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Literature summary for 1.1.1.146 extracted from

  • Xu, Z.; Tice, C.M.; Zhao, W.; Cacatian, S.; Ye, Y.J.; Singh, S.B.; Lindblom, P.; McKeever, B.M.; Krosky, P.M.; Kruk, B.A.; Berbaum, J.; Harrison, R.K.; Johnson, J.A.; Bukhtiyarov, Y.; Panemangalore, R.; Scott, B.B.; Zhao, Y.; Bruno, J.G.; Togias, J.; Guo, J.; Guo, R.; Carroll, P.J.; McGeehan, G.M.; Zhuang, L. et al.
    Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (2011), J. Med. Chem., 54, 6050-6062.
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
expression in CHO cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(2',4'-difluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one displays more than 1000fold selectivity for isoform 11beta-HSD1 over three related hydroxysteroid dehydrogenases, three CYP isozymes, hERG, and three nuclear receptors. When dosed orally at 30 mg/kg to mice, compound is distributed into adipose and liver Homo sapiens
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000005
-
 pH 7.4, 22°C, microsomal assay Homo sapiens (6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
0.0000008
-
 pH 7.4, 22°C, microsomal assay Homo sapiens (6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(2',4'-difluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one