Compounds > tug-891
Page last updated: 2024-11-13

tug-891

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

GPU-028: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID57522038
CHEMBL ID2058533
SCHEMBL ID15264542
MeSH IDM0589704

Synonyms (32)

Synonym
CHEMBL2058533 ,
bdbm50420167
S6775
AKOS016340424
tug 891
tug891
3-(4-{[5-fluoro-2-(4-methylphenyl)phenyl]methoxy}phenyl)propanoic acid
tug-891
gtpl6490
KG-0018
1374516-07-0
SCHEMBL15264542
4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]-benzenepropanoic acid
3-(4-((4-fluoro-4'-methylbiphenyl-2-yl)methoxy)phenyl)propanoic acid
HY-100881
CS-6138
EX-A1220
3-{4-[(4-fluoro-4'-methylbiphenyl-2-yl)methoxy]phenyl}propanoic acid
mfcd22421654
BCP19294
3-(4-((4-fluoro-4'-methyl-[1,1'-biphenyl]-2-yl)methoxy)phenyl)propanoic acid
Q27089037
AMY10839
C72503
gpu-028
3-[4-[[5-fluoro-2-(4-methylphenyl)phenyl]methoxy]phenyl]propanoic acid
AC-36080
ZEC51607
3-{4-[(4-fluoro-4'-methyl-2-biphenylyl)methoxy]phenyl}propanoic a cid
A920732
yn9 ,
3-{4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]phenyl}propanoic acid
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Free fatty acid receptor 1Homo sapiens (human)EC50 (µMol)39.01540.00030.73698.8000AID1367361; AID1699892; AID673112; AID673121
Free fatty acid receptor 4Homo sapiens (human)EC50 (µMol)0.16880.04372.35477.5858AID1313436; AID1367360; AID1699890; AID673111; AID673114
Free fatty acid receptor 4Mus musculus (house mouse)EC50 (µMol)0.01700.01700.01700.0170AID673115
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
phospholipase C-activating G protein-coupled receptor signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationFree fatty acid receptor 1Homo sapiens (human)
insulin secretionFree fatty acid receptor 1Homo sapiens (human)
negative regulation of interleukin-1 beta productionFree fatty acid receptor 1Homo sapiens (human)
glucose homeostasisFree fatty acid receptor 1Homo sapiens (human)
positive regulation of calcium ion transportFree fatty acid receptor 1Homo sapiens (human)
response to fatty acidFree fatty acid receptor 1Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
ligand-gated ion channel signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
positive regulation of insulin secretionFree fatty acid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
negative regulation of cytokine productionFree fatty acid receptor 4Homo sapiens (human)
inflammatory responseFree fatty acid receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayFree fatty acid receptor 4Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayFree fatty acid receptor 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationFree fatty acid receptor 4Homo sapiens (human)
regulation of glucose transmembrane transportFree fatty acid receptor 4Homo sapiens (human)
negative regulation of interleukin-1 beta productionFree fatty acid receptor 4Homo sapiens (human)
ghrelin secretionFree fatty acid receptor 4Homo sapiens (human)
negative regulation of apoptotic processFree fatty acid receptor 4Homo sapiens (human)
positive regulation of osteoblast differentiationFree fatty acid receptor 4Homo sapiens (human)
negative regulation of inflammatory responseFree fatty acid receptor 4Homo sapiens (human)
white fat cell differentiationFree fatty acid receptor 4Homo sapiens (human)
brown fat cell differentiationFree fatty acid receptor 4Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of tasteFree fatty acid receptor 4Homo sapiens (human)
positive regulation of glucagon secretionFree fatty acid receptor 4Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeFree fatty acid receptor 4Homo sapiens (human)
negative regulation of somatostatin secretionFree fatty acid receptor 4Homo sapiens (human)
positive regulation of brown fat cell differentiationFree fatty acid receptor 4Homo sapiens (human)
positive regulation of cold-induced thermogenesisFree fatty acid receptor 4Homo sapiens (human)
cellular response to hormone stimulusFree fatty acid receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayFree fatty acid receptor 4Homo sapiens (human)
hormone secretionFree fatty acid receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityFree fatty acid receptor 1Homo sapiens (human)
lipid bindingFree fatty acid receptor 1Homo sapiens (human)
bioactive lipid receptor activityFree fatty acid receptor 1Homo sapiens (human)
G protein-coupled receptor activityFree fatty acid receptor 4Homo sapiens (human)
fatty acid bindingFree fatty acid receptor 4Homo sapiens (human)
taste receptor activityFree fatty acid receptor 4Homo sapiens (human)
peptide bindingFree fatty acid receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
plasma membraneFree fatty acid receptor 1Homo sapiens (human)
plasma membraneFree fatty acid receptor 1Homo sapiens (human)
lysosomal membraneFree fatty acid receptor 4Homo sapiens (human)
plasma membraneFree fatty acid receptor 4Homo sapiens (human)
ciliumFree fatty acid receptor 4Homo sapiens (human)
endosome membraneFree fatty acid receptor 4Homo sapiens (human)
endocytic vesicleFree fatty acid receptor 4Homo sapiens (human)
ciliary membraneFree fatty acid receptor 4Homo sapiens (human)
plasma membraneFree fatty acid receptor 4Homo sapiens (human)
plasma membraneFree fatty acid receptor 4Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID1699891Agonist activity at human FFA4 receptor expressed in CHO-K1 cells assessed as efficacy of increase in amplitude of dynamic mass redistribution response by DMR assay relative to control2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
AID673118Agonist activity at mouse GPR120 relative to control2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1447427Antagonist activity at human FFAR4 expressed in CHO cells assessed as inhibition of TUG-89-induced beta-arrestin recruitment at 10 uM preincubated for 30 mins followed by TUG-89 addition measured after 90 mins by beta-galactosidase complementation assay
AID673121Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID673123Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay relative to TUG-4242012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1367363Clearance in Sprague-Dawley rat at 10 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID1699890Agonist activity at human FFA4 receptor expressed in CHO-K1 cells assessed as increase in amplitude of dynamic mass redistribution response by DMR assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
AID673116Agonist activity at FFAR2 by [35S]GTPgammaS assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1367360Agonist activity at human FFAR4 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by luminescence assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID1367364Cmax in Sprague-Dawley rat at 10 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID673111Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1367366Half life in Sprague-Dawley rat at 10 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID673114Agonist activity at GPR120 expressed in Flp-In TREx293 cells by calcium assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID673117Agonist activity at FFAR3 by [35S]GTPgammaS assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID673120Agonist activity at FFAR1 expressed in Flp-In TREx cells by calcium assay relative to control2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1367359Plasma clearance in rat2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID1313436Agonist activity at GPR120 (unknown origin) by Fluo-4 AM dye based calcium mobilization assay2016ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.
AID673112Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1367365AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID1699893Selectivity index, ratio of EC50 for agonist activity at human FFA1 receptor expressed in CHO-K1 cells to EC50 for agonist activity at human FFA4 receptor expressed in CHO-K1 cells by DMR assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
AID1367362Selectivity index, ratio of EC50 for human FFAR1 to EC50 for human FFAR42017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID673119Agonist activity at FFAR1 expressed in Flp-In TREx293 cells by calcium assay relative to control2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1699892Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
AID673115Agonist activity at mouse GPR1202012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Discovery of a potent and selective GPR120 agonist.
AID1447425Agonist activity at human FFAR4 expressed in CHO cells assessed as beta-arrestin recruitment at 10 uM after 90 mins by beta-galactosidase complementation assay
AID1367361Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (80.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.98

