orlistat
Ligand Summary
A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.
UNII: 95M8R751W8
PubChem: 3034010
Guide to Pharmacology: 5277
ChEMBL: CHEMBL175247
DrugCentral: 1996
LyCHI: F17BATCFGD4H
Target Activities
ABHD12
Monoacylglycerol lipase ABHD12
7 Activities
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1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.1 | |||||
IC50 | 7.1 | Bioorg. Med. Chem. Lett., (2008) 18:22:5838 | ||||
IC50 | 6.72 | Bioorg. Med. Chem. Lett., (2015) 25:7:1436 | ||||
IC50 | 6.72 | Bioorg. Med. Chem. Lett., (2015) 25:7:1436 | ||||
IC50 | 6.72 | Bioorg. Med. Chem., (2015) 23:19:6335 | ||||
IC50 | 6.72 | Bioorg. Med. Chem., (2015) 23:19:6335 | ||||
IC50 | 7.1 | |||||
ABHD6
Monoacylglycerol lipase ABHD6
7 Activities
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1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.88 | Bioorg. Med. Chem., (2015) 23:19:6335 | ||||
IC50 | 7.85 | Bioorg. Med. Chem., (2015) 23:19:6335 | ||||
IC50 | 7.7 | Bioorg. Med. Chem., (2015) 23:19:6335 | ||||
IC50 | 7.43 | Bioorg. Med. Chem., (2015) 23:19:6335 | ||||
IC50 | 7.32 | Bioorg. Med. Chem. Lett., (2015) 25:7:1436 | ||||
IC50 | 7.32 | Bioorg. Med. Chem. Lett., (2015) 25:7:1436 | ||||
IC50 | 7.32 | |||||
DAGLA
Sn1-specific diacylglycerol lipase alpha
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.2 | |||||
IC50 | 9 | Bioorg. Med. Chem., (2016) 24:7:1455 | ||||
IC50 | 8 | Bioorg. Med. Chem. Lett., (2012) 22:14:4585 | ||||
IC50 | 7.22 | Bioorg. Med. Chem. Lett., (2008) 18:22:5838 | ||||
IC50 | 6 | J. Med. Chem., (2008) 51:21:6970 | ||||
IC50 | 8 | |||||
DAGLB
Sn1-specific diacylglycerol lipase beta
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7 | |||||
IC50 | 7.22 | Bioorg. Med. Chem. Lett., (2008) 18:22:5838 | ||||
IC50 | 6.38 | Bioorg. Med. Chem., (2016) 24:7:1455 | ||||
IC50 | 7.22 | |||||
PNLIP
Pancreatic triacylglycerol lipase
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.9 | |||||
IC50 | 8.22 | ACS Med Chem Lett, (2018) 9:12:1263 | ||||
IC50 | 6.72 | ACS Med Chem Lett, (2018) 9:7:662 | ||||
IC50 | 8.9 | INHIBITOR | ||||
ABHD16A
Protein ABHD16A
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.52 | Bioorg. Med. Chem. Lett., (2008) 18:22:5838 | ||||
IC50 | 6.77 | ACS Med Chem Lett, (2018) 9:12:1269 | ||||
IC50 | 7.52 | |||||
LPL
Lipoprotein lipase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.18 | ACS Med Chem Lett, (2018) 9:12:1263 | ||||
IC50 | 7.18 | |||||
LIPC
Hepatic triacylglycerol lipase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52 | ACS Med Chem Lett, (2018) 9:12:1263 | ||||
IC50 | 8.52 | |||||
PLA2G7
Platelet-activating factor acetylhydrolase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.3 | Bioorg. Med. Chem. Lett., (2008) 18:22:5838 | ||||
IC50 | 7.3 | |||||
LIPG
Endothelial lipase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.22 | ACS Med Chem Lett, (2018) 9:12:1263 | ||||
IC50 | 8.22 | |||||
FASN
Fatty acid synthase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.55 | J. Med. Chem., (2011) 54:16:5615 | ||||
LIPF
Gastric triacylglycerol lipase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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INHIBITOR | ||||||