Protein targets for small molecule screening

With our cutting-edge technology, we specialize in optimizing protein targets to facilitate the discovery of novel hits, leads, or compounds with enhanced affinity and precision.

Utilizing top-notch soluble and membrane proteins provided by Eurofins DiscoverX® and Eurofins CALIXAR, biophysics becomes applicable across various stages of early drug discovery. This application spans from initial hit identification to final candidate selection across multiple modalities, encompassing fragments, small molecules, targeted protein degraders, RNA/DNA binders, aptamers, peptides, and biologics. 

Biophysical technologies are available to realize small molecule screening through high quality soluble proteins and membrane proteins. For custom assay projects, take advantage of Eurofins CALIXAR’s expertise. Our scientific experts utilize the latest in laboratory technology to perform relevant analyses.

Surface Plasmon Resonance (SPR) 

The SPR is a powerful technique used in biology and chemistry to study real-time molecular interactions. It relies on the ability of surface plasmons (electromagnetic waves) to interact with changes in mass density at the surface of a material, typically a thin metallic layer.

In a typical SPR apparatus, a sensitive sensor detects changes in refractive index near the metallic surface. When target molecules bind to molecules immobilized on this surface, it locally alters the refractive index, leading to a shift in the resonance angle of surface plasmons. 

By monitoring these angle changes, one can quantify and characterize biomolecular interactions such as antibody-antigen binding or receptor-ligand binding, providing insights into the kinetics and affinity of the interaction.

High-Throughput Surface Plasmon Resonance (LSA)

The Carterra LSA (Laser-Enabled Surface & Bulk Analysis) platform is a structural biology platform primarily used for analyzing protein-protein, protein-DNA, protein-RNA interactions, and other molecular interactions.

This platform integrates advanced technologies such as Surface Plasmon Resonance (SPR) and BioLayer Interferometry (BLI) to enable real-time quantitative study of molecular interactions. It's often employed in pharmaceutical and biotechnological research to expedite drug discovery processes and for detailed characterization of biomolecular interactions.

The Carterra LSA platform offers advantages like high sensitivity, increased automation, and the ability to analyze multiple interactions simultaneously. This makes it a valuable tool for understanding complex molecular interactions and for developing more effective drugs.

MicroScale Thermophoresis (MST) 

The MST is a technique used to measure interactions between molecules, particularly biomolecules, in a solution-based system. It relies on the movement of molecules in a temperature gradient, where variations in temperature create local differences in solute concentration, causing molecules to move from warm to cold regions.

By observing the movement of fluorescently labeled molecules under a microscope, MST quantifies the changes in fluorescence signal as a result of molecular interactions. This allows for the determination of binding affinities, kinetics, and the characterization of various biomolecular interactions, making MST a valuable tool in drug discovery, protein research, and the study of molecular interactions in solution.

Isothermal Titration Calorimetry (ITC)

The ITC is a technique used to measure the heat changes that occur during a biomolecular interaction in a solution-based system. It operates by titrating one reactant into another while maintaining a constant temperature, typically measuring the binding of a ligand to a macromolecule (such as a protein or nucleic acid).

ITC directly monitors the heat released or absorbed as the molecules interact. From the heat changes recorded during titration, key parameters such as binding affinity (Kd), stoichiometry, enthalpy, and entropy of the interaction can be determined. 

This method provides insights into the thermodynamics of molecular interactions, aiding in understanding the strength and nature of binding between biomolecules. ITC is widely used in drug discovery, protein-ligand interactions, and the study of molecular interactions.

Ternary complex formation with Proteolysis-targeting Chimeras (PROTACs)

PROTACs is a strategy used in drug development to induce the degradation of specific proteins within cells. PROTACs are molecules designed to bring a target protein in proximity to an E3 ubiquitin ligase and thereby tag the target protein for degradation by the cellular proteasome machinery.

This technique involves a three-part molecule: one end binds to the target protein, the other end attaches to the E3 ligase, and the linker joining the two ends allows for proximity-induced degradation. Once assembled into a complex, the E3 ligase tags the target protein with ubiquitin, marking it for degradation by the cell's proteasome.

PROTACs offer a unique approach to targeted protein degradation, providing a potential therapeutic strategy to eliminate disease-causing proteins within cells. This technique has gained attention in drug development due to its ability to selectively degrade specific proteins of interest, offering potential applications in treating various diseases, including cancer and other disorders. 

Best-in-class membrane proteins for drug discovery

High-quality native membrane protein targets ideally for advancing small molecule drug discovery efforts.

The discovery of small molecules as ligands is a pivotal aspect of drug development, as these molecules can selectively bind to target proteins, enabling the modulation of specific biological processes and offering potential solutions for various medical conditions. To facilitate the discovery of ligands, Eurofins CALIXAR produces high-quality native membrane protein targets by screening with  Fragment-based Drug Discovery – FBDD and Structure-Based Drug Design - SBDD. 

Our protein targets are compatible with all screening platforms: High Throughput Screening (HTS), Surface Plasmon Resonance (SPR), Affinity Selection-Mass Spectrometry (AS-MS), Saturation Transfer Difference-Nuclear Magnetic Resonance (STD-NMR), DNA Encoded Library screening (DEL). These methods enable the rapid screening of potential drug candidates, uncovering their interactions with target molecules, elucidating their three-dimensional structures, and providing critical insights into the development of safe and effective pharmaceuticals, ultimately expediting the drug discovery process.

Our high-quality native, pure, stable and functional active proteins are a valuable asset for drug discovery scientists, including Biochemists, Structural Biologists, Biophysicists, and Medicinal Chemists. 

In addition, Eurofins CALIXAR provides a deeper understanding of ligand-protein recognition and promotes the discovery of the mechanism of action (orthosteric vs allosteric).

Obtain access to Eurofins CALIXAR's drug discovery technology

All of our clients get access to our proprietary technology and expertise (8 patent families, more than 28 publications).

The CALIXAR® platform uses patented technologies exclusively possible for clients under specific arrangements (license, co-development, and service).

You can leverage Eurofins CALIXAR’s proprietary technology, alongside other top-tier active protein technologies that are unobtainable in the market.

Secure and boost
your discovery programs

Starting from native material or recombinant systems, we succeed with all types of proteins: Kinases, Phosphatases, Ubiquitins, Epigenetic Proteins, GPCRs, Ion Channels, Transporters, Receptors and Viral Proteins.