Orforglipron Derivatives: Small-Molecule GLP-1 Receptor Agonists

Orforglipron derivatives 17-P1 and 24-P1 are small-molecule agonists for the glucagon-like peptide-1 receptor (GLP-1R). The dataset likely contains results from structure–activity relationship studies, including EC50 values, permeability measurements, and oral bioavailability percentages. Mengya Li uploaded the data to figshare on 2026-05-06.

Use Cases

• Compare in vitro potency of drug candidates based on hGLP-1R agonistic EC50 values.
• Evaluate drug permeability based on Caco-2 Papp measurements.
• Assess oral pharmacokinetics based on mouse bioavailability percentages.
• Analyze glucose-lowering and food-intake-suppressing effects based on in vivo results.

Strengths

• Includes specific potency measurements (EC50 = 0.64 and 0.53 nM).
• Provides concrete permeability data (Caco-2 Papp = 2.83 and 4.75 nm/s).
• Reports quantitative oral bioavailability results in mice (54.0% and 72.4%).

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• The dataset is very small (509.0 KB), indicating limited scope.

Provenance

Source

figshare

Collection Method

Likely contains experimental data from systematic structure–activity relationship studies.

Freshness

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