Real-Time NanoBRET Target Engagement Data for PROTAC Permeability

A 2.6 KB dataset published by Alexander Engstrom on May 15, 2026, describing a method to measure membrane permeability of PROTACs and E3 ligase ligands. It contains quantitative permeability profiles for BET-targeting degraders, derived from real-time NanoBRET live-cell target engagement assays. The data aims to rationalize discrepancies in degradation efficiency and cytotoxicity for compounds previously considered unmeasurable.

Use Cases

• Modeling permeability-activity relationships for BET-targeting degraders based on the described permeability rates.
• Comparing permeability measurement methods by benchmarking real-time NanoBRET data against transwell assay results mentioned in the description.
• Guiding structural optimization of PROTACs by analyzing how subtle structural changes correlate with differing permeabilities.
• Validating computational models of cytosolic access for unmodified PROTACs using the quantitative permeability profiles.

Strengths

• Dataset is small (2.6 KB), enabling quick download and inspection.
• Method described provides a direct measure of cytosolic access, a limitation of common assays like PAMPA and Caco-2.
• License (CC-BY-NC-4.0) is clearly specified, defining permissible use.

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• The dataset's scope is limited to BET-targeting PROTACs and related E3 ligase ligands.

Provenance

Source

figshare

Collection Method

Data likely generated from NanoBRET live-cell target engagement assays measuring permeability rates of PROTACs.

Freshness

Last updated 2026-05-15 18:11:21; freshness should be verified.