-carboxamide