General Information of the Protein
Protein ID
PT02536
Protein Name
Diacylglycerol O-acyltransferase 1
Secondarily
Protein Name
ACAT-related gene product 1
Acyl-CoA retinol O-fatty-acyltransferase
Diglyceride acyltransferase
Gene Name
DGAT1
Secondarily
Gene Name
AGRP1
DGAT
Sequence
MGDRGSSRRRRTGSRPSSHGGGGPAAAEEEVRDAAAGPDVGAAGDAPAPAPNKDGDAGVGSGHWELRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKYGILVDPIQVVSLFLKDPYSWPAPCLVIAANVFAVAAFQVEKRLAVGALTEQAGLLLHVANLATILCFPAAVVLLVESITPVGSLLALMAHTILFLKLFSYRDVNSWCRRARAKAASAGKKASSAAAPHTVSYPDNLTYRDLYYFLFAPTLCYELNFPRSPRIRKRFLLRRILEMLFFTQLQVGLIQQWMVPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWLFHSCLNAVAELMQFGDREFYRDWWNSESVTYFWQNWNIPVHKWCIRHFYKPMLRRGSSKWMARTGVFLASAFFHEYLVSVPLRMFRLWAFTGMMAQIPLAWFVGRFFQGNYGNAAVWLSLIIGQPIAVLMYVHDYYVLNYEAPAAEA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Catalyzes the terminal and only committed step in triacylglycerol synthesis by using diacylglycerol and fatty acyl CoA as substrates (PubMed:16214399, PubMed:18768481, PubMed:28420705, PubMed:9756920, PubMed:32433611, PubMed:32433610). Highly expressed in epithelial cells of the small intestine and its activity is essential for the absorption of dietary fats (PubMed:18768481). In liver, plays a role in esterifying exogenous fatty acids to glycerol, and is required to synthesize fat for storage (PubMed:16214399). Also present in female mammary glands, where it produces fat in the milk (By similarity). May be involved in VLDL (very low density lipoprotein) assembly (PubMed:18768481). In contrast to DGAT2 it is not essential for survival (By similarity). Functions as the major acyl-CoA retinol acyltransferase (ARAT) in the skin, where it acts to maintain retinoid homeostasis and prevent retinoid toxicity leading to skin and hair disorders (PubMed:16214399). Exhibits additional acyltransferase activities, includin acyl CoA:monoacylglycerol acyltransferase (MGAT), wax monoester and wax diester synthases (By similarity). Also able to use 1-monoalkylglycerol (1-MAkG) as an acyl acceptor for the synthesis of monoalkyl-monoacylglycerol (MAMAG) (PubMed:28420705).
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Uniprot ID
Primary ID:
O75907

Secondarily ID:
B2RWQ2
D3DWL6
Q96BB8
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Ensembl ID
ENSG00000185000
HGNC ID
HGNC:2843
Subcellular Location
Endoplasmic reticulum membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000034 , Caco-2
Compound ID Compound Name Compound Formula
CP0388551
ethyl 6-(3-tert-butyl-1,2,4-oxadiazol-5-yl)-2-morpholin-4-yl-4-phenyl-7-propylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C29H35N5O4
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0411910
ethyl 6-(3-cyclopentyl-1,2,4-oxadiazol-5-yl)-2-morpholin-4-yl-4-phenyl-7-propylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C30H35N5O4
 1
1
IC50 < 30 nM
   TI
   LI
   LO
   TS
CP0435339
ethyl 6-(3-cyclohexyl-1,2,4-oxadiazol-5-yl)-2-morpholin-4-yl-4-phenyl-7-propylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C31H37N5O4
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0412013
ethyl 2-morpholin-4-yl-4-phenyl-6-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)-7-propylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C28H33N5O4
 1
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
CP0435340
ethyl 6-(3-butyl-1,2,4-oxadiazol-5-yl)-2-morpholin-4-yl-4-phenyl-7-propylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C29H35N5O4
 1
1
IC50 = 69 nM
   TI
   LI
   LO
   TS
CP0388552
ethyl 2-morpholin-4-yl-4-phenyl-7-propyl-6-(3-pyrrolidin-1-yl-1,2,4-oxadiazol-5-yl)pyrrolo[1,2-b]pyridazine-5-carboxylate
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C29H34N6O4
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0388555
