Cloned (Comment) | Organism |
---|---|
the 11beta-HSD1 enzyme is expressed in Escherichia coli | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
11beta-HSD1 (24-292) C272S mutant, hanging drop vapour diffusion method, using 25% (w/v) PEG 3350, 0.2 M ammonium acetate, and 0.1 M sodium citrate buffer (pH 5.6) | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(+/-)-2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(1-adamantylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(1-adamantylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(cycloheptylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(cycloheptylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(cyclohexylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(cyclohexylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(cyclooctylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-ethyl-5-methyl-2-(1-norbornylamino)-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-ethyl-5-methyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-ethyl-5-methyl-2-(7-norbornylamino)-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-ethyl-5-methyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-methyl-2-(1-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-methyl-2-(3-noradamantylamino)-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-methyl-2-(7-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
(+/-)-5-methyl-5-propyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
2-(1-adamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
2-(1-adamantylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
2-(3-noradamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
2-(cyclooctylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens | |
5,5-diethyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one | inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P28845 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisone + NADPH + H+ | - |
Homo sapiens | cortisol + NADP+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
11beta-HSD1 | - |
Homo sapiens |
11beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADP+ | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000003 | - |
2-(3-noradamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000012 | - |
(+/-)-5-methyl-2-(3-noradamantylamino)-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000013 | - |
(+/-)-5-ethyl-5-methyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000013 | - |
5,5-diethyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000014 | - |
2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | pH and temperature not specified in the publication | Homo sapiens | |
0.00002 | - |
2-(1-adamantylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000024 | - |
(+/-)-2-(1-adamantylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000024 | - |
(+/-)-2-(1-adamantylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000025 | - |
(+/-)-5-methyl-2-(1-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000026 | - |
2-(cyclooctylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000028 | - |
(+/-)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000028 | - |
2-(1-adamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000032 | - |
(+/-)-2-(cycloheptylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000034 | - |
(+/-)-2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000038 | - |
(+/-)-5-methyl-5-propyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000047 | - |
(+/-)-2-(cyclooctylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000055 | - |
(+/-)-2-(cyclohexylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000058 | - |
(+/-)-5-ethyl-5-methyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000064 | - |
(+/-)-2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000073 | - |
(+/-)-5-ethyl-5-methyl-2-(1-norbornylamino)-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000082 | - |
(+/-)-2-(cycloheptylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000126 | - |
(+/-)-2-(cyclohexylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000149 | - |
(+/-)-5-methyl-2-(7-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens | |
0.000372 | - |
(+/-)-5-ethyl-5-methyl-2-(7-norbornylamino)-1,3-thiazol-4-(5H)-one | pH and temperature not specified in the publication | Homo sapiens |