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Literature summary extracted from

  • Koike, T.; Shiraki, R.; Sasuga, D.; Hosaka, M.; Kawano, T.; Fukudome, H.; Kurosawa, K.; Moritomo, A.; Mimasu, S.; Ishii, H.; Yoshimura, S.
    Discovery and biological evaluation of potent and orally active human 11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes mellitus (2019), Chem. Pharm. Bull., 67, 824-838 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 (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
1.1.1.146 (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
1.1.1.146 2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine
-
 Homo sapiens
1.1.1.146 2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
-
 Homo sapiens
1.1.1.146 3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 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
1.1.1.146 3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-chloro-2-methyl-N-[4-[2-(3-oxomorpholin-4-yl)ethyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide BVT-3498 Homo sapiens
1.1.1.146 3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole MK-0916 Homo sapiens
1.1.1.146 3-[[(2-chlorophenyl)methyl]sulfanyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
 Homo sapiens
1.1.1.146 4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
-
 Homo sapiens
1.1.1.146 5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile
-
 Homo sapiens
1.1.1.146 AMG-221
-
 Homo sapiens
1.1.1.146 BI-135585
-
 Homo sapiens
1.1.1.146 BVT-3498
-
 Homo sapiens
1.1.1.146 HSD-016
-
 Homo sapiens
1.1.1.146 MK-0916
-
 Homo sapiens
1.1.1.146 PF-915275
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.146 microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

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+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens P28845
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.146 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+
-
 Homo sapiens cortisol + NADP+
-
 ?

Synonyms

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

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.146 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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
1.1.1.146 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