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Literature summary for 2.3.1.16 extracted from

  • Nagase, T.; Takahashi, T.; Sasaki, T.; Nagumo, A.; Shimamura, K.; Miyamoto, Y.; Kitazawa, H.; Kanesaka, M.; Yoshimoto, R.; Aragane, K.; Tokita, S.; Sato, N.
    Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors (2009), J. Med. Chem., 52, 4111-4114.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-(phenylsulfonyl)-N-[4-(propan-2-yl)phenyl]-8-azabicyclo[3.2.1]octane-8-carboxamide
-
Homo sapiens
N-(4-methylphenyl)-3-(phenylsulfonyl)-8-azabicyclo[3.2.1]octane-8-carboxamide lead compound Homo sapiens
N-[4-(1,1-difluoroethyl)phenyl]-3-(phenylsulfonyl)-8-azabicyclo[3.2.1]octane-8-carboxamide
-
Homo sapiens
N-[4-(1,1-difluoroethyl)phenyl]-3-(pyridin-2-ylsulfonyl)-8-azabicyclo[3.2.1]octane-8-carboxamide excellent selectivity over the other human ELOVL subtypes, with IC50 above 5 microM for ELOVL1, -2, -3, and -5, selective against the hERG K+ channel Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
Elovl6
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000032
-
-
Homo sapiens 3-(phenylsulfonyl)-N-[4-(propan-2-yl)phenyl]-8-azabicyclo[3.2.1]octane-8-carboxamide
0.000078
-
-
Homo sapiens N-[4-(1,1-difluoroethyl)phenyl]-3-(phenylsulfonyl)-8-azabicyclo[3.2.1]octane-8-carboxamide
0.000079
-
-
Homo sapiens N-[4-(1,1-difluoroethyl)phenyl]-3-(pyridin-2-ylsulfonyl)-8-azabicyclo[3.2.1]octane-8-carboxamide
0.00175
-
-
Homo sapiens N-(4-methylphenyl)-3-(phenylsulfonyl)-8-azabicyclo[3.2.1]octane-8-carboxamide