How it Works
Active-site Directed Competition Binding Platform Overview
DiscoveRx's proprietary active-site directed competition binding technology affords investigators the ability to leverage a growing portfolio of services against multiple target classes and maximixe the value of novel and chemistry assets through all stages of drug discovery. This robust and reliable assay technology enables accurate, precise, reproducible and quantitative measurements of interactions between test compounds and the target protein.
Platform Benefits & Features
- Rapid turnaround time
- Flexible: screen any number of compounds
- High throughput: >1.7 million interactions/month
- Accurate affinity (Kd) measurements from <100 pM to >10 uM
- ATP not required: delivers true thermodynamic affinity data as opposed to IC50s
- No interference from compound fluorescence
- All assays performed in parallel under standardized conditions as a single experiment
- Accurate, precise, reproducible data
- Technology translates to any protein class with the few requirements
Assay Principle
Compounds that bind the active site and directly (sterically) or indirectly (allosterically) prevent protein binding to the immobilized ligand, will reduce the amount of protein captured on the solid support (Panels A & B). Conversely, test molecules that do not bind the protein have no effect on the amount of protein captured on the solid support (Panel C). Screening “hits” are identified by measuring the amount of protein captured in test versus control samples by using a quantitative, precise and ultra-sensitive qPCR method that detects the associated DNA label (Panel D). In a similar manner, dissociation constants (Kds) for test compound-protein interactions are calculated by measuring the amount of protein captured on the solid support as a function of the test compound concentration.
Panel A Panel B Panel C Panel D
Applications
See how DiscoveRx is using this technology platform to develop assays & screening solutions to different target classes
KINOMEscan Kinase Inhibitor Screening Platform
BROMOscan Bromodomain Inhibitor Assay Panel