Comparison of (bio-)transformation methods for the generation of metabolite-like compound libraries of p38α MAP kinase inhibitors using high-resolution screening

- p38α MAP kinase inhibitors were modified by hydrogen peroxide or visible light.
- Integrated approach for modification, separation, structure and bioaffinity.
- Comparison of methods for generation of metabolite-like lead libraries.
- Many bioactive, mostly more hydrophilic conversion products were yielded.
- High-resolution screening excellent approach for library assessment and initial SAR.