Drug Discovery Unleashed

CETSA® by Pelago Bioscience

The Cellular Thermal Shift Assay (CETSA® by Pelago Bioscience) has multiple assay formats that make it a keystone of decision making throughout the drug discovery pipeline.

Unlike other solutions on the market today, its unique approach allows the assessment and quantification of target engagement under physiological conditions – without the need to modify the compound or protein. This provides data that is both actionable and biologically relevant.

Think of CETSA® as snapshots of true target engagement inside the cell, any time you need them.

In lab at pelago

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HOW DO I KNOW IF MY
COMPOUND WILL BE EFFECTIVE?

A wide range of services from early discovery to confirmation

Our CETSA® teams offer a range of customized services, designed to help you make better decisions faster, no matter where you are in the drug discovery process.

True target engagement assessment

Target
Identification

Lead
generation

Lead
optimization

Preclinical
studies

Clinical
trials

Approved
drugs

Target Identification

CETSA® Explore (also known as TPP or PISA) combines the power of Mass Spectrometry with CETSA® and allows for unbiased proteome-wide target identification. Being unbiased and hypothesis–free, CETSA® Explore can be used for target deconvolution studies for hit compounds from phenotypic screens. Since CETSA® can be performed in any sample matrix, the profiling and deconvolution can be conducted directly in disease relevant systems.

Lead Generation

CETSA® Navigate HT is a perfect tool to unlock novel chemistry in lead generation programs using compound library sets of up to 500k. Or alternatively use CETSA® Navigate for rapid hit confirmation or the CETSA® Explore for proteome-wide profiling of lead compounds.

Lead Optimization

CETSA® Navigate and Navigate HT are both commonly used within lead optimization programs, with the choice being dependent on the number of compounds tested.  Navigate HT offers greater volumes at lower data point costs in shorter time. Navigate provides a faster assay development and is applicable to a wider range of assay matrices and therefore an ideal format to progress into translational studies. In addition, the CETSA® Explore can assess the selectivity profile of the lead series to highlight safety issues that needs to be addressed.

Preclinical Studies

CETSA® Navigate’s flexibility makes it the first choice for translations studies where confirming target engagement within tissue samples is required and in patient derived material can provide a vital clue to the drug candidate probable efficacy in human studies.

Clinical Trials

Biomarkers are important to facilitate translation, validate the therapeutic hypothesis and monitor effects in clinical trials and beyond. CETSA® Explore can be used to identify novel markers that would not be identified by conventional ‘omics approaches, and if necessary CETSA® Navigate or Navigate HT can be used to monitor these in patient samples once the biomarker has been identified.

Approved Drugs

Many drugs have poorly understood, complex and diverse modes of action. CETSA® Explore is a powerful tool that provides deep insights into the selectivity and action of drugs. These insights can be used to identify drug repurposing opportunities, drug synergy and new targets.

Technology
One proven assay. Many flexible formats.

The Cellular Thermal Shift Assay (CETSA®) is a well-established, proven and accurate technique for measuring compound binding to target proteins. While CETSA® can be adapted for different applications to support any stage of the drug discovery process – from low-throughput confirmation and medium-throughput discovery to proteome-wide exploration – these different methods all rely on the same principle: measurements of the ‘thermal shift’ that occurs when a ligand interacts with a protein.

When a compound binds to a protein, the denaturation temperature of that protein can be altered. By applying heat shocks to cells or tissue, then quantifying the difference in the amount of soluble protein in presence compared to absence of the compound, we are able to create snapshots of target engagement under actual physiological conditions. This is how CETSA® can be used to assess and quantify compound-protein interactions.

“At AstraZeneca we are applying CETSA® HT in high-throughput screening and lead optimization to identify and characterize hit and lead compounds for a number of novel targets.”

Thomas Lundbäck,
Associate Director,
AstraZeneca,

”CETSA® data is a keystone in our SAR analysis, and by assessing cellular engagement of our compounds across multiple cell lines we gain confidence in our project prioritizations.”

Peter Joyce,
CEO & co-founder,
Grey Wolf Therapeutics

”Chemoproteomics is like taking a watch to pieces and counting the cogs—it doesn’t tell you which cogs drive which process and how the wider system works. This is why using CETSA® MS can add so much value to your target identification studies”

Pär Nordlund,
Professor & inventor of CETSA®
Karolinska Institute

About Pelago


Using our world leading expertise in CETSA® we have created a faster and more efficient drug discovery process. We take great pride in knowing our customers are bringing new medicines to market more quickly thanks to our help.

Michael Dabrowski
CEO, Pelago Bioscience

Speak to our experts

Learn how CETSA® can enable your project by talking to one of our Drug Discovery experts.

Latest news

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