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Literature summary for 2.7.1.153 extracted from

  • Sanchez, R.M.; Erhard, K.; Hardwicke, M.A.; Lin, H.; McSurdy-Freed, J.; Plant, R.; Raha, K.; Rominger, C.M.; Schaber, M.D.; Spengler, M.D.; Moore, M.L.; Yu, H.; Luengo, J.I.; Tedesco, R.; Rivero, R.A.
    Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent beta isoform selective phosphatidylinositol 3-kinase inhibitors (2012), Bioorg. Med. Chem. Lett., 22, 3198-3202.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
-
 Homo sapiens
2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
-
 Homo sapiens
2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42338 catalytic subunit beta isoform
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000003
-
 beta isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.0000004
-
 beta isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.0000006
-
 beta isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.000004
-
 delta isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00002
-
 delta isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.000025
-
 delta isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00006
-
 gamma isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00032
-
 alpha isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00032
-
 alpha isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00063
-
 alpha isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00079
-
 gamma isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.0013
-
 gamma isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one