Serine hydrolases
Profile serine hydrolase activity and inhibitor selectivity at the depth your program needs.
Use activity-based profiling to compare inhibitor activity across serine hydrolases, from rapid gel-based assessment to deeper mass-spectrometry profiling in living cells. The choice of readout depends on the stage of your development and the desired level of analytical depth.
Gel-based profiling
Fast, focused profiling for larger compound sets.
Gel-based profiling provides a simpler, faster and lower-cost way to compare serine hydrolase inhibitors. It is particularly useful earlier in a programme, when you want to evaluate a larger number of compounds before selecting which should move into deeper profiling.
Typical coverage: approximately 10–15 quantifiable serine hydrolases.
Best suited for:
- Earlier-stage inhibitor profiling
- Comparing larger compound sets
- Enzymatic activity readouts
- Rapid assessment of selected serine hydrolase targets
Mass spectrometry profiling
Greater depth across the serine hydrolase family.
Once a smaller set of inhibitors has been selected, mass spectrometry-based chemical proteomics provides a much deeper view of inhibitor activity and selectivity. Profiling can be performed in living cells, allowing target engagement to be studied in a more biologically relevant environment.
Omivera has achieved coverage of approximately 100 serine hydrolases in live-cell profiling across three different cell lines.
Best suited for:
- Detailed inhibitor selectivity profiling
- Smaller, prioritised compound sets
- Broader serine hydrolase coverage
- Live-cell target engagement studies
- Comparing activity in lysate and living cells
1. Compare compounds
Use gel-based profiling to assess a larger set of inhibitors quickly.
2. Prioritise candidates
Identify the compounds that warrant more detailed investigation.
3. Profile in greater depth
Use mass spectrometry to assess activity across a broader range of serine hydrolases.
4. Activity in living cells
Generate a more detailed picture of how selected inhibitors behave in a cellular environment.
Activity-based serine hydrolase profiling is supported by published work using the lysate-based approach.
