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Literature summary for 1.1.1.146 extracted from

  • Ye, X.Y.; Chen, S.Y.; Nayeem, A.; Golla, R.; Seethala, R.; Wang, M.; Harper, T.; Sleczka, B.G.; Li, Y.X.; He, B.; Kirby, M.; Gordon, D.A.; Robl, J.A.
    Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1) (2011), Bioorg. Med. Chem. Lett., 21, 6699-6704.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid lead compound for high throughput screening of inhibitors. A hydrophobic group at C-2 position dramatically enhances potency Homo sapiens
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
-
 Mus musculus
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid good in vitro potency for the human enzyme while exhibiting enhanced metabolic stability in liver microsomes compared to lead compound [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid Homo sapiens
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
-
 Mus musculus
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
-
 Homo sapiens
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
-
 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 [9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
0.000012
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
0.000013
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens [5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
0.00012
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
0.000184
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus [9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
0.001616
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus [5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid