ArticleACS medicinal chemistry letters2016
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
3 citing papers in PubMed, 14 citations in OpenAlex.
- Pyridine Derivatives: A Comprehensive Review of Their Potential as Anti-Diabetic Agents.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Insights to the emerging potential of glucokinase activators as antidiabetic agent.Pharmaceutical patent analyst · 2024Review
- 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.ACS medicinal chemistry letters · 2016Article
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Authors and funding
23 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glucokinase (GK) catalyzes the phosphorylation of glucose to glucose-6-phosphate. We present the structure-activity relationships leading to the discovery of AM-2394, a structurally distinct GKA. AM-2394 activates GK with an EC50 of 60 nM, increases the affinity of GK for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes.
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