Literature summary for 2.3.1.20 extracted from

Mougenot, P.; Namane, C.; Fett, E.; Goumy, F.; Dadji-Faihun, R.; Langot, G.; Monseau, C.; Onofri, B.; Pacquet, F.; Pascal, C.; Crespin, O.; Ben-Hassine, M.; Ragot, J.L.; Van-Pham, T.; Philippo, C.; Chatelain-Egger, F.; Peron, P.; Le Bail, J.C.; Guillot, E.; Chamiot-Clerc, P.; Chabanaud, M.A.; Pruniaux, M.-P.
Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 25-32.

Cloned(Commentary)

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

Inhibitors

Inhibitors	Comment	Organism
(trans-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenyl]cyclohexyl)acetic acid	-	Homo sapiens
(trans-4-[4-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbamoyl]phenyl]cyclohexyl)acetic acid	-	Homo sapiens
(trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl]cyclohexyl)acetic acid	-	Homo sapiens
cis-4-(4-[[5-(cyclopentylamino)-1,3,4-thiadiazol-2-yl]carbamoyl]phenoxy)cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-([5-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]pyridin-2-yl]oxy)cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[4-([3-[(3,5-difluorophenyl)methyl]-1,2,4-oxadiazol-5-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[4-[(5-anilino-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
cis-4-[[5-([5-[(3-chlorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)pyridin-2-yl]oxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-carbamoylcyclohexyl)benzamide	-	Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(dimethylamino)ethyl]carbamoyl]cyclohexyl)benzamide	-	Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(morpholin-4-yl)ethyl]carbamoyl]cyclohexyl)benzamide	-	Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2,3-dihydroxypropyl)carbamoyl]cyclohexyl]benzamide	-	Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-hydroxy-2-methylpropyl)carbamoyl]cyclohexyl]benzamide	-	Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-methoxyethyl)carbamoyl]cyclohexyl]benzamide	-	Homo sapiens
P-7435	-	Homo sapiens
pradigastat	-	Homo sapiens
trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid	-	Homo sapiens
[trans-4-(4-[[5-(2-cyclopentylethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]phenyl)cyclohexyl]acetic acid	-	Homo sapiens
[trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid	-	Homo sapiens
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-oxadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid	-	Homo sapiens
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid	-	Homo sapiens
[trans-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid	-	Homo sapiens
[trans-4-[4-([5-[2-(oxolan-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid	-	Homo sapiens
[trans-4-[4-([5-[2-(oxolan-3-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid	-	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
octanoyl-CoA + 1,2-di-(cis-9-octadecenoyl)-sn-glycerol	Homo sapiens	-	CoA + 1,2-di-(cis-9-octadecenoyl)-3-octanoyl-sn-glycerol	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
octanoyl-CoA + 1,2-di-(cis-9-octadecenoyl)-sn-glycerol	-	Homo sapiens	CoA + 1,2-di-(cis-9-octadecenoyl)-3-octanoyl-sn-glycerol	-	?

Synonyms

Synonyms	Comment	Organism
DGAT-1	-	Homo sapiens
diacylglycerol acyltransferase type 1	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.000004	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[4-[(5-anilino-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
0.000009	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
0.000011	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
0.000012	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
0.000016	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
0.000019	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-(4-[[5-(2-cyclopentylethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]phenyl)cyclohexyl]acetic acid
0.000022	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-(4-[[5-(cyclopentylamino)-1,3,4-thiadiazol-2-yl]carbamoyl]phenoxy)cyclohexane-1-carboxylic acid
0.000036	-	at pH 7.4 and 37°C	Homo sapiens	(trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
0.000038	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
0.000045	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-([5-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]pyridin-2-yl]oxy)cyclohexane-1-carboxylic acid
0.000048	-	at pH 7.4 and 37°C	Homo sapiens	N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-carbamoylcyclohexyl)benzamide
0.000055	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[[5-([5-[(3-chlorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)pyridin-2-yl]oxy]cyclohexane-1-carboxylic acid
0.000057	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
0.000081	-	at pH 7.4 and 37°C	Homo sapiens	N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2,3-dihydroxypropyl)carbamoyl]cyclohexyl]benzamide
0.000088	-	at pH 7.4 and 37°C	Homo sapiens	N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-methoxyethyl)carbamoyl]cyclohexyl]benzamide
0.000092	-	at pH 7.4 and 37°C	Homo sapiens	N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-hydroxy-2-methylpropyl)carbamoyl]cyclohexyl]benzamide
0.00012	-	at pH 7.4 and 37°C	Homo sapiens	cis-4-[4-([3-[(3,5-difluorophenyl)methyl]-1,2,4-oxadiazol-5-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
0.000122	-	at pH 7.4 and 37°C	Homo sapiens	N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(morpholin-4-yl)ethyl]carbamoyl]cyclohexyl)benzamide
0.000144	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-[4-([5-[2-(oxolan-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
0.00016	-	at pH 7.4 and 37°C	Homo sapiens	trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
0.000233	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-[4-([5-[2-(oxolan-3-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
0.000253	-	at pH 7.4 and 37°C	Homo sapiens	(trans-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
0.000279	-	at pH 7.4 and 37°C	Homo sapiens	N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(dimethylamino)ethyl]carbamoyl]cyclohexyl)benzamide
0.00028	-	at pH 7.4 and 37°C	Homo sapiens	trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
0.000286	-	at pH 7.4 and 37°C	Homo sapiens	(trans-4-[4-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
0.0006	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
0.00139	-	at pH 7.4 and 37°C	Homo sapiens	[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-oxadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid