Non-prostanoid EP4 Agonist Data for Inflammatory Bowel Disease Treatment

A high-throughput screening campaign identified a novel non-prostanoid chemotype for the EP4 receptor, a target linked to intestinal homeostasis. Lead compound 11a demonstrated efficacy in a mouse model of inflammatory bowel disease and was profiled in pharmacokinetic studies. The dataset, authored by Heidi L. Perez, was last updated in April 2026.

Use Cases

• Optimize lead compound 11a using structure-activity relationship data from the screening campaign.
• Validate EP4 agonist efficacy by analyzing results from the mouse model of inflammatory bowel disease.
• Assess pharmacokinetic properties and hemodynamic effects using data from the mouse pharmacokinetic study.
• Investigate binding mechanisms using insights from high-throughput mutagenesis and computational modeling of the PGE2 site.

Strengths

• Data includes results from a high-throughput screening campaign, indicating a systematic discovery process.
• Lead compound validation includes both in vivo efficacy in a mouse model and pharmacokinetic profiling.

Limitations

• Dataset size is only 7.0 KB, suggesting a very limited scope of data points or summary results.
• All experimental data is derived from mouse models, limiting direct translation to human biology.
• Specific numerical data, such as row counts or quantitative assay results, are not provided in the description.

Provenance

Source

Heidi L. Perez via figshare.

Collection Method

High-throughput screening, structure-activity relationship studies, mouse model experiments, pharmacokinetic profiling, mutagenesis, and computational modeling.

Freshness

Last updated in April 2026.