Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T51385 | Target Info | |||
| Target Name | G-protein coupled receptor 120 (GPR120) | ||||
| Synonyms |
PGR4; Omega3 fatty acid receptor 1; Omega-3 fatty acid receptor 1; O3FAR1; Gprotein coupled receptor PGR4; Gprotein coupled receptor GT01; Gprotein coupled receptor 129; GPR129; G-protein coupled receptor PGR4; G-protein coupled receptor GT01; G-protein coupled receptor 129; Free fatty acid receptor 4
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| Target Type | Literature-reported Target | ||||
| Gene Name | FFAR4 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 32 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
12-hydroxylauric acid
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Investigative | Compound Info | ||
| Synonyms |
12-Hydroxydodecanoic acid; 505-95-3; 12-hydroxylauric acid; 12-hydroxy-dodecanoic acid; Dodecanoic acid, 12-hydroxy-; omega-Hydroxydodecanoic acid; 12-hydroxy lauric acid; Dodecanoic acid,12-hydroxy-; CHEBI:39567; ZDHCZVWCTKTBRY-UHFFFAOYSA-N; NSC664211; AK-51216; omega-hydroxydodecanoate; J-504146; 12H; Sabinic acid; EINECS 208-025-0; omega-OH lauric acid; NSC 159293; NSC 664211; omega hydroxy dodecanoate; omega-OH dodecanoic acid; AC1L2WIA; omega-hydroxy lauric acid; AC1Q7CPY; ACMC-209x3w; 12-hydroxy dodecanoic acid; omega-hydroxy d
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-hydroxylauric acid
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Investigative | Compound Info | ||
| Synonyms |
3-hydroxy lauric acid
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| Activity |
EC50 ~ 100000 nM
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[1] | |||
| Compound Name |
2-hydroxylauric acid
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Investigative | Compound Info | ||
| Synonyms |
2-OH-C12; 2-hydroxy lauric acid
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[4-[(2-Phenylphenyl)methylamino]phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1773259; BDBM50420152
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| Activity |
EC50 = 51286.14 nM
|
[2] | |||
| Compound Name |
3-[4-(Benzylamino)phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
3-(4-(benzylamino)phenyl)propanoic acid; carboxylic acid agonist, 34; CHEMBL234834; SCHEMBL2596544; BDBM22517
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| Activity |
EC50 = 57543.99 nM
|
[2] | |||
| Compound Name |
3-(4-{[(4-Phenylphenyl)methyl]amino}phenyl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
carboxylic acid agonist, 19; CHEMBL234269; BDBM22502
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| Activity |
EC50 = 58884.37 nM
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[2] | |||
| Compound Name |
3-[2-Fluoro-4-[2-[3-(methylsulfonylmethyl)phenyl]ethynyl]phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386367; SCHEMBL12985288; BDBM50434300
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| Activity |
EC50 = 64565.42 nM
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[3] | |||
| Compound Name |
3-[6-(2-Phenylethynyl)pyridin-3-yl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386357; BDBM50434310
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| Activity |
EC50 = 91201.08 nM
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[3] | |||
| Compound Name |
3-[4-[[3-(2,6-Dimethylphenyl)phenyl]methylamino]-2-fluorophenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2164241; BDBM50395073
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| Activity |
EC50 = 93325.43 nM
|
[4] | |||
| Compound Name |
3-[2-Fluoro-4-[2-[3-(2-methylsulfonylethoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386369; BDBM50434298
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-[2-Fluoro-4-[2-[2-(2-methylsulfonylethoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386368; BDBM50434299
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
10-Hydroxylauric acid
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Investigative | Compound Info | ||
| Synonyms |
10-hydroxydodecanoic Acid; 10-hydroxy-dodecanoic acid; (omega-2)-hydroxylauric acid; SCHEMBL974964; CHEMBL4280780
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[4-(3-Methylbut-3-en-1-ynyl)phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3785544; BDBM50157613
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
11-Hydroxylauric acid
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Investigative | Compound Info | ||
| Synonyms |
11-Hydroxydodecanoic acid; Dodecanoic acid, 11-hydroxy-; 11-hydroxy-dodecanoic acid; Dodecanoic acid,11-hydroxy-; 11-HYDROXY LAURIC ACID; SCHEMBL1882126; CHEMBL4291425; CTK4G8742; DTXSID00954211; LMFA01050165; AKOS027447761; J-018745; Q27146452
