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Literature summary for 1.1.1.146 extracted from

  • Kim, S.H.; Ramu, R.; Kwon, S.W.; Lee, S.H.; Kim, C.H.; Kang, S.K.; Rhee, S.D.; Bae, M.A.; Ahn, S.H.; Ha, D.C.; Cheon, H.G.; Kim, K.Y.; Ahn, J.H.
    Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 1065-1069.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
Homo sapiens
(4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
Homo sapiens
(4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
Homo sapiens
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone
-
Homo sapiens
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone
-
Homo sapiens
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
-
Homo sapiens
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
-
Mus musculus
2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone
-
Homo sapiens
3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
-
Homo sapiens
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid
-
Homo sapiens
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
-
Homo sapiens
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
-
Mus musculus
carbenoxolone
-
Homo sapiens
ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
-
Homo sapiens
ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
-
Homo sapiens
methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate
-
Homo sapiens
[4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum
-
Mus musculus 5783
-
endoplasmic reticulum
-
Homo sapiens 5783
-

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisone + NADPH + H+
-
Mus musculus cortisol + NADP+
-
?
cortisone + NADPH + H+
-
Homo sapiens cortisol + NADP+
-
?

Synonyms

Synonyms Comment Organism
11beta-hydroxysteroid dehydrogenase 1
-
Mus musculus
11beta-hydroxysteroid dehydrogenase 1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000028
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone
0.00003
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone
0.000031
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
0.000031
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate
0.00004
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
0.000234
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens [4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone
0.000254
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
0.000388
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
0.0005
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens carbenoxolone
0.000547
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone
0.00072
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid
0.00074
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
0.003
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
0.0045
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
0.0078
-
pH not specified in the publication, temperature not specified in the publication Mus musculus 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
0.009
-
pH not specified in the publication, temperature not specified in the publication Mus musculus 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
0.0148
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone