Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T28692 | Target Info | |||
| Target Name | Lipoprotein lipase (LPL) | ||||
| Synonyms |
LIPD
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| Target Type | Successful Target | ||||
| Gene Name | LPL | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 21 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-Nonylphenylboronic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952301; (2-nonylphenyl)boronic acid; BDBM50364288
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Pinacol(4-Undecylphenyl)Boronate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952305; BDBM50364293; 4,4,5,5-tetramethyl-2-(4-undecylphenyl)-1,3,2-dioxaborolane
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
3-(4-Chlorophenyl)-N-methyl-N-phenyl-5-(2,2,2-trifluoroethylsulfanyl)-1,2,4-triazole-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL131588; BDBM50138737; 3-(4-chlorophenyl)-N-methyl-N-phenyl-5-(2,2,2-trifluoroethylthio)-1H-1,2,4-triazole-1-carboxamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
Pinacol(4-Pentylphenyl)Boronate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952303; BDBM50364290; 4,4,5,5-tetramethyl-2-(4-pentylphenyl)-1,3,2-dioxaborolane
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
Pinacol(4-Nonylphenyl)Boronate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1949700; BDBM50364292
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
5-Methylsulfanyl-3-(4-trifluoromethoxy-phenyl)-[1,2,4]triazole-1-carboxylic acid methyl-phenyl-amide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL131051; BDBM50138751; N-methyl-5-(methylthio)-N-phenyl-3-(4-(trifluoromethoxy)phenyl)-1H-1,2,4-triazole-1-carboxamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(S)-4-Isopropyl-3-methyl-2-(3-methylpiperidine-1-carbonyl)isoxazol-5(2H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL106126; BAY 59-9435; BDBM50138735; HY-102056; CS-0022858; 4-Isopropyl-3-methyl-2-((S)-3-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one; 4-isopropyl-3-methyl-2-[1-(3-(s)-methyl-piperidin-1-yl)-methanoyl]-2h-isoxazol-5-one
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-Undecylphenylboronic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952298; (4-undecylphenyl)boronic acid; SCHEMBL7781648; BDBM50364285
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
3-Nonylphenylboronic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952300; (3-nonylphenyl)boronic acid; BDBM50364287
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
3-Pentylphenylboronic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952299; (3-pentylphenyl)boronic acid; SCHEMBL1997891; BDBM50364286
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| Activity |
IC50 = 50000 nM
|
[1] | |||
| Compound Name |
Pinacol(4-(4-Fluorophenyl)Phenyl)Boronate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952308; SCHEMBL792244; BDBM50364296; J3.640.376D; 2-[4-(4-fluorophenyl)phenyl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolane; 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolane-2-yl)-4'-fluorobiphenyl; 2-(4'-fluoro-[1,1'-biphenyl]-4-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
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| Activity |
IC50 = 55000 nM
|
[1] | |||
| Compound Name |
Pinacol(4-Heptylphenyl)Boronate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952304; BDBM50364291; 2-(4-heptylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
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| Activity |
IC50 = 55000 nM
|
[1] | |||
| Compound Name |
2-[(3S)-3-[(5-Fluoropyridin-2-yl)methoxy]pyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093393; BDBM50444141
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| Activity |
IC50 = 76300 nM
|
[3] | |||
| Compound Name |
2-[(3S)-3-[(3-Fluoropyridin-2-yl)methoxy]pyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093394; BDBM50444140
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| Activity |
IC50 = 77200 nM
|
[3] | |||
| Compound Name |
Chembl4212095
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL15953334; BDBM50458647; N-[3-(3,4-dichlorophenyl)propyl]-3-hydroxy-1-methyl-2-oxopyridine-4-carboxamide
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| Activity |
IC50 ~ 90000 nM
|
[4] | |||
| Compound Name |
2-[(3S)-3-(4-Fluorophenoxy)pyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093302; BDBM50444144
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2-[(3S)-3-(2-Ethoxyethoxy)pyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093398; BDBM50444146
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Pinacol(3-Pentylphenyl)Boronate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952306; BDBM50364294
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|
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
2-[(3S)-3-Butoxypyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093391; BDBM50444143
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2-[(3S)-3-[2-(2-Methoxyethoxy)ethoxy]pyrrolidin-1-yl]-5-(trifluoromethyl)benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093399; BDBM50444142
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-[3-[4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1952314; BDBM50364302
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| Activity |
IC50 = 120000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and synthesis of boronic acid inhibitors of endothelial lipase. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1397-401. | ||||
| REF 2 | Synthesis and structure-activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase. J Med Chem. 2004 Jan 15;47(2):400-10. | ||||
| REF 3 | Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. | ||||
| REF 4 | PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor. ACS Med Chem Lett. 2018 Jun 15;9(7):673-678. | ||||
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