ethyl 2-morpholin-4-yl-4-phenyl-6-(3-phenyl-1,2,4-oxadiazol-5-yl)-7-propylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C31H31N5O4
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0388556
ethyl 7-(2-hydroxyethyl)-6-[3-(2-hydroxyethyl)-1,2,4-oxadiazol-5-yl]-2-morpholin-4-yl-4-phenylpyrrolo[1,2-b]pyridazine-5-carboxylate
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C26H29N5O6
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0067443
CHEMBL2036730
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C23H22F2N4O4
 2
1 IC50 = 2 nM
2 IC50 = 36 nM
CP0223870
CHEMBL3741505
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C22H22N4O4S
 1
1 IC50 = 4 nM
CP0238531
2-[4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]-3-chlorophenyl]acetic acid
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C21H18ClN3O3
 1
1 IC50 = 6.31 nM
CP0658357
cis-(4-(5-(5-(3,4-difluorophenylamino)-1,3,4-oxadiazole-2-carboxamido)-pyridin-2-yloxy)cyclohexyl)acetic acid
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C22H21F2N5O5
 1
1 IC50 = 7 nM
CP0240421
(2S)-2-[4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)-2-fluorophenyl]-3-chlorophenyl]propanoic acid
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C22H19ClFN3O3
 1
1 IC50 = 7.943 nM
CP0169155
CHEMBL1834554
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C20H23N3O4
 1
1 IC50 = 10 nM
CP0070847
CHEMBL2178953
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C21H25N3O3
 1
1 IC50 = 10 nM
CP0070794
CHEMBL3741095
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C23H21F2N3O4S
 1
1 IC50 = 11 nM
CP0448175
CHEMBL3741333
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C22H27N3O5S
 1
1 IC50 = 12 nM
CP0149070
CHEMBL3741569
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C23H23N3O4S
 1
1 IC50 = 16 nM
CP0235742
CHEMBL1833980
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C20H23N3O4
 1
1 IC50 = 18 nM
CP0085747
CHEMBL1835919
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C21H24N4O4
 1
1 IC50 = 19 nM
CP0209945
(1R,2R)-2-[(4-{4-[(phenylcarbamoyl)amino]phenyl}phenyl)carbonyl]cyclopentane-1-carboxylic acid
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C26H24N2O4
 1
1 IC50 = 20 nM
CP0223869
CHEMBL3739742
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C21H26N4O4S
 1
1 IC50 = 22 nM
CP0197867
CHEMBL2414696
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C22H26N4O4
 1
1 IC50 = 31.62 nM
CP0235312
CHEMBL2012625
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C24H25N3O3S
 1
1 IC50 = 36 nM
CP0115631
CHEMBL3233872
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C29H28N2O3
 1
1 IC50 = 37 nM
CP0137702
2-Phenyl-5-trifluoromethyloxazole-4-carboxylic Acid{6-[(2-Methoxyethyl)methylamino]pyridin-3-yl}amide
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C20H19F3N4O3
 1
1 IC50 = 38 nM
CP0313000
CHEMBL3740753
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C23H29N3O4S
 1
1 IC50 = 38 nM
CP0083969
CHEMBL3741723
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C22H22N4O4S
 1
1 IC50 = 45 nM
CP0531336
CHEMBL3741943
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C22H21ClN4O4S
 1
1 IC50 = 55 nM
CP0191591
N-(3-oxo-1-propyl-2H-indazol-5-yl)-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C21H17F3N4O3
 1
1 IC50 = 60 nM
CP0060386
CHEMBL3233884
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C29H30N2O4
 1
1 IC50 = 65 nM
CP0037325
2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl}phenyl)cyclohexyl]acetic acid
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C22H26N4O3
 1
1 IC50 = 72 nM
CP0367764
(1R,2R)-2-[4-[3-fluoro-4-[(6-fluoro-1,3-benzothiazol-2-yl)amino]phenyl]benzoyl]cyclopentane-1-carboxylic acid
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C26H20F2N2O3S
 1
1 IC50 = 73 nM
CP0291276
N-(2-morpholin-4-yl-1,3-thiazol-5-yl)-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C18H15F3N4O3S
