Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T16688 | Target Info | |||
| Target Name | Diacylglycerol acyltransferase 1 (DGAT1) | ||||
| Synonyms |
Retinol O-fatty-acyltransferase; Diglyceride acyltransferase; Diacylglycerol O-acyltransferase 1; DGAT; Acyl-CoA retinol O-fatty-acyltransferase; ARAT; AGRP1; ACAT-related gene product 1
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| Target Type | Successful Target | ||||
| Gene Name | DGAT1 | ||||
| Biochemical Class | Acyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-[4-[2-(Benzenesulfonamido)ethylcarbamoyl]phenoxy]adamantane-1-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3613337; BDBM50117145
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-[4-(2-Aminoethylcarbamoyl)phenoxy]adamantane-1-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3613335; BDBM50117147
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
[(3R)-1-[2-[(1S)-1-(4-Chloropyrazol-1-yl)ethyl]-1H-imidazo[4,5-b]pyridin-5-yl]piperidin-3-yl]-pyrrolidin-1-ylmethanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3893203; SCHEMBL15322898; BDBM215629; US9296745, 196-A; US9296745, 196-B
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-[4-(2-Benzamidoethylcarbamoyl)phenoxy]adamantane-1-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3613338; BDBM50117191
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4280459
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
N-(2-Cyclobutyl-2H-1,2,3-triazol-4-yl)-2-(2-(3-methoxyphenyl)acetyl)isoindoline-5-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
PF-06471553; CHEMBL3613709; SB19236; HY-108339; CS-0028403; N-(2-Cyclobutyl-2H-1,2,3-triazole-4-yl)-2-(3-methoxyphenylacetyl)isoindoline-5-sulfonamide
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
2-[4-[4-(5-Carbamoylpyridin-3-yl)phenyl]cyclohexyl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2178385; SCHEMBL2254352; SCHEMBL2254359; BDBM50399706; ZINC95580297
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| Activity |
IC50 = 60000 nM
|
[4] | |||
| Compound Name |
4-Amino-6-cyclopentyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2414693; BDBM50438697
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| Activity |
IC50 = 92100 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes. Eur J Med Chem. 2015 Aug 28;101:716-35. | ||||
| REF 2 | Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile. Medchemcomm. 2016 Nov 22;8(4):771-779. | ||||
| REF 3 | Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72. | ||||
| REF 4 | Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687). J Med Chem. 2012 Dec 13;55(23):10610-29. | ||||
| REF 5 | Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor. Bioorg Med Chem. 2013 Sep 1;21(17):5081-97. | ||||
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