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Literature summary for 1.1.1.146 extracted from

  • Zhang, X.; Zhou, Y.; Shen, Y.; Du, L.L.; Chen, J.H.; Leng, Y.; Shen, J.H.
    Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro (2009), Acta Pharmacol. Sin., 30, 1344-1350.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.1.1.146

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293 cell Homo sapiens
expressed in HEK-293 cell Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
-
 Homo sapiens
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
-
 Mus musculus
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
-
 Homo sapiens
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
-
 Mus musculus
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
-
 Homo sapiens
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
-
 Mus musculus
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
 Homo sapiens
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
 Mus musculus
3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
 Homo sapiens
3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
 Mus musculus
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
 Homo sapiens
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
 Mus musculus
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
 Homo sapiens
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
 Mus musculus
3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
 Homo sapiens
3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
 Mus musculus
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
 Homo sapiens
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
 Mus musculus
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
 Homo sapiens
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
 Mus musculus
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
-
 Homo sapiens
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
-
 Mus musculus
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
-
 Homo sapiens
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
-
 Mus musculus
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
-
 Homo sapiens
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
-
 Mus musculus
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
 Homo sapiens
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
 Mus musculus
N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
 Homo sapiens
N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
 Mus musculus
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
 Homo sapiens
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
 Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-
Mus musculus P50172
-
-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 18.94% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
additional information
-
 18.95% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
additional information
-
 21.8% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
additional information
-
 22.82% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
additional information
-
 27.21% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
additional information
-
 27.68% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
additional information
-
 28.0% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
additional information
-
 28.08% inhibition at 0.001 mM Homo sapiens 3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
additional information
-
 30.88% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
additional information
-
 31.44% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
additional information
-
 32.05% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
additional information
-
 35.31% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
additional information
-
 36.61% inhibition at 0.001 mM, pH 7.4, 37°C Homo sapiens 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
additional information
-
 40.43% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
additional information
-
 40.43% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
additional information
-
 8.42% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
additional information
-
 8.49% inhibition at 0.001 mM, pH 7.4, 37°C Mus musculus 3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
0.000006
-
 pH 7.4, 37°C Homo sapiens 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
0.000024
-
 pH 7.4, 37°C Mus musculus N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
0.000045
-
 pH 7.4, 37°C Mus musculus 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
0.000057
-
 pH 7.4, 37°C Homo sapiens 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
0.000078
-
 pH 7.4, 37°C Homo sapiens 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
0.00008
-
 pH 7.4, 37°C Mus musculus 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
0.000084
-
 pH 7.4, 37°C Homo sapiens N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
0.000143
-
 pH 7.4, 37°C Homo sapiens N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
0.00021
-
 pH 7.4, 37°C Mus musculus N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
0.000222
-
 pH 7.4, 37°C Homo sapiens 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
0.000279
-
 pH 7.4, 37°C Mus musculus 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
0.000307
-
 pH 7.4, 37°C Mus musculus 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
0.000375
-
 pH 7.4, 37°C Homo sapiens 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
0.000849
-
 pH 7.4, 37°C Mus musculus 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
0.001055
-
 pH 7.4, 37°C Mus musculus 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide