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Literature summary for 1.1.1.146 extracted from

  • Webster, S.P.; Binnie, M.; McConnell, K.M.; Sooy, K.; Ward, P.; Greaney, M.F.; Vinter, A.; Pallin, T.D.; Dyke, H.J.; Gill, M.I.; Warner, I.; Seckl, J.R.; Walker, B.R.
    Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles (2010), Bioorg. Med. Chem. Lett., 20, 3265-3271.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
-
Mus musculus
expression in HEK-293 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone poor stability in liver microsomes Homo sapiens
1-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone poor stability in liver microsomes Homo sapiens
3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one moderate stability in liver microsomes Homo sapiens
3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one displays good levels of inhibition in liver, subcutaneous adipose tissue and brain following an oral dose Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-
Mus musculus P50172
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000114
-
pH 7.0, 22°C, cellular assay Homo sapiens 3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one
0.000116
-
pH 7.0, 22°C, cellular assay Homo sapiens 1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
0.000257
-
pH 7.0, 22°C, cellular assay Homo sapiens 1-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone