Page last updated: 2024-08-07 15:22:31
Free fatty acid receptor 1
A free fatty acid receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O14842]
Synonyms
G-protein coupled receptor 40
Research
Bioassay Publications (57)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 6 (10.53) | 29.6817 |
2010's | 45 (78.95) | 24.3611 |
2020's | 6 (10.53) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
gw9508 | Homo sapiens (human) | Ki | 0.2188 | 1 | 1 |
tak-875 | Homo sapiens (human) | Ki | 0.0183 | 2 | 2 |
amg-837 | Homo sapiens (human) | Ki | 0.0219 | 2 | 2 |
tug-469 | Homo sapiens (human) | Ki | 0.0059 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
gw9508 | Homo sapiens (human) | Activity | 0.2230 | 1 | 1 |
am 1638 | Homo sapiens (human) | fEC50 | 0.0001 | 1 | 1 |
Succinct synthesis of saturated hydroxy fatty acids and MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.ACS medicinal chemistry letters, , Jun-09, Volume: 7, Issue:6, 2016
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.ACS medicinal chemistry letters, , Sep-13, Volume: 3, Issue:9, 2012
Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 29, Issue:6, 2019
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 18, Issue:24, 2008
Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Discovery of a potent and selective GPR120 agonist.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
[no title available]Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 30, Issue:24, 2020
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 28, Issue:15, 2018
SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Homology modeling and explicit membrane molecular dynamics simulation to delineate the mode of binding of thiazolidinediones into FFAR1 and the mechanism of receptor activation.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
Discovery of a potent and selective GPR120 agonist.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.ACS medicinal chemistry letters, , Oct-14, Volume: 1, Issue:7, 2010
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Synthesis and activity of small molecule GPR40 agonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
Design and Identification of a GPR40 Full Agonist (Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.Bioorganic & medicinal chemistry, , 07-01, Volume: 28, Issue:13, 2020
Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 29, Issue:6, 2019
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.ACS medicinal chemistry letters, , Jan-10, Volume: 10, Issue:1, 2019
Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.Bioorganic & medicinal chemistry, , 02-01, Volume: 26, Issue:3, 2018
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.European journal of medicinal chemistry, , Nov-05, Volume: 159, 2018
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.Bioorganic & medicinal chemistry, , 12-01, Volume: 26, Issue:22, 2018
Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 28, Issue:18, 2018
Nitric oxide donor-based FFA1 agonists: Design, synthesis and biological evaluation as potential anti-diabetic and anti-thrombotic agents.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.ACS medicinal chemistry letters, , Dec-14, Volume: 8, Issue:12, 2017
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
[no title available]ACS medicinal chemistry letters, , Dec-08, Volume: 7, Issue:12, 2016
The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 23, Issue:1, 2015
Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.Bioorganic & medicinal chemistry, , Nov-15, Volume: 23, Issue:22, 2015
Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.European journal of medicinal chemistry, , Nov-05, Volume: 159, 2018
[no title available]ACS medicinal chemistry letters, , Dec-08, Volume: 7, Issue:12, 2016
Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Discovery of the imidazole-derived GPR40 agonist AM-3189.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
Optimization of GPR40 Agonists for Type 2 Diabetes.ACS medicinal chemistry letters, , May-08, Volume: 5, Issue:5, 2014
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.ACS medicinal chemistry letters, , Sep-13, Volume: 3, Issue:9, 2012
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Discovery of a potent and selective GPR120 agonist.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.ACS medicinal chemistry letters, , Oct-14, Volume: 1, Issue:7, 2010
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 30, Issue:24, 2020
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Discovery of a potent and selective GPR120 agonist.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
[no title available]Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Design and Identification of a GPR40 Full Agonist (Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 29, Issue:14, 2019
Discovery of a novel potent GPR40 full agonist.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.ACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.ACS medicinal chemistry letters, , Feb-09, Volume: 8, Issue:2, 2017
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.ACS medicinal chemistry letters, , Sep-13, Volume: 3, Issue:9, 2012
Enables
This protein enables 3 target(s):
Target | Category | Definition |
G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
lipid binding | molecular function | Binding to a lipid. [GOC:ai] |
bioactive lipid receptor activity | molecular function | Combining with a bioactive lipid and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. A bioactive lipid is a lipid for which changes in lipid levels result in functional consequences in a variety of cellular processes. [GOC:bf, GOC:mah, PMID:12215548, PMID:18216770] |
Located In
This protein is located in 1 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 11 target(s):
Target | Category | Definition |
phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
insulin secretion | biological process | The regulated release of proinsulin from secretory granules accompanied by cleavage of proinsulin to form mature insulin. In vertebrates, insulin is secreted from B granules in the B cells of the vertebrate pancreas and from insulin-producing cells in insects. [GOC:mah, ISBN:0198506732] |
negative regulation of interleukin-1 beta production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-1 beta production. [GOC:mah] |
glucose homeostasis | biological process | Any process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators] |
positive regulation of calcium ion transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
response to fatty acid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a fatty acid stimulus. [GOC:lp] |
ion channel modulating, G protein-coupled receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, where the pathway proceeds through activation or inhibition of an ion channel. [GOC:dos] |
ligand-gated ion channel signaling pathway | biological process | The series of molecular signals initiated by activation of a ligand-gated ion channel on the surface of a cell. The pathway begins with binding of an extracellular ligand to a ligand-gated ion channel and ends with a molecular function that directly regulates a downstream cellular process, e.g. transcription. [GOC:bhm, PMID:25869137] |
positive regulation of insulin secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of insulin. [GOC:mah] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |