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Literature summary for 1.1.1.146 extracted from
- 11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development (2010), Curr. Med. Chem., 17, 412-422.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine | - |
Homo sapiens |  |
| 1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine | - |
Homo sapiens | |
| 1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one | - |
Homo sapiens | |
| 1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one | - |
Homo sapiens | |
| 2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide | - |
Homo sapiens | |
| 2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide | - |
Mus musculus | |
| 2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one | - |
Homo sapiens | |
| 2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide | - |
Homo sapiens | |
| 2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one | - |
Homo sapiens | |
| 3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide | - |
Homo sapiens | |
| 3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole | - |
Homo sapiens | |
| 3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole | - |
Mus musculus | |
| 3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide | - |
Homo sapiens | |
| 3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine | - |
Homo sapiens | |
| 3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine | - |
Mus musculus | |
| 4-(1-benzofuran-2-ylcarbonyl)-5-(2-fluorophenyl)-3-hydroxy-1-[5-[(4-methylbenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-1,5-dihydro-2H-pyrrol-2-one | - |
Homo sapiens | |
| 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid | - |
Homo sapiens | |
| 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid | - |
Mus musculus | |
| 4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole | - |
Homo sapiens | |
| 4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole | - |
Mus musculus | |
| 4-propyl-N-[2-(thiophen-2-yl)ethyl]benzenesulfonamide | - |
Homo sapiens | |
| 7-hydroxy-2-(2-hydroxyethyl)-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate | - |
Homo sapiens | |
| 7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate | - |
Homo sapiens | |
| carbenoxolone | - |
Homo sapiens | |
| ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate | - |
Homo sapiens | |
| glycyrrhetinic acid | - |
Homo sapiens | |
| gossypol | - |
Homo sapiens | |
| N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide | - |
Homo sapiens | |
| N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide | - |
Mus musculus | |
| N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide | - |
Homo sapiens | |
| N'-[(E)-(5-bromo-2-hydroxyphenyl)methylidene]-2-([5-[(phenylamino)methyl]-4-(prop-2-en-1-yl)-4H-1,2,4-triazol-3-yl]sulfanyl)propanehydrazide | - |
Homo sapiens | |
| N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide | - |
Homo sapiens | |
| N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide | - |
Homo sapiens | |
| N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide | - |
Mus musculus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| adipose tissue | - |
Mus musculus | - |
| adipose tissue | - |
Homo sapiens | - |
| brain | - |
Mus musculus | - |
| brain | - |
Homo sapiens | - |
| liver | - |
Mus musculus | - |
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| cortisone + NADPH + H+ | - |
Mus musculus | cortisol + NADP+ | - |
? | |
| cortisone + NADPH + H+ | - |
Homo sapiens | cortisol + NADP+ | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| 11beta-hydroxysteroid dehydrogenase type 1 | - |
Mus musculus |
| 11beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| additional information | - |
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication | Mus musculus | N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide | |
| additional information | - |
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication | Mus musculus | 2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide | |
| additional information | - |
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication | Mus musculus | N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide | |
| additional information | - |
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication | Mus musculus | 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-(1-benzofuran-2-ylcarbonyl)-5-(2-fluorophenyl)-3-hydroxy-1-[5-[(4-methylbenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-1,5-dihydro-2H-pyrrol-2-one | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide | |
| additional information | - |
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N'-[(E)-(5-bromo-2-hydroxyphenyl)methylidene]-2-([5-[(phenylamino)methyl]-4-(prop-2-en-1-yl)-4H-1,2,4-triazol-3-yl]sulfanyl)propanehydrazide | |
| additional information | - |
IC50 value between 0.0023 to 0.0032 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide | |
| additional information | - |
IC50 value between 0.0023 to 0.0032 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-propyl-N-[2-(thiophen-2-yl)ethyl]benzenesulfonamide | |
| additional information | - |
IC50 value between 0.0023 to 0.0032 mM, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide | |
| 0.000001 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole | |
| 0.0000013 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine | |
| 0.0000014 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | 3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole | |
| 0.000004 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine | |
| 0.0000078 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole | |
| 0.0000135 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | 3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine | |
| 0.000016 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine | |
| 0.000052 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide | |
| 0.000098 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | 4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole | |
| 0.0001 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one | |
| 0.00011 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one | |
| 0.00023 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate | |
| 0.00024 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 7-hydroxy-2-(2-hydroxyethyl)-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate | |
| 0.01 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one | |
| 0.034 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one | |
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