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Literature summary extracted from

  • Nakajima, K.; April, M.; Brewer, J.T.; Daniels, T.; Forster, C.J.; Gilmore, T.A.; Jain, M.; Kanter, A.; Kwak, Y.; Li, J.; McQuire, L.; Serrano-Wu, M.H.; Streeper, R.; Szklennik, P.; Thompson, J.; Wang, B.
    Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 1245-1248.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.20 expressed in Sf9 insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.20 (2S)-1-(3-[[(2S)-1-ethoxy-4-phenylbutan-2-yl]sulfamoyl]anilino)-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
-
 Homo sapiens
2.3.1.20 (2S)-1-[(1-[[(1S)-1-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3-phenylpropyl]carbamoyl]cyclopentyl)amino]-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
-
 Homo sapiens
2.3.1.20 N-(1-[[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]amino]-2-methyl-1-oxopropan-2-yl)-4-fluorobenzamide
-
 Homo sapiens
2.3.1.20 N-[(2S)-1-ethoxy-4-phenylbutan-2-yl]-1-[2-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamido]cyclopentane-1-carboxamide
-
 Homo sapiens
2.3.1.20 N-[1,5-bis(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
 Homo sapiens
2.3.1.20 N-[1-(4-fluoro-2-methylphenyl)-5-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
 Homo sapiens
2.3.1.20 N-[1-(4-fluorophenyl)-5-[2-(4-fluorophenyl)propan-2-yl]-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
 Homo sapiens
2.3.1.20 N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-(1-methylcyclopropane-1-carbonyl)alaninamide
-
 Homo sapiens
2.3.1.20 N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
 Homo sapiens
2.3.1.20 tert-butyl (2S)-2-[[1-([(2S)-2-[(2,2-dimethylpropanoyl)oxy]-4-methylpentanoyl]amino)cyclopentane-1-carbonyl]amino]-4-phenylbutanoate
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.20 endoplasmic reticulum
-
 Homo sapiens 5783
-

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.20 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.20 oleoyl-CoA + 1,2-dioleoyl-sn-glycerol
-
 Homo sapiens CoA + trioleoylglycerol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.20 DGAT1
-
 Homo sapiens
2.3.1.20 diacylglycerol acyltransferase 1
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.20 0.000007
-
 at pH 7.5 and 25°C Homo sapiens tert-butyl (2S)-2-[[1-([(2S)-2-[(2,2-dimethylpropanoyl)oxy]-4-methylpentanoyl]amino)cyclopentane-1-carbonyl]amino]-4-phenylbutanoate
2.3.1.20 0.000011
-
 at pH 7.5 and 25°C Homo sapiens (2S)-1-[(1-[[(1S)-1-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3-phenylpropyl]carbamoyl]cyclopentyl)amino]-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
2.3.1.20 0.000027
-
 at pH 7.5 and 25°C Homo sapiens N-[(2S)-1-ethoxy-4-phenylbutan-2-yl]-1-[2-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamido]cyclopentane-1-carboxamide
2.3.1.20 0.000062
-
 at pH 7.5 and 25°C Homo sapiens N-[1-(4-fluoro-2-methylphenyl)-5-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
2.3.1.20 0.00076
-
 at pH 7.5 and 25°C Homo sapiens N-[1,5-bis(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
2.3.1.20 0.0014
-
 at pH 7.5 and 25°C Homo sapiens N-[1-(4-fluorophenyl)-5-[2-(4-fluorophenyl)propan-2-yl]-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
2.3.1.20 0.0035
-
 at pH 7.5 and 25°C Homo sapiens N-(1-[[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]amino]-2-methyl-1-oxopropan-2-yl)-4-fluorobenzamide
2.3.1.20 0.0048
-
 at pH 7.5 and 25°C Homo sapiens N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
2.3.1.20 0.01
-
 IC50 less than 0.01 mM, at pH 7.5 and 25°C Homo sapiens (2S)-1-(3-[[(2S)-1-ethoxy-4-phenylbutan-2-yl]sulfamoyl]anilino)-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
2.3.1.20 0.01
-
 IC50 less than 0.01 mM, at pH 7.5 and 25°C Homo sapiens N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-(1-methylcyclopropane-1-carbonyl)alaninamide