Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,6,7-trimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 30.88% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2,6-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 17.65% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2,7-dimethyl-6-nitro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-(bromomethyl)-6,7-dimethyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 33.82% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-(bromomethyl)-7-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-(bromomethyl)-7-methyl-6-nitro-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-(iodomethyl)-2,3,6,7,8,9-hexahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one | 27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-(iodomethyl)-2,3,7,8,9,10-hexahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one | 23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-(iodomethyl)-6-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 29.41% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-methyl-6,7,8,9-tetrahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one | 13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
2-methyl-7,8,9,10-tetrahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one | 14.71% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
6-bromo-2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
6-bromo-2-(bromomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 25% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
6-bromo-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one | selective inhibitor for isoform 11beta-HSD1, 59.15% inhibition of isoform 11beta-HSD1 at 0.01 mM, 4.74% inhibition of isoform 11beta-HSD2 at 0.01 mM | Homo sapiens | |
7-(cyclohexylmethyl)-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
7-ethyl-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
7-ethyl-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one | 23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens | |
carbenoxolone | 89.7% inhibition of isoform 11beta-HSD1 at 0.01 mM | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisone + NADPH + H+ | Homo sapiens | - |
cortisol + NADP+ | - |
ir |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P28845 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
adipose tissue | - |
Homo sapiens | - |
brain | - |
Homo sapiens | - |
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisone + NADPH + H+ | - |
Homo sapiens | cortisol + NADP+ | - |
ir |
Synonyms | Comment | Organism |
---|---|---|
11beta-HSD1 | isoform | Homo sapiens |
11beta-hydroxysteroid dehydrogenase | - |
Homo sapiens |
11beta-hydroxysteroid type 1 dehydrogenase | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | dependent on | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0069 | - |
isoform 11beta-HSD1, at pH 7.4 and 37°C | Homo sapiens | 7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one |