Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T95558 | Target Info | |||
| Target Name | Diacylglycerol O-acyltransferase 2 (DGAT2) | ||||
| Synonyms |
UNQ738/PRO1433; HMFN1045; Diglyceride acyltransferase 2
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| Target Type | Successful Target | ||||
| Gene Name | DGAT2 | ||||
| Biochemical Class | Acyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-[[1-[5-[(3-Phenoxybenzoyl)amino]pyridin-2-yl]piperidin-4-yl]methoxy]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2334082; SCHEMBL10113679; BDBM50429008
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4126883
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Investigative | Compound Info | ||
| Synonyms |
BDBM50272088
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
[5-(3-Methoxyphenyl)isoquinolin-8-yl]methanamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3735953; SCHEMBL17571771; BDBM50499294
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
Chembl4126331
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Investigative | Compound Info | ||
| Synonyms |
BDBM50272089
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
2-[4-[4-[1-(Phenylcarbamoyl)indol-5-yl]phenyl]cyclohexyl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3233872; SCHEMBL384546; SCHEMBL384547; SCHEMBL10197149; SCHEMBL10197691; BDBM50009391
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
4-[4-[2-[(4-Phenylbenzoyl)amino]ethylcarbamoyl]phenoxy]adamantane-1-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3613340; CHEMBL3613349; CHEMBL3613350; BDBM50117149; BDBM50117152; BDBM50117189
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
4-(4-{4-[(2-Phenyl-5-trifluoromethyloxazole-4-carbonyl)-amino]phenyl}piperidine-1-carbonyl)-cis-cyclohexanecarboxylic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1766811; CHEMBL1766812; SCHEMBL594863; SCHEMBL1101806; SCHEMBL1102060; BDBM50341782; BDBM50341783
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| 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 ~ 100000 nM
|
[7] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
AZD7687
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|
Phase 1 | Compound Info | ||
| Synonyms |
AZD7687; 1166827-44-6; CHEMBL2178944; CHEMBL2178953; AZD-7687; AZD 7687; UNII-6QTJ9P2NYT; 6QTJ9P2NYT; SCHEMBL2252415; SCHEMBL5532381; SCHEMBL2252417; GTPL7827; SCHEMBL2255196; DTXSID60655297; YXFNPRHZMOGREC-SHTZXODSSA-N; 3466AH; ZINC43206395; BDBM50399684; BDBM50399710; AZD 7687;AZD-7687; ZINC101581684; AKOS030526281; CS-1026; NCGC00378858-01; HY-15497; KB-144428; W-5990; {4-[4-(6-Carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid; {trans-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid
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| Activity |
IC50 > 300000 nM
|
[8] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors. Bioorg Med Chem Lett. 2013 Feb 15;23(4):985-8. | ||||
| REF 2 | Discovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1686-1692. | ||||
| REF 3 | Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors. J Med Chem. 2015 Dec 10;58(23):9345-53. | ||||
| REF 4 | Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors. ACS Med Chem Lett. 2014 Mar 1;5(5):544-9. | ||||
| REF 5 | 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 6 | Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem. 2011 Apr 14;54(7):2433-46. | ||||
| REF 7 | Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72. | ||||
| REF 8 | 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. | ||||
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