Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94309 | Target Info | |||
| Target Name | Pancreatic triacylglycerol lipase (PNLIP) | ||||
| Synonyms |
Pancreatic lipase; PTL; PL
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| Target Type | Successful Target | ||||
| Gene Name | PNLIP | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 7 binders) | Download | Top | |||
|---|---|---|---|---|---|
| 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
|
[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
|
[1] | |||
| 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
|
[1] | |||
| Compound Name |
N'-[(2S)-1-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-N-(4-heptoxyphenyl)butanediamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2022676; BDBM50381861
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| Activity |
Ki = 67000 nM
|
[2] | |||
| Compound Name |
Methyl 2-[[(2E,8E)-deca-2,8-dienoyl]amino]-3-(5-hydroxy-6-oxo-3,8-dioxatricyclo[5.1.0.02,4]octan-5-yl)propanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL263831; BDBM50213686
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| Activity |
IC50 = 120000 nM
|
[3] | |||
| Compound Name |
Koenimbine
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Investigative | Compound Info | ||
| Synonyms |
Kenimbine; Koenimbin; 8-methoxy-3,3,5-trimethyl-11H-pyrano[3,2-a]carbazole; 3,11-Dihydro-8-methoxy-3,3,5-trimethylpyrano(3,2-a)carbazole; 8-Methoxy-3,3,5-trimethyl-3,11-dihydropyrano[3,2-a]carbazole; Pyrano(3,2-a)carbazole, 3,11-dihydro-8-methoxy-3,3,5-trimethyl-; NSC127152; Koenimbine, analytical standard; CHEMBL2323768; CTK8D5869; DTXSID90175317; ZINC1715690; BDBM50207384; NSC 127152; NSC-127152; 3,11-Dihydro-8-methoxy-3,3,5-trimethylpyrano[3,2-a]carbazole, 9CI
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| Activity |
IC50 = 168600 nM
|
[4] | |||
| Compound Name |
N'-[(2S)-1-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-N-(4-butoxyphenyl)butanediamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2022680; BDBM50381860
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| Activity |
Ki = 170000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Methyl (2R)-2-[[(2E,8E)-deca-2,8-dienoyl]amino]-3-[(5R)-5-hydroxy-6-oxo-3,8-dioxatricyclo[5.1.0.02,4]octan-5-yl]propanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL253780; BDBM50213694
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| Activity |
IC50 = 270000 nM
|
[3] | |||
| Compound Name |
N'-[(1S)-2-[[(1S)-2-Amino-1-naphthalen-2-yl-2-oxoethyl]amino]-1-naphthalen-2-yl-2-oxoethyl]-N-(4-butoxyphenyl)butanediamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2022681; BDBM50381859
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| Activity |
Ki = 360000 nM
|
[2] | |||
| Compound Name |
Koenigicine
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Investigative | Compound Info | ||
| Synonyms |
Kenidine; CHEMBL3893262; 8,9-dimethoxy-3,3,5-trimethyl-11H-pyrano[3,2-a]carbazole; Kenigicine; Kenimbidine; Koenimbidine; Koenidine; NSC127151; 8,9-dimethoxy-3,3,5-trimethyl-3,11-dihydropyrano[3,2-a]carbazole; CTK4F2963; DTXSID00298965; BDBM50207383; NSC-127151; 3,11-Dihydro-8,9-dimethoxy-3,3,5-trimethylpyrano[3,2-a]carbazole, 9CI; Pyrano[3,2-a]carbazole,3,11-dihydro-8,9-dimethoxy-3,3,5-trimethyl-
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| Activity |
IC50 = 428600 nM
|
[4] | |||
| Compound Name |
N'-[(2S)-1-[[(2S)-1-Amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-N-(4-butoxyphenyl)butanediamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2022679; BDBM50381858
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| Activity |
Ki = 550000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | An approach for differentiating isozymes. Construction of libraries containing short aromatic peptides as part of a method to design selective inhibitors against lipases. Bioorg Med Chem Lett. 2012 May 1;22(9):3147-51. | ||||
| REF 3 | The biology and chemistry of hyperlipidemia. Bioorg Med Chem. 2007 Jul 15;15(14):4674-99. | ||||
| REF 4 | Synthesis, evaluation and molecular modelling studies of 2-(carbazol-3-yl)-2-oxoacetamide analogues as a new class of potential pancreatic lipase inhibitors. Bioorg Med Chem. 2017 Jan 15;25(2):609-620. | ||||
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