121 articles for thisTarget
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Design, synthesis and structure-activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker.
China Pharmaceutical University
Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
Shanghai Institute of Materia Medica
Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist.
Glaxosmithkline
Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835.
Saint Petersburg State University
Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.
Merck
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with
Merck
GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space.
Shanghai University
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Merck
Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835.
Saint Petersburg State University
Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity.
University of Southern Denmark
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.
East China Normal University
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
University of Southern Denmark
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold.
Saint Petersburg State University
Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.
China Pharmaceutical University
Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
China Pharmaceutical University
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy.
University of Southern Denmark
Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
China Pharmaceutical University
Design, synthesis, and biological evaluation of novel thiazolidinediones as PPAR¿/FFAR1 dual agonists.
Suez Canal University
Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
China Pharmaceutical University
Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
China Pharmaceutical University
Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558.
Daiichi Sankyo
Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40).
Enamine
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
China Pharmaceutical University
Homology modeling and explicit membrane molecular dynamics simulation to delineate the mode of binding of thiazolidinediones into FFAR1 and the mechanism of receptor activation.
Suez Canal University
Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists.
Daiichi Sankyo
Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
University of Southern Denmark
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Amgen
Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability.
University of Southern Denmark
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.
University of Southern Denmark
Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties.
University of Southern Denmark
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.
Takeda Pharmaceutical
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
Takeda Pharmaceutical
Identification of fused-ring alkanoic acids with improved pharmacokinetic profiles that act as G protein-coupled receptor 40/free fatty acid receptor 1 agonists.
Takeda Pharmaceutical
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.
Merck Research Laboratories
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.
TBA
Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists.
Takeda Pharmaceutical
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Merck Research Laboratories
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists.
Pfizer
Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.
Nagoya City University
Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.
Piramal Life Sciences
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.
University of Southern Denmark
Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening.
National Institute of Diabetes and Digestive and Kidney Diseases
Bidirectional, iterative approach to the structural delineation of the functional"chemoprint" in GPR40 for agonist recognition.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Guangdong Pharmaceutical University
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Bristol Myers Squibb
Current anti-diabetic agents and their molecular targets: A review.
University of Kwazulu-Natal
Optimization of First-in-Class Dual-Acting FFAR1/FFAR4 Allosteric Modulators with Novel Mode of Action.
University of Copenhagen
GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.
University of Siena
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
Guangdong Pharmaceutical University
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
Guangdong Pharmaceutical University
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.
University of Siena
Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.
Sungkyunkwan University
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).
Lilly Research Laboratories
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
Dalian Institute of Chemical Physics
Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
China Pharmaceutical University
Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.
East China Normal University
Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.
Guangdong Pharmaceutical University
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
Janssen Research & Development
Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
China Pharmaceutical University
Design, synthesis and biological activity of deuterium-based FFA1 agonists with improved pharmacokinetic profiles.
Guangdong Pharmaceutical University
Synthesis and activity of small molecule GPR40 agonists.
Glaxosmithkline Research and Development
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
Guangdong Pharmaceutical University
Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
East China Normal University
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
Peking Union Medical College
Nitric oxide donor-based FFA1 agonists: Design, synthesis and biological evaluation as potential anti-diabetic and anti-thrombotic agents.
Guangdong Pharmaceutical University
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.
China Pharmaceutical University
Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
Guangdong Pharmaceutical University
GPR40 Receptor Agonists for the Treatment of Type 2 Diabetes and Related Diseases.
Therachem Research Medilab
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
Amgen Discovery Research
Continued SAR exploration of 1,2,4-thiadiazole-containing scaffolds in the design of free fatty acid receptor 1 (GPR40) agonists.
Saint Petersburg State University
Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
China Pharmaceutical University
Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
Janssen Research and Development
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
Guangdong Pharmaceutical University
Design, synthesis and structure-activity relationship studies of GPR40 agonists containing amide linker.
Chinese Academy of Sciences
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.
Merck
SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.
Sungkyunkwan University
Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.
Janssen Research and Development
Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.
Suez Canal University
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Bristol-Myers Squibb
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy.
Astrazeneca
Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.
Eli Lilly
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Bristol-Myers Squibb
Diindolylmethane Derivatives: Potent Agonists of the Immunostimulatory Orphan G Protein-Coupled Receptor GPR84.
University of Bonn
1,3-DIHYDRO-2H-PYRROLO[3,4-C]PYRIDINE DERIVATIVES AS GABAA A5 RECEPTOR MODULATORS
Richter Gedeon
Combinations comprising substituted imidazo[1,5-a]pyrazinones as PDE1 inhibitors
H. Lundbeck
Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
Shanghai Yingli Pharmaceutical
Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
Jiangsu Hansoh Pharmaceutical
Chrysophaentin analogs that inhibit FtsZ protein
The United States of America, As Represented By The Secretary, Department of Health and Human Services