General Information of the Protein
Protein ID
PT02150
Protein Name
Lipoprotein lipase
Secondarily
Protein Name
Phospholipase A1
Gene Name
LPL
Secondarily
Gene Name
LIPD
Sequence
MESKALLVLTLAVWLQSLTASRGGVAAADQRRDFIDIESKFALRTPEDTAEDTCHLIPGVAESVATCHFNHSSKTFMVIHGWTVTGMYESWVPKLVAALYKREPDSNVIVVDWLSRAQEHYPVSAGYTKLVGQDVARFINWMEEEFNYPLDNVHLLGYSLGAHAAGIAGSLTNKKVNRITGLDPAGPNFEYAEAPSRLSPDDADFVDVLHTFTRGSPGRSIGIQKPVGHVDIYPNGGTFQPGCNIGEAIRVIAERGLGDVDQLVKCSHERSIHLFIDSLLNEENPSKAYRCSSKEAFEKGLCLSCRKNRCNNLGYEINKVRAKRSSKMYLKTRSQMPYKVFHYQVKIHFSGTESETHTNQAFEISLYGTVAESENIPFTLPEVSTNKTYSFLIYTEVDIGELLMLKLKWKSDSYFSWSDWWSSPGFAIQKIRVKAGETQKKVIFCSREKVSHLQKGKAPAVFVKCHDKSLNKKSG
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Key enzyme in triglyceride metabolism. Catalyzes the hydrolysis of triglycerides from circulating chylomicrons and very low density lipoproteins (VLDL), and thereby plays an important role in lipid clearance from the blood stream, lipid utilization and storage (PubMed:8675619, PubMed:11342582, PubMed:27578112). Although it has both phospholipase and triglyceride lipase activities it is primarily a triglyceride lipase with low but detectable phospholipase activity (PubMed:7592706, PubMed:12032167). Mediates margination of triglyceride-rich lipoprotein particles in capillaries (PubMed:24726386). Recruited to its site of action on the luminal surface of vascular endothelium by binding to GPIHBP1 and cell surface heparan sulfate proteoglycans (PubMed:11342582, PubMed:27811232).
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Uniprot ID
Primary ID:
P06858

Secondarily ID:
B2R5T9
Q16282
Q16283
Q96FC4
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HGNC ID
HGNC:6677
Subcellular Location
Cell membrane
Secreted
Secreted
Extracellular space
Extracellular matrix
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: CL000053 , COS-7
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0058220
 Compound Info 
(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl (2S)-2-formamido-4-methylpentanoate
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C29H53NO5
  1
1
IC50 = 66 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0384154
 Compound Info 
2-[methylsulfonyl-(6-phenyl-1,3-benzothiazol-2-yl)methyl]-5-[(sulfamoylamino)methyl]-1,3,4-oxadiazole
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C18H17N5O5S3
  1
1
IC50 = 12000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0480000
 Compound Info 
N-[3-(3,4-dichlorophenyl)propyl]-4-hydroxy-1-methyl-5-oxo-2H-pyrrole-3-carboxamide
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C15H16Cl2N2O3
  1
1
IC50 > 37000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0410982
 Compound Info 
N-[3-(3,4-dichlorophenyl)propyl]-3-hydroxy-1-methyl-2-oxopyridine-4-carboxamide
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C16H16Cl2N2O3
  1
1
IC50 > 90000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0275760
 Compound Info 
4,4,5,5-tetramethyl-2-(4-phenylphenyl)-1,3,2-dioxaborolane
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C18H21BO2
  1
1 IC50 = 4400 nM
CP0069649
 Compound Info 
4,4,5,5-tetramethyl-2-(4-thiophen-2-ylphenyl)-1,3,2-dioxaborolane
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C16H19BO2S
  1
1 IC50 = 7000 nM
CP0275756
 Compound Info 
(4-propylphenyl)boronic acid
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C9H13BO2
  1
1 IC50 = 8000 nM
CP0076286
 Compound Info 
(4-methylphenyl)boronic acid
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C7H9BO2
  1
