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Literature summary extracted from

  • Olson, S.; Aster, S.D.; Brown, K.; Carbin, L.; Graham, D.W.; Hermanowski-Vosatka, A.; LeGrand, C.B.; Mundt, S.S.; Robbins, M.A.; Schaeffer, J.M.; Slossberg, L.H.; Szymonifka, M.J.; Thieringer, R.; Wright, S.D.; Balkovec, J.M.
    Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (2005), Bioorg. Med. Chem. Lett., 15, 4359-4362.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.B40 3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.B40 3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.B40 3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.B40 3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.B40 3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM Homo sapiens
1.1.1.B40 3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM Mus musculus
1.1.1.B40 3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM Homo sapiens
1.1.1.B40 3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM Mus musculus
1.1.1.B40 3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.B40 3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.B40 3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.B40 3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.B40 3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM Homo sapiens
1.1.1.B40 3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM Mus musculus
1.1.1.B40 3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.B40 3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.B40 3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM Homo sapiens
1.1.1.B40 3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine isozyme 11beta-HSD1 IC50: 98 nM, isozyme 11beta-HSD2 IC50: above 0.01 mM Mus musculus
1.1.1.B40 3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.B40 3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.B40 adamantyl triazoles eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview Homo sapiens
1.1.1.B40 adamantyl triazoles eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview Mus musculus
1.1.1.B40 n-alkyl-substituted adamantyl triazoles substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview Homo sapiens
1.1.1.B40 n-alkyl-substituted adamantyl triazoles substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview Mus musculus
1.1.1.146 3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.146 3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.146 3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.146 3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.146 3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM Homo sapiens
1.1.1.146 3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM Mus musculus
1.1.1.146 3-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 118 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 104 nM, 11betaHSD1; IC50: above 10000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 50 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM Homo sapiens
1.1.1.146 3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM Mus musculus
1.1.1.146 3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 292 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.146 3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.146 3-(3-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 417 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.146 3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.146 3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 1674 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 365 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM Homo sapiens
1.1.1.146 3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM Mus musculus
1.1.1.146 3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.146 3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.146 3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM Homo sapiens
1.1.1.146 3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine isozyme 11beta-HSD1 IC50: 98 nM, isozyme 11beta-HSD2 IC50: above 0.01 mM Mus musculus
1.1.1.146 3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Homo sapiens
1.1.1.146 3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM Mus musculus
1.1.1.146 3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 35 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine IC50: 9.2 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine IC50: 4.6 nM, 11betaHSD1; IC50: about 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine IC50: 16 nM, 11betaHSD1; IC50: about 10000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine IC50: 1112 nM, 11betaHSD1; IC50: above 10000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine IC50: 11650 nM, 11betaHSD2; IC50: 2.2 nM, 11betaHSD1 Mus musculus
1.1.1.146 3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine IC50: 4563 nM, 11betaHSD2; IC50: 8 nM, 11betaHSD1 Mus musculus
1.1.1.146 3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine IC50: 98 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole IC50: 10000 nM, 11betaHSD2; IC50: 6820 nM, 11betaHSD1 Mus musculus
1.1.1.146 3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine IC50: 587 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole IC50: 14 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole IC50: 91 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole IC50: 23 nM, 11betaHSD1; IC50: 50 nM, 11betaHSD2 Mus musculus
1.1.1.146 5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole IC50: 270 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole IC50: 109 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole IC50: 50 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 Mus musculus
1.1.1.146 adamantyl triazoles eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview Homo sapiens
1.1.1.146 adamantyl triazoles eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview Mus musculus
1.1.1.146 n-alkyl-substituted adamantyl triazoles substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview Homo sapiens
1.1.1.146 n-alkyl-substituted adamantyl triazoles substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview Mus musculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.146 endoplasmic reticulum associated, isozyme 11beta-HSD1 Homo sapiens 5783
-
1.1.1.146 endoplasmic reticulum associated, isozyme 11beta-HSD1 Mus musculus 5783
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.B40 cortisol + NAD+ Homo sapiens isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ cortisone + NADH
-
 ir
1.1.1.B40 cortisol + NAD+ Mus musculus isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ cortisone + NADH
-
 ir
1.1.1.146 cortisol + NAD+ Mus musculus isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ cortisone + NADH
-
 ir
1.1.1.146 cortisone + NADPH + H+ Homo sapiens isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH cortisol + NADP+
-
 ir
1.1.1.146 cortisone + NADPH + H+ Mus musculus isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH cortisol + NADP+
-
 ir

