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Literature summary for 2.3.1.22 extracted from

  • Adachi, R.; Ishii, T.; Ogawa, K.; Matsumoto, S.; Satou, T.; Sakamoto, J.; Sato, K.; Kawamoto, T.
    Pharmacological characterization of a series of aryl-sulfonamide derivatives that potently and selectively inhibit monoacylglycerol acyltransferase 2 (2016), Eur. J. Pharmacol., 791, 569-577 .
    View publication on PubMed
Search for more literature for 2.3.1.22

Inhibitors

Inhibitors Comment Organism Structure
1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2 Homo sapiens
1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
-
 Mus musculus
1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2 Homo sapiens
1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
-
 Mus musculus
2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]-N-(2,2,3,3,3-pentafluoropropyl)pyrimidine-5-carboxamide ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2 Homo sapiens
2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]-N-(2,2,3,3,3-pentafluoropropyl)pyrimidine-5-carboxamide
-
 Mus musculus
benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2 Homo sapiens
benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate
-
 Mus musculus
N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-phenyl-2,3-dihydro-1H-indole-5-sulfonamide ex hibits more than 100fold selectivity over human MGAT3, human DGAT1, and human DGAT2 Homo sapiens
N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-phenyl-2,3-dihydro-1H-indole-5-sulfonamide
-
 Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens Q3SYC2
-
-
Mus musculus Q80W94
-
-

Source Tissue

Source Tissue Comment Organism Textmining
intestine
-
 Homo sapiens
-
intestine
-
 Mus musculus
-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000006
-
 pH 7.4, 23°C Mus musculus N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-phenyl-2,3-dihydro-1H-indole-5-sulfonamide
0.0000011
-
 pH 7.4, 23°C Mus musculus benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate
0.0000014
-
 pH 7.4, 23°C Homo sapiens 1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
0.0000016
-
 pH 7.4, 23°C Mus musculus 1-([1,1'-biphenyl]-4-yl)-N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide
0.0000019
-
 pH 7.4, 23°C Mus musculus 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]-N-(2,2,3,3,3-pentafluoropropyl)pyrimidine-5-carboxamide
0.0000032
-
 pH 7.4, 23°C Homo sapiens N-(2,4-difluorophenyl)-7-(2-oxopyrrolidin-1-yl)-1-phenyl-2,3-dihydro-1H-indole-5-sulfonamide
0.0000034
-
 pH 7.4, 23°C Homo sapiens benzyl 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(5-oxopyrazolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]pyrimidine-5-carboxylate
0.0000038
-
 pH 7.4, 23°C Mus musculus 1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate
0.0000051
-
 pH 7.4, 23°C Homo sapiens 2-[5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indol-1-yl]-N-(2,2,3,3,3-pentafluoropropyl)pyrimidine-5-carboxamide
0.0000067
-
 pH 7.4, 23°C Homo sapiens 1-(2,2,3,3,3-pentafluoropropyl)piperidin-4-yl 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxoimidazolidin-1-yl)-2,3-dihydro-1H-indole-1-carboxylate