Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T93788 | Target Info | |||
| Target Name | Glucose-dependent insulinotropic receptor (GPR119) | ||||
| Synonyms |
GPR119; G-protein coupled receptor 119
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| Target Type | Successful Target | ||||
| Gene Name | GPR119 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 2 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4288001
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50466485
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Tert-butyl 4-[3-(4-methylsulfonylphenoxy)cyclohexyl]oxypiperidine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3598116
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| Activity |
EC50 ~ 100000 nM
|
[2] | |||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Tert-butyl 4-[5-[(3-methylsulfonylpyridin-4-yl)methoxy]pyrimidin-2-yl]piperazine-1-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2086681; SCHEMBL1448605; BDBM50420844
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| Activity |
EC50 > 30000000 nM
|
[3] | |||
| Compound Name |
3-Fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2204974; SCHEMBL876891; BDBM50400777
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| Activity |
EC50 = 100000000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles. Bioorg Med Chem. 2018 Dec 1;26(22):5780-5791. | ||||
| REF 2 | Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series. Bioorg Med Chem Lett. 2015 Aug 1;25(15):3034-8. | ||||
| REF 3 | Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation. J Med Chem. 2012 Jun 14;55(11):5361-79. | ||||
| REF 4 | GPR119 Modulators for the Treatment of Diabetes, Obesity, and Related Diseases: Patent Highlight. ACS Med Chem Lett. 2012 Oct 10;3(12):955-8. | ||||
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