Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Homo sapiens | |
3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Mus musculus | |
3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Homo sapiens | |
3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Mus musculus | |
3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM | Homo sapiens | |
3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM | Mus musculus | |
3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM | Homo sapiens | |
3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM | Mus musculus | |
3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Homo sapiens | |
3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Mus musculus | |
3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Homo sapiens | |
3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Mus musculus | |
3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM | Homo sapiens | |
3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM | Mus musculus | |
3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol | isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Homo sapiens | |
3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol | isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Mus musculus | |
3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine | isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM | Homo sapiens | |
3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine | isozyme 11beta-HSD1 IC50: 98 nM, isozyme 11beta-HSD2 IC50: above 0.01 mM | Mus musculus | |
3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Homo sapiens | |
3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM | Mus musculus | |
adamantyl triazoles | eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview | Homo sapiens | |
adamantyl triazoles | eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview | Mus musculus | |
n-alkyl-substituted adamantyl triazoles | substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview | Homo sapiens | |
n-alkyl-substituted adamantyl triazoles | substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview | Mus musculus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisol + NAD+ | Homo sapiens | isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ | cortisone + NADH | - |
ir | |
cortisol + NAD+ | Mus musculus | isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ | cortisone + NADH | - |
ir |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P80365 | isozymes 11beta-HSD1 and 11beta-HSD2 | - |
Mus musculus | P51661 | isozymes 11beta-HSD1 and 11beta-HSD2 | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisol + NAD+ | isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ | Homo sapiens | cortisone + NADH | - |
ir | |
cortisol + NAD+ | isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ | Mus musculus | cortisone + NADH | - |
ir |
Synonyms | Comment | Organism |
---|---|---|
11beta-HSD2 | - |
Homo sapiens |
11beta-HSD2 | - |
Mus musculus |