1 IC50 = 9000 nM
CP0076293
 Compound Info 
(4-ethylphenyl)boronic acid
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C8H11BO2
  1
1 IC50 = 9000 nM
CP0128905
 Compound Info 
2-[4-(furan-2-yl)phenyl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
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C16H19BO3
  1
1 IC50 = 9600 nM
CP0291699
 Compound Info 
4,4,5,5-tetramethyl-2-(4-thiophen-3-ylphenyl)-1,3,2-dioxaborolane
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C16H19BO2S
  1
1 IC50 = 13000 nM
CP0275757
 Compound Info 
(4-pentylphenyl)boronic acid
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C11H17BO2
  1
1 IC50 = 15000 nM
CP0282933
 Compound Info 
2-[4-(furan-3-yl)phenyl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
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C16H19BO3
  1
1 IC50 = 15000 nM
CP0235662
 Compound Info 
4,4,5,5-tetramethyl-2-(4-naphthalen-2-ylphenyl)-1,3,2-dioxaborolane
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C22H23BO2
  1
1 IC50 = 22000 nM
CP0291700
 Compound Info 
4,4,5,5-tetramethyl-2-(4-propylphenyl)-1,3,2-dioxaborolane
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C15H23BO2
  1
1 IC50 = 25000 nM
CP0275758
 Compound Info 
(4-heptylphenyl)boronic acid
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C13H21BO2
  1
1 IC50 = 30000 nM
CP0126566
 Compound Info 
(4-nonylphenyl)boranediol
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C15H25BO2
  1
1 IC50 = 42000 nM
CP0275755
 Compound Info 
4,4,5,5-tetramethyl-2-(3-pentylphenyl)-1,3,2-dioxaborolane
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C17H27BO2
  1
1 IC50 = 45000 nM
CP0128880
 Compound Info 
(4-undecylphenyl)boronic acid
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C17H29BO2
  1
1 IC50 = 50000 nM
CP0235765
 Compound Info 
4,4,5,5-tetramethyl-2-(4-nonylphenyl)-1,3,2-dioxaborolane
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C21H35BO2
  1
1 IC50 = 50000 nM
CP0275754
 Compound Info 
(3-pentylphenyl)boronic acid
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C11H17BO2
  1
1 IC50 = 50000 nM
CP0298058
 Compound Info 
4,4,5,5-tetramethyl-2-(4-pentylphenyl)-1,3,2-dioxaborolane
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C17H27BO2
  1
1 IC50 = 50000 nM
CP0126569
 Compound Info 
2-(4-heptylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
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C19H31BO2
  1
1 IC50 = 55000 nM
CP0293797
 Compound Info 
2-[4-(4-fluorophenyl)phenyl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
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C18H20BFO2
  1
1 IC50 = 55000 nM
CP0126567
 Compound Info 
(3-nonylphenyl)boronic acid
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C15H25BO2
  1
1 IC50 > 50000 nM
CP0126568
 Compound Info 
(2-nonylphenyl)boronic acid
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C15H25BO2
  1
1 IC50 > 50000 nM
CP0275759
 Compound Info 
4,4,5,5-tetramethyl-2-(4-undecylphenyl)-1,3,2-dioxaborolane
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C23H39BO2
  1
1 IC50 > 50000 nM
Clinical Information about the Protein
Target 1 ( Lipoprotein lipase (LPL) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Dysbetalipoproteinemia [ICD-11: 5C80.2]
2 Hyperlipidaemia [ICD-11: 5C80]
Approved Drug(s) 2 Approved Drugs  2
1 Clofibrate
 Drug Info 
Approved
Dysbetalipoproteinemia
2 Gemfibrozil
 Drug Info 
Approved
Hyperlipidaemia
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Ibrolipim
 Drug Info 
Phase 2
Hyperlipidaemia