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Literature summary for 2.3.1.22 extracted from

  • Adachi, R.; Ishii, T.; Matsumoto, S.; Satou, T.; Sakamoto, J.; Kawamoto, T.
    Discovery of human intestinal MGAT inhibitors using high-throughput mass spectrometry (2017), SLAS Discov., 22, 360-365 .
    View publication on PubMed

Application

Application Comment Organism
analysis development of a MGAT enzymatic assay of human intestinal microsomes using a high-throughput mass spectrometry-based detection system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(4-chlorophenoxy)-N-[5-[(4-methoxyphenyl)sulfamoyl]-2-methylphenyl]acetamide potent inhibitory activity toward human intestinal MGAT and recombinant human MGAT2, with selectivity over MGAT3. IC50 value in intestinal microsomes 0.000021 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q3SYC2
-
-

Source Tissue

Source Tissue Comment Organism Textmining
intestine
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
oleoyl-CoA + 2-oleoylglycerol
-
Homo sapiens CoA + 1,2-dioleoylglycerol
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000083
-
pH 7.5, 23°C Homo sapiens 2-(4-chlorophenoxy)-N-[5-[(4-methoxyphenyl)sulfamoyl]-2-methylphenyl]acetamide