PMID

Data

Article Title

Organization

Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist.

Cadila Healthcare

Discovery of the imidazole-derived GPR40 agonist AM-3189.

Amgen

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.

Merck Research Laboratories

Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.

Merck Research Laboratories

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

Merck Research Laboratories

Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.

Neurocrine Biosciences

Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.

Neurocrine Biosciences

Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.

Neurocrine Biosciences

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.

Merck Research Laboratories

Discovery of a beta-MSH-derived MC-4R selective agonist.

Eli Lilly

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

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.

Merck

Discovery of a novel potent GPR40 full agonist.

Janssen Research & Developmen

Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid ?-Fluorination.

Janssen Research & Development

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

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

On-chip fragment-based approach for discovery of high-affinity bivalent inhibitors.

Antibiotics Laboratory