Analysis and Planning
- Team Assembly
- Target access assessment
- Target analysis
- HTS library selection
- Screening cascade defined
- Assays identified
- Structural biology planning
Platform Establishment
- Establishment of protein production
- Establishment of assay systems
- Establishment of structural biology
Library Screening
- Fragment screening
[3k hand-picked fragments] - Range Finder screening
[fragment enriched 41k small molecule library] - Small molecule HTS
[150k high-quality small molecules] - Reporter Displacement
- Enzymatic Assays
- SPR, MST, nanoDSF, nanoBRET, TSA
Hit Confirmation
- Reporter displacement assays
- Binding affinity and kinetic profiling via SPR
- Enzymatic profiling of impact of inhibitors
- MicroScale Thermophoresis binding assays
- Label-free nanoDSF binding assays
- nanoBRET target engagement
- Luminescence interaction analysis using Alpha LISA Screening
- Interaction thermodynamic analysis using Isothermal titration calorimetry
Hit Characterization
- Reporter displacement assays
- Enzymatic Assays
- Luminescence interaction analysis using Alpha LISA Screening
- Binding affinity and kinetic profiling via SPR
- MicroScale Thermophoresis binding assays
- Label-free nanoDSF binding assays
- Interaction thermodynamic analysis using Isothermal titration calorimetry
- nanoBRET target engagement
Structural Elucidation
- X-ray crystallography
- Cryo-EM
Qualified Hits
At the end of the process you will receive the deeply characterized qualified hits,
which meet the project specifications.