Literature summary for 2.3.1.20 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.

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Cloned(Commentary)

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

Inhibitors

Inhibitors	Comment	Organism	Structure
(2S)-1-(3-[[(2S)-1-ethoxy-4-phenylbutan-2-yl]sulfamoyl]anilino)-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate	-	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	-	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	-	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	-	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	-	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	-	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	-	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	-	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	-	Homo sapiens
tert-butyl (2S)-2-[[1-([(2S)-2-[(2,2-dimethylpropanoyl)oxy]-4-methylpentanoyl]amino)cyclopentane-1-carbonyl]amino]-4-phenylbutanoate	-	Homo sapiens

Localization

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
DGAT1	-	Homo sapiens
diacylglycerol acyltransferase 1	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
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
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
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
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
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
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
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
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
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
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

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Release 2023.1 (January 2023)