Literature summary for 2.7.8.27 extracted from

Gong, H.; Zhou, L.; Ye, D.; Gao, X.; Li, Y.; Qi, X.; Chu, Y.
Novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase Design, synthesis and evaluation (2016), Lett. Drug Des. Discov., 13, 1025-1032 .

No PubMed abstract available

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-[[2-((5-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)pentyl)oxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide	compound shows dual activity against both phospholipase A2 and sphingomyelin synthase	Homo sapiens
2-[[2-((6-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)hexyl)oxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide	-	Homo sapiens
2-[[2-(3-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)propoxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide	-	Homo sapiens
2-[[2-(4-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)butoxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide	-	Homo sapiens
additional information	design of dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase by linking or fusing sphingomyelin synthase inhibitor fragment Ly18 (N-pyridine-3-amide moiety) with phospholipase A2 inhibitor fragment (indole-3-acetamide structure) by 3-6 carbon chain	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q8NHU3	-	-

Synonyms

Synonyms	Comment	Organism
Sgms2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0253	-	pH 7.4, 37°C	Homo sapiens	2-[[2-((5-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)pentyl)oxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide
0.0265	-	pH 7.4, 37°C	Homo sapiens	2-[[2-(3-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)propoxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide
0.0287	-	pH 7.4, 37°C	Homo sapiens	2-[[2-((6-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)hexyl)oxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide
0.0617	-	pH 7.4, 37°C	Homo sapiens	2-[[2-(4-(3-(2-amino-2-oxoethyl)-5-methoxy-2-methyl-1H-indol-1-yl)butoxy)benzyl]oxy]-N-(pyridin-3-yl)benzamide

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Release 2023.1 (January 2023)