Add to ORKGThe identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound 1, found in a phenotypic screening campaign, was transformed into compound 2 with good activity on both the rat and human GPR39 receptor. This compound was further optimized to improve ligand efficiency and pharmacokinetic properties to yield GPR39 agonists for the potential oral treatment of type 2 diabetes. Thus, compound 3 is the first potent GPR39 agonist (EC50s ≤ 1nM for human and rat receptor) that is orally bioavailable in mice and robustly induced acute GLP-1 levels
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for ty...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activati...
<div><p>G protein-coupled receptor 119 (GPR119) is highly expressed in pancreatic β cells and entero...
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound <b>...
G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in ente...
With growing needs for new antidiabetic drugs which are safe and effective alone or in combination w...
Screening hit 5 was identified in a biochemical screen for GPR119 agonists. Compound 5 was structura...
G protein-coupled receptor 119 (GPR119) is highly expressed in pancreatic β cells and enteroendocrin...
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...
GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cell...
Activation of the G-protein coupled receptor (GPCR) Takeda G-protein receptor 5 (TGR5), also known a...
Type 2 diabetes is characterized by impaired glucose homeostasis due to defects in insulin secretion...
GPR40 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR40 a...
<div><p>Type 2 diabetes (T2D) occurs when there is insufficient insulin release to control blood glu...
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for ty...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activati...
<div><p>G protein-coupled receptor 119 (GPR119) is highly expressed in pancreatic β cells and entero...
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound <b>...
G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in ente...
With growing needs for new antidiabetic drugs which are safe and effective alone or in combination w...
Screening hit 5 was identified in a biochemical screen for GPR119 agonists. Compound 5 was structura...
G protein-coupled receptor 119 (GPR119) is highly expressed in pancreatic β cells and enteroendocrin...
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...
GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cell...
Activation of the G-protein coupled receptor (GPCR) Takeda G-protein receptor 5 (TGR5), also known a...
Type 2 diabetes is characterized by impaired glucose homeostasis due to defects in insulin secretion...
GPR40 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR40 a...
<div><p>Type 2 diabetes (T2D) occurs when there is insufficient insulin release to control blood glu...
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for ty...
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activati...
<div><p>G protein-coupled receptor 119 (GPR119) is highly expressed in pancreatic β cells and entero...