Literature summary for 1.1.1.146 extracted from

Sun, D.; Wang, Z.; Cardozo, M.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Jaen, J.C.; Labelle, M.; Liu, J.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) (2009), Bioorg. Med. Chem. Lett., 19, 1522-1527.

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Cloned(Commentary)

Cloned (Comment)	Organism
Baculovirus-produced recombinant protein	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine	-	Homo sapiens
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine	-	Homo sapiens
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine	-	Homo sapiens
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine	-	Homo sapiens
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine	-	Homo sapiens
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine	-	Homo sapiens
(2R)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine	-	Homo sapiens
(2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine	-	Homo sapiens
(2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine	-	Homo sapiens
(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine	-	Homo sapiens
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol	-	Homo sapiens
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol	-	Homo sapiens
1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine	-	Homo sapiens
1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol	-	Homo sapiens
1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide	-	Homo sapiens
1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide	-	Homo sapiens
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide	-	Homo sapiens
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide	-	Homo sapiens
2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol	-	Homo sapiens
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol	-	Homo sapiens
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol	-	Homo sapiens
4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide	-	Homo sapiens
4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline	-	Homo sapiens
4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine	-	Homo sapiens
[1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
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

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.0000004	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
0.0000005	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
0.0000005	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
0.0000006	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
0.0000006	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
0.0000007	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
0.0000008	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
0.0000009	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
0.000001	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine
0.0000011	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
0.0000012	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide
0.0000013	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
0.0000017	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide
0.0000022	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
0.000003	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine
0.000003	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide
0.0000034	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine
0.000004	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine
0.000004	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	[1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol
0.000005	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
0.0000053	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
0.0000073	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline
0.0000079	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
0.000008	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine
0.00001	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine
0.00001	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
0.0000113	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine
0.000012	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol
0.000016	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
0.00003	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
0.000036	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
0.000094	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine