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Literature summary for 1.1.1.146 extracted from

  • Udagawa, S.; Sakami, S.; Takemura, T.; Sato, M.; Arai, T.; Nitta, A.; Aoki, T.; Kawai, K.; Iwamura, T.; Okazaki, S.; Takahashi, T.; Kaino, M.
    Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1 (2013), Bioorg. Med. Chem. Lett., 23, 1617-1621.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one shows excellent stability against cytochrome P450 metabolism Homo sapiens
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one compound is orally active and shows the same tendency as pioglitazone in diet-induced obesity mice Mus musculus
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one methyl substitution at the 8-position achieves an approximately 15fold improvement in potency over the non-substituted compound Homo sapiens
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one compound is orally active and shows the same tendency as pioglitazone in diet-induced obesity mice Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-
Mus musculus P50172
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
0.0000089
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
0.0000098
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
0.000035
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one