 1
1 IC50 = 100 nM
CP0115904
2-[4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)-2-chlorophenyl]phenyl]acetic acid
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C21H18ClN3O3
 1
1 IC50 = 100 nM
CP0050575
4-(4-{4-[(2-Phenyl-5-trifluoromethyloxazole-4-carbonyl)-amino]phenyl}piperidine-1-carbonyl)-trans-cyclohexanecarboxylic Acid
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C30H30F3N3O5
 1
1 IC50 = 114 nM
CP0531337
CHEMBL3741016
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C23H21F2N3O5
 1
1 IC50 = 120 nM
CP0275315
N-(6-morpholin-4-ylpyridin-3-yl)-5-phenyl-2-(trifluoromethyl)furan-3-carboxamide
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C21H18F3N3O3
 1
1 IC50 = 140 nM
CP0291277
4-methyl-N-(6-morpholin-4-ylpyridin-3-yl)-2-phenyl-1,3-oxazole-5-carboxamide
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C20H20N4O3
 1
1 IC50 = 150 nM
CP0291275
N-(6-morpholin-4-ylpyridin-3-yl)-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C20H17F3N4O3
 1
1 IC50 = 160 nM
CP0573784
CHEMBL3741896
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C23H21F2N3O4S
 1
1 IC50 = 160 nM
CP0281746
CHEMBL1834558
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C21H25N3O4
 1
1 IC50 = 245 nM
CP0295979
CHEMBL1834556
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C20H22N4O2
 1
1 IC50 = 249 nM
CP0205880
N-[6-(diethylamino)pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C20H19F3N4O2
 1
1 IC50 = 253 nM
CP0246522
US8637507, B-17
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C27H25N3O4
 1
1 IC50 = 275 nM
CP0151924
N-(4-morpholin-4-ylphenyl)-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C21H18F3N3O3
 1
1 IC50 = 330 nM
CP0260178
N-(2-morpholin-4-ylpyrimidin-5-yl)-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C19H16F3N5O3
 1
1 IC50 = 380 nM
CP0339410
N-[6-(2-methoxyethylamino)pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C19H17F3N4O3
 1
1 IC50 = 407 nM
CP0260180
N-[6-[2-hydroxyethyl(methyl)amino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C19H17F3N4O3
 1
1 IC50 = 554 nM
CP0313002
CHEMBL2012627
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C24H24FN3O3S
 1
1 IC50 = 600 nM
CP0260179
5-chloro-N-(6-morpholin-4-ylpyridin-3-yl)-2-phenyl-1,3-oxazole-4-carboxamide
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C19H17ClN4O3
 1
1 IC50 = 610 nM
CP0240422
2-[4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]phenyl]acetic acid
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C21H19N3O3
 1
1 IC50 = 630.96 nM
CP0077134
N-[6-[ethyl(2-methoxyethyl)amino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C21H21F3N4O3
 1
1 IC50 = 653 nM
CP0275237
4-methyl-N-(6-morpholin-4-ylpyridin-3-yl)-2-phenyl-1,3-thiazole-5-carboxamide
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C20H20N4O2S
 1
1 IC50 = 660 nM
CP0260181
N-[6-[(2-methoxyacetyl)-methylamino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
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C20H17F3N4O4
 1
1 IC50 = 699 nM
CP0275314
5-ethyl-N-(6-morpholin-4-ylpyridin-3-yl)-2-phenyl-1,3-oxazole-4-carboxamide
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C21H22N4O3
 1
1 IC50 = 700 nM
CP0273348
4-{4-[(2-Phenyl-5-trifluoromethyloxazole-4-carbonyl)-amino]phenyl}piperidine-1-carboxylic Acid Methyl Ester
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C24H22F3N3O4
 1
1 IC50 < 500 nM
Clinical Information about the Protein
Target 1 ( Diacylglycerol acyltransferase 1 (DGAT1) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 High blood cholesterol level [ICD-11: 5C80.00]
Approved Drug(s) 1 Approved Drug  1
1 Hesperetin Approved
High blood cholesterol level
Target 2 ( DGAT1 messenger RNA (DGAT1 mRNA) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02560 Diacylglycerol O-acyltransferase 1 Mus musculus, Mouse