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
6-Hydroxydodecanoic acid
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Investigative | Compound Info | ||
| Synonyms |
6-hydroxylauric acid; SCHEMBL667755; CHEMBL4279005; CTK8I4014; DTXSID60275398
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[4-[2-(Cyclohexen-1-yl)ethynyl]phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3786524; BDBM50157603
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-(3-Fluoro-5-phenylmethoxyphenyl)-3H-1,2-benzothiazole 1,1-dioxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3958418; SCHEMBL1724414; BDBM50196395
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| Activity |
EC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
3-[5-(2-Phenylethynyl)pyridin-2-yl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386356; BDBM50434311
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-[2-Fluoro-4-[2-[3-(3-methylsulfonylpropoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386371; BDBM50434296
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-[2-Fluoro-4-[2-[2-(methylsulfonylmethyl)phenyl]ethynyl]phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386366; SCHEMBL12984540; BDBM50434301
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-[2-Fluoro-4-(3-methylbut-3-en-1-ynyl)phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3787463; SCHEMBL12985313; BDBM50157615
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
3-[4-[2-(1-Hydroxycyclohexyl)ethynyl]phenyl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3787165; BDBM50157602
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
9-Hydroxy-dodecanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
9-hydroxydodecanoic acid; 9-hydroxylauric acid; LMFA01050167; (omega-3)-hydroxylauric acid; SCHEMBL1881322; CHEMBL4288021
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
7-Hydroxylauric acid
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|
Investigative | Compound Info | ||
| Synonyms |
7-hydroxydodecanoic acid; 7-hydroxy-dodecanoic acid; LMFA01050166; SCHEMBL1527361; CHEMBL4287270; C21080; Q27158612
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|
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[2-Fluoro-4-[2-[2-(3-methylsulfonylpropoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2386370; BDBM50434297
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|
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-[4-(2-Cyclopropylethynyl)phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3786964; BDBM50157571
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|
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
5-Hydroxydodecaneoic acid sodium salt
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4294243
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|
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[2-Fluoro-4-[(Z)-5-hydroxy-3-methylpent-3-en-1-ynyl]phenyl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3785413; SCHEMBL12984132; BDBM50157620
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Chembl4246529
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Investigative | Compound Info | ||
| Synonyms |
BDBM50462856
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| Activity |
EC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
3-(4-Ethynylphenyl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3785667; SCHEMBL1550658; BDBM50157566
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| Activity |
EC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Sodium 4-hydroxydodecanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4283659; SCHEMBL10913917
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
8-Hydroxydodecanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
8-hydroxylauric acid; Dodecanoic acid, 8-hydroxy-; 8-hydroxy-dodecanoic acid; (omega-4)-hydroxylauric acid; SCHEMBL1882579; CHEMBL4277376; CTK0A8412; DTXSID20560515
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids on FFA1, FFA4 and GPR84. Medchemcomm. 2017 May 12;8(6):1360-1365. | ||||
| REF 2 | Discovery of a potent and selective GPR120 agonist. J Med Chem. 2012 May 10;55(9):4511-5. | ||||
| REF 3 | Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013 May 9;4(5):441-445. | ||||
| REF 4 | Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J Med Chem. 2012 Jul 26;55(14):6624-8. | ||||
| REF 5 | Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy. J Med Chem. 2016 Mar 24;59(6):2841-6. | ||||
| REF 6 | Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity. J Med Chem. 2016 Oct 13;59(19):8868-8878. | ||||
| REF 7 | Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2599-2604. | ||||
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