Benzofuran Oxoacetic Acid Compounds as EPAC1 Activators

A 2026 study by David Morgan reports the development and evaluation of benzofuran oxoacetic acid compounds as non-nucleotide EPAC1 activators. The dataset includes synthesized analogues, their binding engagement with EPAC isoforms, and cellular assay results measuring Rap1-GTP increases and antifibrotic effects.

Use Cases

• Analyze the binding engagement of specific analogues like DM244, DM357, and DM408 with EPAC1 versus EPAC2 isoforms.
• Evaluate the potency of compounds such as DM243, DM244, and DM245 in attenuating IL-6/STAT3 signaling in human umbilical vascular endothelial cells.
• Compare the inhibitory effects of the benzofuran series on TGF-β1-induced fibroblast-to-myofibroblast transition against known drugs SB525334 and nintedanib.
• Investigate the relationship between C2-diversification in synthesis and the resulting signaling bias or phenotype disconnects observed in cellular assays.

Strengths

• Data originates from a 2026 published scientific study, ensuring recency.
• Includes direct comparisons of novel compounds against established reference drugs SB525334 and nintedanib.
• Reports compound yields (3–7%) and midmicromolar potencies from cellular assays.

Limitations

• The dataset is extremely small at 1.3 KB, indicating limited scope and likely a summary table rather than raw experimental data.
• Specific sample sizes, row counts, and column definitions are unknown, limiting analytical depth.
• Data is confined to the specific chemical series and assays described, with no broader chemical or biological context.

Provenance

Source

figshare, authored by David Morgan.

Collection Method

Convergent chemical synthesis and subsequent biological assays (fluorescent competition, transfected U2OS cell assays, endothelial and fibroblast models).

Time Range

Study published in 2026.

Freshness

Last updated March 2026.

Geography

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