Reliable, HTS-ready, biologically and pharmacologically relevant for cell-based GPCR screening

Robust cell-based assays are essential for the success of drug discovery and development.

They are more physiologically relevant than biochemical assay while higher throughput and lower cost than animal models. Cell-based assays are not only versatile tools for elucidating the biology and disease relevance of drug targets, they are also powerful tools in high throughput screening (HTS), lead optimization, and safety studies in compound selection. 

Using mammalian cell engineering technologies, a target can be overexpressed or knocked down in cells derived from humans or animals. However, these modified cells do not automatically mean robust HTS assays. A number of questions need to be asked. Do the cells give HTS-compatible assay window from the signal to background ratio? Will the cells stay stable and endure the journeys of multi-year projects?

Commercially available cell lines often share some prevalent and detrimental drawbacks such as a) heavily engineered targets tagged with sizable protein fragments; b) non-clonal “stable” pools of cells that deteriorate quickly; c) parental cells with high expression of the target and related targets; d) one cell line for one assay and another cell line for another to compare the 2 signaling pathways; e) modified signaling components; and f) overamplified protein expression.

Not all commercially available stable cell lines are created equal.

Leveraging the unique combination of cell engineering and assay development expertise, Multispan’s researchers focus on native targets and native signaling. Each MULTISCREEN™ stable cell line is are designed, cloned and developed specifically for the purpose of robust HTS cell-based assays. Each of these cell line product reflects high standards and uncompromising quality that will withstand the test of time. This is the reason behind the 100% successful track record of the MULTISCREEN™ stable cell lines in our customers’ hands and in the HTS operation in our own lab.

For example, our signature MULTISCREEN™ GPCR stable cell lines offer several distinct unique benefits:

  • Preservation of all endogenous cell signaling pathways: Calcium, cAMP, beta-arrestin, pGRK2, IP-1, pERK, pNFκB, radioligand binding, GTPγS, chemotaxis, cytokine secretion, cell proliferation, Luciferase reporter and internalization
  • Gold standard for studying all GPCR cell signaling biases in ONE cell line
  • Multi-screen capability in the same cell line across multiple assays for counter screens
  • Available as division-arrested cells and membranes
  • Rigorously validated in MULTISCREEN™ No Wash Calcium Assay and cAMP Assay Kits
  • Expression and pharmacology-matched human and ortholog protein target pairs, including rhesus monkey, cynomolgus monkey, dog, ferret, rabbit, rat, and mouse

The Multispan Approach

We enjoy learning the biology of each target and developing high-performance cell lines for disease-relevant assays. It serves our mission to help “make better medicine, one assay at a time”.

Our over 500 MULTISCREEN™ GPCRs stable cell line clones have been referenced in over 100 peered reviewed journals and patents. Combined with MULTISCREEN™ Beta-Arrestin Sensor, Calcium and cAMP assay kits, and customized protocols for each stable cell line, the complete solution is truly HTS-ready. 

Beyond GPCRs, we have applied our extensive knowledge in successful stable cell line and assay development for kinases, nuclear hormone receptors (NHRs), transporters, integrins, ion-channels and more. 

The MULTISCREEN™ stable cell line platform is built on a foundation of rigorous science, proprietary expression, vectors optimized for cell surface expression and a wealth of knowhow. It is driven by native-signaling based HTS assays from the get-go. As a result, the stable cell lines are highly differentiated to decipher multiple physiologically disease-relevant pathways using native targets in the same cell line. Multispan’s expertise in cell sciences, assay development and high throughput screening uniquely ensures that the MULTISCREEN™ stable cell line products possess the highest quality in the industry for the drug discovery HTS needs.  

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