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Literature summary for 1.1.1.146 extracted from

  • Sun, D.; Wang, Z.; Di, Y.; Jaen, J.C.; Labelle, M.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tomooka, C.S.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
    Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) (2008), Bioorg. Med. Chem. Lett., 18, 3513-3516.
    View publication on PubMed

Application

Application Comment Organism
analysis high-throughput screening for potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I Mus musculus
analysis high-throughput screening for potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine
-
Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
11 beta-hydroxysteroid dehydrogenase type 1
-
Mus musculus
-
11beta-hydroxysteroid dehydrogenase type 1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1,2-dehydrocortisone + NADPH
-
Mus musculus 1,2-dehydrocortisol + NADP+
-
?
1,2-dehydrocortisone + NADPH
-
Homo sapiens 1,2-dehydrocortisol + NADP+
-
?
cortisone + NADPH + H+
-
Homo sapiens cortisol + NADP+
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane
0.000003
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine
0.000004
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.000007
-
pH and temperature not specified in the publication Homo sapiens 1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.000009
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.000009
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.00001
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.000011
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.000013
-
pH and temperature not specified in the publication Homo sapiens 1-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.000016
-
pH and temperature not specified in the publication Homo sapiens 1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine