Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R)-1,1,1-trifluoro-2-(3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine-1-sulfonyl]phenyl)propan-2-ol | HSD-016 | Homo sapiens | |
(6S)-6-(2-hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-one | BI-135585 | Homo sapiens | |
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine | - |
Homo sapiens | |
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3,4-dicyclopropyl-5-[2-[3-fluoro-5-(trifluoromethyl)thiophen-2-yl]propan-2-yl]-4H-1,2,4-triazole | potent and selective inhibitor for isoform 11beta-HSD1 | Homo sapiens | |
3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3-chloro-2-methyl-N-[4-[2-(3-oxomorpholin-4-yl)ethyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide | BVT-3498 | Homo sapiens | |
3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | - |
Homo sapiens | |
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole | MK-0916 | Homo sapiens | |
3-[[(2-chlorophenyl)methyl]sulfanyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole | - |
Homo sapiens | |
4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole | - |
Homo sapiens | |
4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | - |
Homo sapiens | |
4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine | - |
Homo sapiens | |
5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile | - |
Homo sapiens | |
AMG-221 | - |
Homo sapiens | |
BI-135585 | - |
Homo sapiens | |
BVT-3498 | - |
Homo sapiens | |
HSD-016 | - |
Homo sapiens | |
MK-0916 | - |
Homo sapiens | |
PF-915275 | - |
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+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P28845 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisone + NADPH + H+ | - |
Homo sapiens | cortisol + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
11beta-HSD1 | isoform | Homo sapiens |
11beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000048 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole | |
0.0000079 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | |
0.0000086 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole | |
0.0000087 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | |
0.0000096 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole | |
0.00001 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000011 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000012 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000012 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | |
0.000012 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole | |
0.000013 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000013 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000014 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000014 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | |
0.000014 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole | |
0.000015 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole | |
0.000016 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000019 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000022 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole | |
0.000023 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000024 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole | |
0.000043 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole | |
0.000051 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000051 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000095 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile | |
0.000134 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole | |
0.000343 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine | |
0.000591 | - |
isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine | |
0.003 | - |
IC50 above 0.003 mM, isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine | |
0.003 | - |
IC50 above 0.003 mM, isoform 11beta-HSD1, at pH 6.6 and 25°C | Homo sapiens | 4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole |