Assays for Measuring the Cell Permeability of Proteolysis-Targeting Chimeras (PROTACs): Performance, Correlations, Applicability and Recommendations
Christina Brenner, Yunhai Cui, Denis Schmidt, Johannes Kirchmair, Lu Tan, Nina Braun · 2026
Read Assays for Measuring the Cell Permeability of Proteolysis-Targeting Chimeras (PROTACs): Performance, Correlations, Applicability and Recommendations by Christina Brenner, Yunhai Cui, Denis Schmidt, Johannes Kirchmair, Lu Tan, Nina Braun (2026) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-13343507.txt.
Description
Christina Brenner and colleagues tested PROTAC permeability tests in 2026 across 3,271 PROTAC drugs spanning varied chemistry and targets. Most PROTACs break Rule of Five limits, and crossing cell walls is key to their drug success. Drugs were measured in up to three test types: NanoBRET target binding, Caco-2 permeability, and P-glycoprotein efflux tests.
Strong links between NanoBRET readouts and other tests emerged in set chemical spaces, while trust varied outside them. The work maps where each test can be trusted and where it misleads. Drug makers gain a hands on guide for picking permeability tests in PROTAC drug design.
Catalog record
| CREATOR | Christina Brenner, Yunhai Cui, Denis Schmidt, Johannes Kirchmair, Lu Tan, Nina Braun |
|---|---|
| YEAR | 2026 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 49 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |