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Literature summary for 2.3.1.16 extracted from

  • Mizutani, T.; Ishikawa, S.; Nagase, T.; Takahashi, H.; Fujimura, T.; Sasaki, T.; Nagumo, A.; Shimamura, K.; Miyamoto, Y.; Kitazawa, H.; Kanesaka, M.; Yoshimoto, R.; Aragane, K.; Tokita, S.; Sato, N.
    Discovery of novel benzoxazinones as potent and orally active long chain fatty acid elongase 6 inhibitors (2009), J. Med. Chem., 52, 7289-7300.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-fluoro-N-[[2-oxo-6-(1H-pyrazol-1-yl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]benzamide
-
Homo sapiens
4-fluoro-N-[[2-oxo-6-(1H-pyrazol-4-yl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]benzamide
-
Homo sapiens
4-fluoro-N-[[2-oxo-6-(1H-pyrazol-5-yl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]benzamide the S-isomer shows potent and selective inhibitory activity toward human ELOVL6 Homo sapiens
N-[[6-chloro-2-oxo-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]-4-fluorobenzamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9H5J4 isoform Elovl6
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
pH 6.5, 37°C Homo sapiens 4-fluoro-N-[[2-oxo-6-(1H-pyrazol-5-yl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]benzamide
0.000022
-
pH 6.5, 37°C Homo sapiens 4-fluoro-N-[[2-oxo-6-(1H-pyrazol-4-yl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]benzamide
0.000026
-
pH 6.5, 37°C Homo sapiens N-[[6-chloro-2-oxo-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]-4-fluorobenzamide
0.000026
-
pH 6.5, 37°C Homo sapiens 4-fluoro-N-[[2-oxo-6-(1H-pyrazol-1-yl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-4-yl]methyl]benzamide