Menu
Menu
An enthusiastic team of experienced scientists provide you with industry-standard solutions for tailored cellular, biochemical and biophysical assay development, optimization and miniaturisation in order to support your lead discovery projects.
Our scientists have both longstanding and proven experience with assay development on the most challenging targets. We believe each project has unique aspects, and we collaborate with you to deliver both tailored and high-quality assays. Basically, we achieve this by detailed scientific assessment of your project requirements. After that, tailor a proposal ranging from a reliable screening cascade to a stand-alone assay to address your particular needs. No matter how challenging your target is, our scientists will ideate out-of-the-box solutions and propose the best fitting approach in order to develop the right assay suitable for target evaluation, ultra-High Throughput Screening (uHTS), hit triaging and hit-to-lead biological profiling. We have broad experience in a variety of phenotypes and target classes ranging from kinases, GPCRs and ion channels till nuclear receptors, proteases and protein interactions with other proteins or nucleic acids in many therapeutic areas.
We provide a broad range of both label-based and label-free biochemical, cellular and biophysical assays, that are optimised to deliver high-quality data. Our scientists have ample experience in a variety of readout technologies including the most conventional label-based biochemical and cellular readouts such as Fluorescence, FRET/HTRF/TR-FRET, FP, Luminescence, absorption, high-content, phenotypic, as well as label-free MALDI-TOF mass spectrometry biochemical, affinity-based and cellular assays.
We offer a proprietary chemical biology framework in order to identify assay liabilities towards various types of readout interferences along with undesired non-drug-like modes-of-action. We tailor both primary assay conditions and triaging assay cascade in a data-driven manner to guarantee the delivery of high-quality and validated hits.
Pivot Park Screening Centre actively pursues customised solutions for profiling novel classes of small molecule modalities such as PROTACs and molecular glues. We also continuously work towards integrating novel disease models based on patient-derived or Crispr/Cas edited induced Pluripotent Stem Cells (iPSC) models such as cardiomyocytes and neuronal cells into our screening capabilities.
Besides the quality of the library and the primary assay, the success of any uHTS-campaign depends on the post-screen hit-triaging. Particularly because of undesired compound-assay interference leading to false-positive data. The undesired false-positive effects of these compounds disturb the hit selection process, thus requiring orthogonal assay readouts and adjustments in the primary assay conditions.
When organizations run many uHTS assays with the same compound library, such interfering molecules become recognized as “frequent hitters.” The main causes for such interference are unquestionably aggregation, metal-ion chelation, redox-activity, auto-fluorescence, absorbance, luciferase inhibition, and chemical reactivity. To dissect these liabilities early in the assay development phase, we subsequently make use of the “robustness set” compound collection. The robustness set comprises of selected molecules from the literature with well-defined assay interfering properties and so-called clean compounds for which we do not expect assay interference. These are also supplemented with many DMSO controls, all in a ready-to-employ single 1536-well plate. The application of the robustness set not only provides a framework to identify assay liabilities and tailor uHTS assay conditions such that minimal interference occurs but also helps to design suitable follow-up assay cascades for successful hit triaging.
Whether you are looking for high-quality assay development based on established techniques, or for more innovative novel assays, the passionate Pivot Park Screening Centre team will strive to deliver what your drug discovery project needs.
|
Fluorescent Intensity |
|
Absorption Based Measurement |
|
Fluorescent Polarisation |
|
Time Resolved Fluorescence (such as FRET, TR FRET, HTRF) |
|
AlphaScreen® |
|
Luminescence |
|
Beta-lactamase |
|
BRET |
|
Aequorin |
|
Calcium Kinetics |
|
Calcium Permeability |
|
Potassium Kinetics |
|
High Content Screening |
|
Mass Spectrometry |
Subscribe to our newsletter
Pivot Park – Banting Building (RE600)
Kloosterstraat 9
5349 AB Oss
The Netherlands
Pivot Park Screening Centre
Building OP
Kloosterstraat 9
5349 AB Oss
The Netherlands
To download this publication we would like to receive your e-mail.
To download this publication we would like to receive your e-mail.
