EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
1.1.1.146 | 2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one | 38.03% inhibition of isoform 11beta-HSD1 at 0.01 mM, 22.6% inhibition of isoform 11beta-HSD2 at 0.01 mM | Homo sapiens | |
1.1.1.146 | 2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one | 71.27% inhibition of isoform 11beta-HSD1 at 0.01 mM, 23.97% inhibition of isoform 11beta-HSD2 at 0.01 mM | Homo sapiens | |
1.1.1.146 | 2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one | 13.46% inhibition of isoform 11beta-HSD1 at 0.01 mM, 1.34% inhibition of isoform 11beta-HSD2 at 0.01 mM | Homo sapiens | |
1.1.1.146 | additional information | not inhibited by 2-(allylamino)thiazol-4(5H)-one, 2-(allylamino)-5-methylthiazol-4(5H)-one, 2-(allylamino)-5-ethylthiazol-4(5H)-one, 2-(allylamino)-5-propylthiazol-4(5H)-one, 2-(allylamino)-5-isopropylthiazol-4(5H)-one, 2-(allylamino)-5,5-dimethylthiazol-4(5H)-one, and 2-(allylamino)-5-phenylthiazol-4(5H)-one | Homo sapiens |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.1.1.146 | cortisone + NADPH + H+ | Homo sapiens | - |
cortisol + NADP+ | - |
ir |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
1.1.1.146 | Homo sapiens | P28845 | - |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
1.1.1.146 | adipose tissue | - |
Homo sapiens | - |
1.1.1.146 | brain | - |
Homo sapiens | - |
1.1.1.146 | liver | - |
Homo sapiens | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.1.1.146 | cortisone + NADPH + H+ | - |
Homo sapiens | cortisol + NADP+ | - |
ir |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
1.1.1.146 | 11beta-HSD1 | isoform | Homo sapiens |
1.1.1.146 | 11beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
1.1.1.146 | 0.0025 | - |
isoform 11beta-HSD1, at pH 7.4 and 37°C | Homo sapiens | 2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one | |
1.1.1.146 | 0.036 | - |
isoform 11beta-HSD1, at pH 7.4 and 37°C | Homo sapiens | 2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one | |
1.1.1.146 | 0.05 | - |
IC50 above 0.05 mM, isoform 11beta-HSD1, at pH 7.4 and 37°C | Homo sapiens | 2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one |