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Literature summary for 1.1.1.146 extracted from

  • Hofer, S.; Kratschmar, D.V.; Schernthanner, B.; Vuorinen, A.; Schuster, D.; Odermatt, A.; Easmon, J.
    Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11beta-hydroxysteroid dehydrogenase 1 inhibitors (2013), Bioorg. Med. Chem. Lett., 23, 5397-5400.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3beta,18alpha)-3-hydroxy-11-oxoolean-12-en-30-oate
-
Homo sapiens
1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
-
Homo sapiens
2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
Homo sapiens
2-[4-(3-methylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzothiazole 89% residual activity at 0.02 mM Homo sapiens
2-[4-(3-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzoxazole 18% residual activity at 0.02 mM Homo sapiens
2-[4-(3-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole 60% residual activity at 0.02 mM Homo sapiens
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole 75% residual activity at 0.02 mM Homo sapiens
2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
Homo sapiens
2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
-
Homo sapiens
2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole
-
Homo sapiens
2-[4-(4-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole 90% residual activity at 0.02 mM Homo sapiens
2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
Homo sapiens
3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide
-
Homo sapiens
4-[4-(1-methyl-1H-benzimidazol-2-yl)piperazine-1-sulfonyl]benzoic acid 90% residual activity at 0.02 mM Homo sapiens
Merck-544
-
Homo sapiens
[4-(1H-benzimidazol-2-yl)piperazin-1-yl](4-methylphenyl)methanone 65% residual activity at 0.02 mM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADPH + H+ Homo sapiens
-
cortisol + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
11beta-HSD1
-
Homo sapiens
11beta-hydroxysteroid dehydrogenase 1
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0007
-
pH and temperature not specified in the publication Homo sapiens 1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
0.0042
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
0.0048
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole
0.0064
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
0.0185
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
0.02
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
0.0272
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole