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Literature summary for 2.3.1.16 extracted from

  • Sasaki, T.; Nagase, T.; Takahashi, T.; Nagumo, A.; Shimamura, K.; Miyamoto, Y.; Kitazawa, H.; Kanesaka, M.; Yoshimoto, R.; Aragane, K.; Tokita, S.; Sato, N.
    Synthesis and evaluation of a novel 2-azabicyclo[2.2.2]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors (2009), Bioorg. Med. Chem., 17, 5639-5647.
    View publication on PubMed
Search for more literature for 2.3.1.16

Inhibitors

Inhibitors Comment Organism Structure
(1R',4S',6R')-(+)-2-[(1-methyl-1H-imidazol-4-yl)sulfonyl]-N-[4-(propan-2-yloxy)phenyl]-2-azabicyclo[2.2.2]octane-6-carboxamide selective over other human ELOVL sub-types, good microsomal stability Homo sapiens
(1R',4S',6R')-(+/-)-2-(butylsulfonyl)-N-[4-(propan-2-yloxy)phenyl]-2-azabicyclo[2.2.2]octane-6-carboxamide racemic mixture of endo-isomers, the exo isomers are inactive Homo sapiens
(1R',4S',6R')-(+/-)-2-(phenylsulfonyl)-N-[4-(propan-2-yloxy)phenyl]-2-azabicyclo[2.2.2]octane-6-carboxamide racemic mixture of endo-isomers, the exo isomers are inactive Homo sapiens
(1R',4S',6R')-(+/-)-N-[4-(propan-2-yloxy)phenyl]-2-(thiophen-3-ylsulfonyl)-2-azabicyclo[2.2.2]octane-6-carboxamide racemic mixture of endo-isomers, the exo isomers are inactive 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
0.000067
-
 pH 6.5, 37°C Homo sapiens (1R',4S',6R')-(+/-)-N-[4-(propan-2-yloxy)phenyl]-2-(thiophen-3-ylsulfonyl)-2-azabicyclo[2.2.2]octane-6-carboxamide
0.00007
-
 pH 6.5, 37°C Homo sapiens (1R',4S',6R')-(+/-)-2-(phenylsulfonyl)-N-[4-(propan-2-yloxy)phenyl]-2-azabicyclo[2.2.2]octane-6-carboxamide
0.00012
-
 pH 6.5, 37°C Homo sapiens (1R',4S',6R')-(+/-)-2-(butylsulfonyl)-N-[4-(propan-2-yloxy)phenyl]-2-azabicyclo[2.2.2]octane-6-carboxamide
0.00022
-
 pH 6.5, 37°C Homo sapiens (1R',4S',6R')-(+)-2-[(1-methyl-1H-imidazol-4-yl)sulfonyl]-N-[4-(propan-2-yloxy)phenyl]-2-azabicyclo[2.2.2]octane-6-carboxamide