Real-Time NanoBRET Target Engagement Data for BET-Targeting PROTACs

Alexander Engstrom published a dataset on figshare in May 2026 detailing a method for measuring membrane permeability of PROTACs and E3 ligase ligands. The data likely contains quantitative permeability rates measured using NanoBRET live-cell target engagement, comparing results to traditional transwell assays. It focuses on BET-targeting degraders with subtle structural changes.

Use Cases

• Quantifying permeability-activity relationships based on real-time NanoBRET target engagement data.
• Comparing membrane permeability rates between PROTACs based on subtle structural changes described.
• Guiding rational PROTAC design based on cytosolic access measurements.
• Validating new permeability assays against traditional transwell system results.

Strengths

• Data enables permeability profiling of PROTACs considered unmeasurable in transwell assays.
• Method quantifies permeability directly into the cytosol of living cells.
• Dataset is small (16.6 KB), facilitating quick download and initial exploration.

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• Description metadata is limited; actual data quality requires manual inspection after download.

Provenance

Source

figshare

Collection Method

Experimental data from NanoBRET live-cell target engagement assays.

Freshness

Last updated 2026-05-15 18:11:20; freshness should be verified.