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Literature summary extracted from

  • Siu, M.; Johnson, T.O.; Wang, Y.; Nair, S.K.; Taylor, W.D.; Cripps, S.J.; Matthews, J.J.; Edwards, M.P.; Pauly, T.A.; Ermolieff, J.; Castro, A.; Hosea, N.A.; LaPaglia, A.; Fanjul, A.N.; Vogel, J.E.
    N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275 (2009), Bioorg. Med. Chem. Lett., 19, 3493-3497.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 (6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)acetic acid
-
 Homo sapiens
1.1.1.146 2-(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)-N,N-diethylacetamide
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-[6-(2-morpholin-4-yl-2-oxoethyl)-pyridin-2-yl]-benzenesulfonamide
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
 Homo sapiens
1.1.1.146 4'-chloro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-cyano-N-(6-cyclopropylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-cyano-N-(6-ethylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-cyano-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-cyano-N-[6-(ethylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-cyano-N-[6-(methylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-cyano-N-[6-(propan-2-yl)pyridin-2-yl]biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-fluoro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4'-methyl-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 4-methoxy-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
 Homo sapiens
1.1.1.146 4-tert-butyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
 Homo sapiens
1.1.1.146 N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 N-(6-methylpyridin-2-yl)-2-(trifluoromethyl)benzenesulfonamide
-
 Homo sapiens
1.1.1.146 N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide
-
 Homo sapiens
1.1.1.146 N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
 Homo sapiens
1.1.1.146 N-(6-methylpyridin-2-yl)naphthalene-1-sulfonamide
-
 Homo sapiens
1.1.1.146 N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide
-
 Homo sapiens
1.1.1.146 N-[6-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]-3-chloro-2-methylbenzenesulfonamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.146 adipose tissue
-
 Homo sapiens
-
1.1.1.146 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.146 additional information
-
 N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide Ki below 0.000001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.0000017
-
 4'-cyano-N-[6-(propan-2-yl)pyridin-2-yl]biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.0000019
-
 4'-cyano-N-(6-cyclopropylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000004
-
 4'-cyano-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.0000048
-
 4'-cyano-N-[6-(ethylamino)pyridin-2-yl]biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.0000058
-
 4'-chloro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.0000066
-
 4'-cyano-N-(6-ethylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.0000098
-
 4'-cyano-N-[6-(methylamino)pyridin-2-yl]biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.00002
-
 4'-fluoro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000048
-
 N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000062
-
 4'-methyl-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000084
-
 N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000108
-
 N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000169
-
 3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000169
-
 3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide pH not specified in the publication, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000287
-
 2-(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)-N,N-diethylacetamide pH not specified in the publication, temperature not specified in the publication Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 additional information
-
 1% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(6-methylpyridin-2-yl)-2-(trifluoromethyl)benzenesulfonamide
1.1.1.146 additional information
-
 10% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(6-methylpyridin-2-yl)naphthalene-1-sulfonamide
1.1.1.146 additional information
-
 11% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
1.1.1.146 additional information
-
 22% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[6-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]-3-chloro-2-methylbenzenesulfonamide
1.1.1.146 additional information
-
 23% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-methoxy-N-(6-methylpyridin-2-yl)benzenesulfonamide
1.1.1.146 additional information
-
 25% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens (6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)acetic acid
1.1.1.146 additional information
-
 32% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-tert-butyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
1.1.1.146 additional information
-
 39% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide
1.1.1.146 additional information
-
 6% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-chloro-2-methyl-N-[6-(2-morpholin-4-yl-2-oxoethyl)-pyridin-2-yl]-benzenesulfonamide
1.1.1.146 additional information
-
 8% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide