Discovery of Small-Molecule GLP‑1 Receptor Agonists with Improved Oral Pharmacokinetics Ba

A dataset likely contains structural and pharmacokinetic data for novel small-molecule GLP-1 receptor agonists derived from orforglipron. It was authored by Mengya Li and uploaded to figshare on May 6, 2026. The data describes compounds designed to overcome the oral exposure plateau of the parent molecule.

Use Cases

• Structure-activity relationship analysis based on modifications at the 4-fluoro-1-methylindazole site
• Predicting oral bioavailability based on permeability measurements (Caco-2 Papp)
• Evaluating in vivo efficacy based on glucose-lowering and food-intake-suppressing effects
• Comparing potency based on subnanomolar hGLP-1R agonistic activity (EC50)
• Optimizing drug candidates based on physicochemical property improvements

Strengths

• Includes specific potency measurements for compounds 17-P1 and 24-P1 (EC50 = 0.64 and 0.53 nM)
• Provides concrete permeability data (Caco-2 Papp = 2.83 and 4.75 nm/s vs 0.14 nm/s)
• Reports oral bioavailability percentages in mice (54.0% and 72.4% vs 6.4%)

Limitations

• Column-level documentation is absent; field semantics must be inferred after download
• Row count is unknown, which may limit suitability assessment
• The dataset is small (508.8 KB), indicating limited scope

Provenance

Source

figshare

Freshness

Last updated 2026-05-06 16:07:05; freshness should be verified