A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic acid, a key pharmacophore for GPR40. Addition of a 4-<i>cis</i>-CF<sub>3</sub> to the pyrrolidine improves the human GPR40 binding <i>K</i><sub>i</sub> and agonist efficacy. After further optimization, the discovery of a minor enantiomeric impurity with agonist activity led to the finding that enantiomers <b>(</b><i><b>R,R</b></i><b>)-68</b> and <b>(</b><i><b>S,S</b></i><b>)-68</b> have differential effects on the radioligand used for the binding assay, with <b>(</b><i><b>R,R</b></i><b>)-68</b> potentiating the radioligand and <b>(</b><i><b>S,S</b...
GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to it...
Agonists of GPR40 (FFA1) have been proposed as a means to treat type 2 diabetes. Through lead optimi...
We recently reported the discovery of a potent GPR40 full agonist AM-1638 (<b>1</b>). Herein, we des...
GPR40 is a G-protein-coupled receptor which mediates fatty acid-induced glucose-stimulated insulin s...
GPR40 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR40 a...
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes ...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activati...
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound <b>...
GPR40 is a free fatty acid receptor that has been shown to regulate glucose-dependent insulin secret...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets and enteroend...
GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cell...
G-protein coupled receptors 40 and 120 (GPR40 and GPR120) are increasingly emerging as potential the...
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound 1, ...
With growing needs for new antidiabetic drugs which are safe and effective alone or in combination w...
G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in ente...
GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to it...
Agonists of GPR40 (FFA1) have been proposed as a means to treat type 2 diabetes. Through lead optimi...
We recently reported the discovery of a potent GPR40 full agonist AM-1638 (<b>1</b>). Herein, we des...
GPR40 is a G-protein-coupled receptor which mediates fatty acid-induced glucose-stimulated insulin s...
GPR40 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR40 a...
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes ...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activati...
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound <b>...
GPR40 is a free fatty acid receptor that has been shown to regulate glucose-dependent insulin secret...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets and enteroend...
GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cell...
G-protein coupled receptors 40 and 120 (GPR40 and GPR120) are increasingly emerging as potential the...
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound 1, ...
With growing needs for new antidiabetic drugs which are safe and effective alone or in combination w...
G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in ente...
GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to it...
Agonists of GPR40 (FFA1) have been proposed as a means to treat type 2 diabetes. Through lead optimi...
We recently reported the discovery of a potent GPR40 full agonist AM-1638 (<b>1</b>). Herein, we des...