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Literature summary for 2.3.1.16 extracted from

  • Takahashi, T.; Nagase, T.; Sasaki, 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 indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors (2009), J. Med. Chem., 52, 3142-3145.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-[1-(4-chlorophenyl)-5-methyl-3-oxo-2,3-dihydro-1H-pyrazol-4-yl]-6,6-dimethyl-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
-
Homo sapiens
4-[4-[6,6-dimethyl-2,4-dioxo-1-phenyl-3-(trifluoromethyl)-2,3,4,5,6,7-hexahydro-1H-indol-3-yl]-5-methyl-3-oxo-2,3-dihydro-1H-pyrazol-1-yl]benzonitrile
-
Homo sapiens
6,6-dimethyl-3-(5-methyl-3-oxo-1-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
-
Homo sapiens
6,6-dimethyl-3-[5-methyl-1-(4-methylphenyl)-3-oxo-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
-
Homo sapiens
6,6-dimethyl-3-[5-methyl-3-oxo-1-[4-(propan-2-yl)phenyl]-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
-
Homo sapiens
6,6-dimethyl-3-[5-methyl-3-oxo-1-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
-
Homo sapiens
6,6-dimethyl-3-[5-methyl-3-oxo-1-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione inhibitor shows sustained plasma exposure and good liver penetrability. After oral administration, it potently inhibits ELOVL6 activity in liver Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoform Elovl6
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Mus musculus
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000087
-
-
Homo sapiens 6,6-dimethyl-3-[5-methyl-1-(4-methylphenyl)-3-oxo-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
0.0000089
-
-
Homo sapiens 6,6-dimethyl-3-[5-methyl-3-oxo-1-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
0.00001
-
-
Homo sapiens 6,6-dimethyl-3-[5-methyl-3-oxo-1-[4-(propan-2-yl)phenyl]-2,3-dihydro-1H-pyrazol-4-yl]-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
0.000012
-
-
Homo sapiens 3-[1-(4-chlorophenyl)-5-methyl-3-oxo-2,3-dihydro-1H-pyrazol-4-yl]-6,6-dimethyl-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione
0.000014
-
-
Homo sapiens 4-[4-[6,6-dimethyl-2,4-dioxo-1-phenyl-3-(trifluoromethyl)-2,3,4,5,6,7-hexahydro-1H-indol-3-yl]-5-methyl-3-oxo-2,3-dihydro-1H-pyrazol-1-yl]benzonitrile
0.00029
-
-
Homo sapiens 6,6-dimethyl-3-(5-methyl-3-oxo-1-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione