Literature summary for 1.1.1.146 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.

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Inhibitors

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
adipose tissue	-	Homo sapiens	-
liver	-	Homo sapiens	-

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-hydroxysteroid dehydrogenase type 1	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
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
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
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
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
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
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
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
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
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
0.000048	-	N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide	pH not specified in the publication, temperature not specified in the publication	Homo sapiens
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
0.000084	-	N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide	pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.000108	-	N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide	pH not specified in the publication, temperature not specified in the publication	Homo sapiens
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
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
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

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
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
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
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
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
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
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
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
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
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
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