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index32.98 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index25.55 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
deuterium
Deuterium: The stable isotope of hydrogen. It has one neutron and one proton in the nucleus.		2.1510dihydrogen
docosahexaenoate
efalex: a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement. docosahexaenoic acid : Any C22 polyunsaturated fatty acid containing six double bonds.. docosahexaenoate : A polyunsaturated fatty acid anion that is the conjugate base of docosahexaenoic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.. all-cis-docosa-4,7,10,13,16,19-hexaenoic acid : A docosahexaenoic acid having six cis-double bonds at positions 4, 7, 10, 13, 16 and 19.		2.1310docosahexaenoic acid;
omega-3 fatty acid		algal metabolite;
antineoplastic agent;
Daphnia tenebrosa metabolite;
human metabolite;
mouse metabolite;
nutraceutical
sodium butyrate
[no description available]		2.1310organic sodium saltEC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
alpha-linolenic acid
linolenic acid : A two-membered subclass of octadecatrienoic acid comprising the (9Z,12Z,15Z)- and (6Z,9Z,12Z)-isomers. Linolenic acids are nutrients essential to the formation of prostaglandins and are also used in making paints and synthetic resins.. linolenate : A polyunsaturated fatty acid anion obtained by deprotonation of the carboxy group of either alpha- or gamma-linolenic acid.		2.0710linolenic acid;
omega-3 fatty acid		micronutrient;
mouse metabolite;
nutraceutical
psn 632408
PSN 632408: a GPR119 agonist; structure in first source		2.1310
gw9508
GW9508: structure in first source		2.5320aromatic amine
tak-875
[no description available]		2.5920biphenyls
tug-469
TUG-469: a GPR40 agonist with antidiabetic activity; structure in first source		2.0710
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus, Adult-Onset
[description not available]		02.0710
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		02.0710
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		02.1510