General Information of the Protein
Protein ID
PT01749
Protein Name
Diacylglycerol O-acyltransferase 2
Secondarily
Protein Name
Acyl-CoA retinol O-fatty-acyltransferase
Diglyceride acyltransferase 2
Gene Name
DGAT2
Secondarily
Gene Name
HMFN1045
UNQ738/PRO1433
Sequence
MKTLIAAYSGVLRGERQAEADRSQRSHGGPALSREGSGRWGTGSSILSALQDLFSVTWLNRSKVEKQLQVISVLQWVLSFLVLGVACSAILMYIFCTDCWLIAVLYFTWLVFDWNTPKKGGRRSQWVRNWAVWRYFRDYFPIQLVKTHNLLTTRNYIFGYHPHGIMGLGAFCNFSTEATEVSKKFPGIRPYLATLAGNFRMPVLREYLMSGGICPVSRDTIDYLLSKNGSGNAIIIVVGGAAESLSSMPGKNAVTLRNRKGFVKLALRHGADLVPIYSFGENEVYKQVIFEEGSWGRWVQKKFQKYIGFAPCIFHGRGLFSSDTWGLVPYSKPITTVVGEPITIPKLEHPTQQDIDLYHTMYMEALVKLFDKHKTKFGLPETEVLEVN
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Essential acyltransferase that catalyzes the terminal and only committed step in triacylglycerol synthesis by using diacylglycerol and fatty acyl CoA as substrates. Required for synthesis and storage of intracellular triglycerides (PubMed:27184406). Probably plays a central role in cytosolic lipid accumulation. In liver, is primarily responsible for incorporating endogenously synthesized fatty acids into triglycerides (By similarity). Functions also as an acyl-CoA retinol acyltransferase (ARAT) (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:
Q96PD7

Secondarily ID:
A6ND76
Q5U810
Q68CL3
Q68DJ0
Q8NDB7
Q96BS0
Q9BYE5
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HGNC ID
HGNC:16940
Subcellular Location
Endoplasmic reticulum membrane
Lipid droplet
Cytoplasm
Perinuclear region
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: CL000013 , Sf9
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0058071
 Compound Info 
N-tert-butyl-8-[[[(1S,2S)-2-(3-methyl-1,2,4-oxadiazol-5-yl)cyclopropanecarbonyl]amino]methyl]-5-[3-(trifluoromethoxy)phenyl]-3,4-dihydro-1H-isoquinoline-2-carboxamide
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C29H32F3N5O4
  1
1
IC50 = 2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0128442
 Compound Info 
N-tert-butyl-5-(3-methoxyphenyl)-8-[[[(1S,2S)-2-(3-methyl-1,2,4-oxadiazol-5-yl)cyclopropanecarbonyl]amino]methyl]-3,4-dihydro-1H-isoquinoline-2-carboxamide
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C29H35N5O4
  1
1
IC50 = 3 nM
 Bioactivity Info 
   TI
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   TS
CP0227630
 Compound Info 
N-tert-butyl-5-(3-methoxyphenyl)-8-[[[(1R,2R)-2-phenylcyclopropanecarbonyl]amino]methyl]-3,4-dihydro-1H-isoquinoline-2-carboxamide
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C32H37N3O3
  1
1
IC50 = 4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0487281
 Compound Info 
tert-butyl 5-(3-methoxyphenyl)-8-[[[(1R,2R)-2-phenylcyclopropanecarbonyl]amino]methyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate
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C32H36N2O4
  1
1
IC50 = 60 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0231766
 Compound Info 
US9828369, Example 155
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C25H19Cl2N3O3
  1
1
IC50 = 120 nM
 Bioactivity Info 
   TI
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CP0257873
 Compound Info 
methyl 3-[4-[[[(1R,2R)-2-phenylcyclopropanecarbonyl]amino]methyl]naphthalen-1-yl]benzoate
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C29H25NO3
  1
1
IC50 = 140 nM
 Bioactivity Info 
   TI
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CP0491031
 Compound Info 
N-((5-(3-methoxyphenyl)isoquinolin- 8-yl)methyl)spiro[2.5]octane-1- carboxamide
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C26H28N2O2
  1
1
IC50 = 180 nM
 Bioactivity Info 
   TI
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CP0128440
 Compound Info 
(1R,2R)-N-[[5-(3-methoxyphenyl)quinolin-8-yl]methyl]-2-phenylcyclopropane-1-carboxamide
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C27H24N2O2
  1
1
IC50 = 300 nM
 Bioactivity Info 
   TI
   LI
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CP0231765
 Compound Info 
