Drawing on a wealth of experience in assay design and development, Axcelead assists client’s problems in the assay construction with in-depth expertise and innovative ideas for achieving optimum system design and HTS.
HTS campaign achievement
Axcelead achieves a high success rate with the design and development of screening strategies in nearly 700 projects. We have extensive experience and expertise with problem-solving in assay construction and HTS campaign across a wide range of target classes. We provide a comprehensive suite of services, from material preparations such as recombinant proteins and stable cell lines to assay construction, HTS campaign, hit profiling, and hit expansion.You would count on Axcelead with an easy mind when finding hit and lead compound.
Assay construction strategies for complicated and challenging targets
We propose suitable platforms optimized to target class and specific client objectives.
| Platform | Application |
|---|---|
| Rapidfire MS | Compound screen using robust enzyme assays to detect the changes in the molecular weight of reaction products |
| AS-MS | Binder screen for targets (typically RNA) that are difficult to detect by biochemical assay |
| GPCR platform | Screen of orphan GPCR targeted drugs, biased ligands, and allosteric modulators |
| HTS using Syncropatch system for ion channel target class | Ion channel drug discovery by monitoring the electrophysiological activity |
| HiBit system | Screen of protein expression and degradation regulators |
| Phenotypic screening using iPS differentiated cells, primary cells and/or spheroid culture | Development of disease-relevant cell-based assays Screening of the compounds that have novel MOA |
Projects
Screen for GPCR biased ligands
In the GPCR target drug field, biased ligands, which selectively regulate cell signals,are focused on as pharmaceutical candidates with fewer side effects.
Axcelead boasts extensive experience and expertise with GPCR targeted drug exploration platforms that are used to find compounds with distinctive profiles, such as biased ligands. For example, we have successfully generated Gs signal selective agonist hits for GPR39. We can assist with chemotype priority ranking using a range of analysis techniques, such as AS-MS binding with VLP, species difference, binding characteristics, and kinetics for hit profiling.
HTS primary assay achievement
GPR39 positive allosteric modulator exploration
Using RapidFire MS to identify enzyme inhibitors
RapidFire MS is a mass spectrometry system designed for rapid screening. Mass spectrometry can be used to design detection systems for complex targets such as lipid enzymes, which are less amenable to assay systems and thereby generate robust HTS. Axcelead has already completed several projects using RapidFire MS to generate hits from HTS. In one particular project, for example, we used RapidFire MS for quantitative measurement of NAD+ and NADH to explore lactate dehydrogenase LDHB inhibitor hits, resulting in the first ever LDHB selective allosteric inhibitor.
Axcelead — for all your assay needs!