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Literature summary 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

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.22 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

EC Number Organism UniProt Comment Textmining
2.3.1.22 Homo sapiens Q3SYC2
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.22 intestine
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.22 0.000083
-
 pH 7.5, 23°C Homo sapiens 2-(4-chlorophenoxy)-N-[5-[(4-methoxyphenyl)sulfamoyl]-2-methylphenyl]acetamide