(1R,2R)-N-[5-(3-methoxyphenyl)isoquinolin-8-yl]-2-(3-methyl-1,2,4-oxadiazol-5-yl)cyclopropane-1-carboxamide
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C23H20N4O3
  1
1
IC50 = 500 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0058070
 Compound Info 
1-(2,3-dichlorophenyl)-3-[[5-(3-methoxyphenyl)isoquinolin-8-yl]methyl]urea
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C24H19Cl2N3O2
  1
1
IC50 = 540 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0487280
 Compound Info 
(1R,2R)-N-[[5-(3-methoxyphenyl)isoquinolin-8-yl]methyl]-2-phenylcyclopropane-1-carboxamide
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C27H24N2O2
  1
1
IC50 = 600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0538644
 Compound Info 
(1R,2R)-N-[[8-(3-methoxyphenyl)isoquinolin-5-yl]methyl]-2-phenylcyclopropane-1-carboxamide
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C27H24N2O2
  1
1
IC50 = 1600 nM
 Bioactivity Info 
   TI
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   TS
CP0573605
 Compound Info 
(1R,2R)-2-phenyl-N-[[5-[3-(trifluoromethoxy)phenyl]isoquinolin-8-yl]methyl]cyclopropane-1-carboxamide
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C27H21F3N2O2
  1
1
IC50 = 2200 nM
 Bioactivity Info 
   TI
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   LO
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CP0265409
 Compound Info 
(1R,2R)-N-[[2-acetyl-5-(3-methoxyphenyl)-3,4-dihydro-1H-isoquinolin-8-yl]methyl]-2-phenylcyclopropane-1-carboxamide
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C29H30N2O3
  1
1
IC50 = 3460 nM
 Bioactivity Info 
   TI
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CP0060386
 Compound Info 
2-[4-[4-[4-(phenylcarbamoyl)-2,3-dihydro-1,4-benzoxazin-7-yl]phenyl]cyclohexyl]acetic acid
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C29H30N2O4
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0295271
 Compound Info 
CHEMBL3287865
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C30H32N2O4
  1
1
IC50 = 10000 nM
 Bioactivity Info 
   TI
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CP0552436
 Compound Info 
1-[(5-chloroisoquinolin-8-yl)methyl]-3-(2,3-dichlorophenyl)urea
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C17H12Cl3N3O
  1
1
IC50 > 12000 nM
 Bioactivity Info 
   TI
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CP0476412
 Compound Info 
2-[[5-(4-benzamidophenyl)-4-methyl-1,2,4-triazol-3-yl]sulfanyl]propanoic acid
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C19H18N4O3S
  1
1
IC50 > 20000 nM
 Bioactivity Info 
   TI
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CP0115631
 Compound Info 
2-[4-[4-[1-(phenylcarbamoyl)indol-5-yl]phenyl]cyclohexyl]acetic acid
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C29H28N2O3
  1
1
IC50 > 50000 nM
 Bioactivity Info 
   TI
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CP0552437
 Compound Info 
[5-(3-methoxyphenyl)isoquinolin-8-yl]methanamine
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C17H16N2O
  1
1
IC50 > 50000 nM
 Bioactivity Info 
   TI
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CP0050575
 Compound Info 
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 > 100000 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0060386
 Compound Info 
CHEMBL3233884
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C29H30N2O4
  1
1 IC50 > 10000 nM
CP0115631
 Compound Info 
CHEMBL3233872
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C29H28N2O3
  1
1 IC50 > 50000 nM
Clinical Information about the Protein
Target 1 ( Diacylglycerol O-acyltransferase 2 (DGAT2) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Lipid metabolism disorder [ICD-11: 5C52.Z]
2 Non-alcoholic steatohepatitis [ICD-11: DB92.1]
Approved Drug(s) 1 Approved Drug  1
1 Vitamin B3
 Drug Info 
Approved
Lipid metabolism disorder
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PF-06865571
 Drug Info 
Phase 2
Non-alcoholic steatohepatitis
Target 2 ( DGAT2 messenger RNA (DGAT2 mRNA) )
Target Type Clinical trial Target