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.B40 Homo sapiens P80365 isozymes 11beta-HSD1 and 11beta-HSD2
-
1.1.1.B40 Mus musculus P51661 isozymes 11beta-HSD1 and 11beta-HSD2
-
1.1.1.146 Homo sapiens
-
 isozymes 11beta-HSD1 and 11beta-HSD2
-
1.1.1.146 Mus musculus P50172 isozymes 11beta-HSD1 and 11beta-HSD2
-
1.1.1.146 Mus musculus P50172 isozyme 11beta-HSD1; isozyme 11beta-HSD1
-
1.1.1.146 Mus musculus P51661 isozyme 11beta-HSD2; isozyme 11beta-HSD2
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.B40 cortisol + NAD+ isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ Homo sapiens cortisone + NADH
-
 ir
1.1.1.B40 cortisol + NAD+ isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ Mus musculus cortisone + NADH
-
 ir
1.1.1.146 cortisol + NAD+ isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+ Mus musculus cortisone + NADH
-
 ir
1.1.1.146 cortisone + NADPH + H+ isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH Homo sapiens cortisol + NADP+
-
 ir
1.1.1.146 cortisone + NADPH + H+ isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH Mus musculus cortisol + NADP+
-
 ir

Synonyms

EC Number Synonyms Comment Organism
1.1.1.B40 11beta-HSD2
-
 Homo sapiens
1.1.1.B40 11beta-HSD2
-
 Mus musculus
1.1.1.146 11beta-HSD1
-
 Homo sapiens
1.1.1.146 11beta-HSD1
-
 Mus musculus
1.1.1.146 11beta-HSD2
-
 Mus musculus
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 1
-
 Mus musculus
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 2
-
 Mus musculus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.146 NAD+ 11beta-HSD2 Mus musculus
1.1.1.146 NADPH 11beta-HSD1 Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 0.0000022
-
 IC50: 2.2 nM, 11betaHSD1 Mus musculus 3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine
1.1.1.146 0.0000046
-
 IC50: 4.6 nM, 11betaHSD1 Mus musculus 3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
1.1.1.146 0.000008
-
 IC50: 8 nM, 11betaHSD1 Mus musculus 3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
1.1.1.146 0.0000092
-
 IC50: 9.2 nM, 11betaHSD1 Mus musculus 3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
1.1.1.146 0.000014
-
 IC50: 14 nM, 11betaHSD1 Mus musculus 5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
1.1.1.146 0.000016
-
 IC50: 16 nM, 11betaHSD1 Mus musculus 3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
1.1.1.146 0.000023
-
 IC50: 23 nM, 11betaHSD1 Mus musculus 5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
1.1.1.146 0.000035
-
 IC50: 35 nM, 11betaHSD1 Mus musculus 3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.00005
-
 IC50: 50 nM, 11betaHSD1 Mus musculus 3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.00005
-
 IC50: 50 nM, 11betaHSD1 Mus musculus 5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
1.1.1.146 0.00005
-
 IC50: 50 nM, 11betaHSD2 Mus musculus 5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
1.1.1.146 0.000091
-
 IC50: 91 nM, 11betaHSD1 Mus musculus 5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
1.1.1.146 0.000098
-
 IC50: 98 nM, 11betaHSD1 Mus musculus 3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.000104
-
 IC50: 104 nM, 11betaHSD1 Mus musculus 3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.000109
-
 IC50: 109 nM, 11betaHSD1 Mus musculus 5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
1.1.1.146 0.000118
-
 IC50: 118 nM, 11betaHSD1 Mus musculus 3-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.00027
-
 IC50: 270 nM, 11betaHSD1 Mus musculus 5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
1.1.1.146 0.000292
-
 IC50: 292 nM, 11betaHSD1 Mus musculus 3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.000365
-
 IC50: 365 nM, 11betaHSD1 Mus musculus 3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.000417
-
 IC50: 417 nM, 11betaHSD1 Mus musculus 3-(3-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.000587
-
 IC50: 587 nM, 11betaHSD1 Mus musculus 3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
1.1.1.146 0.001112
-
 IC50: 1112 nM, 11betaHSD1 Mus musculus 3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
1.1.1.146 0.001674
-
 IC50: 1674 nM, 11betaHSD1 Mus musculus 3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: about 4000 nM, 11betaHSD2 Mus musculus 3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-(3-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
1.1.1.146 0.004
-
 IC50: above 4000 nM, 11betaHSD2 Mus musculus 5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
1.1.1.146 0.004563
-
 IC50: 4563 nM, 11betaHSD2 Mus musculus 3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
1.1.1.146 0.00682
-
 IC50: 6820 nM, 11betaHSD1 Mus musculus 3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
1.1.1.146 0.01
-
 IC50: 10000 nM, 11betaHSD2 Mus musculus 3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
1.1.1.146 0.01
-
 IC50: about 10000 nM, 11betaHSD2 Mus musculus 3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
1.1.1.146 0.01
-
 IC50: above 10000 nM, 11betaHSD2 Mus musculus 3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
1.1.1.146 0.01
-
 IC50: above 10000 nM, 11betaHSD2 Mus musculus 3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
1.1.1.146 0.01165
-
 IC50: 11650 nM, 11betaHSD2 Mus musculus 3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine