Drug-target kinetics with Excellerate
Two expert companies providing an exceptional drug-target kinetics service
Cisbio and Excellerate are partnering to offer you an outstanding drug-target kinetics service.
The team at Excellerate Bioscience have pioneered the use of competition association assays to measure the binding kinetics of unlabeled compounds, and over the past 15 years have successfully implemented them in drug discovery projects across both industry and academia.
They have published over 20 papers, reviews, and book chapters on the measurement and interpretation of the kinetics of drug binding.
Excellerate has selected Cisbio’s Tag-lite as their preferred technology for all their GPCR kinetic binding work more recently, they have significantly improved the throughput of these assays by utilizing Cisbio’s Tag-lite to develop homogeneous continuous-read assays in a 384 well format.
This has enabled the kinetic screening of fragment libraries at membrane proteins in their natural plasma membrane environment, for the first time.
Convinced of the impact of binding kinetics on the clinical performance?
Interested in precisely accessing your compound kinetic parameters but unsure of the methodology to follow?
Cisbio and Excellerate will measure your compound’s Kon, Koff and residence time for you.
The development of kinetic assays at membrane proteins is not a trivial task. In addition to optimizing the overall assay conditions and the read frequency, the choice of a fluorescently-labeled tracer is critical to success.
It can sometimes require the bespoke development of novel tracers with the appropriate optimal properties. At Excellerate, this can be achieved quickly and efficiently through our long-standing collaboration with a chemistry team at the University of Nottingham that has decades of experience developing fluorescent tools for drug discovery applications.
Finally, the analysis and interpretation of kinetic data can be complex. At Excellerate, we are experts in fitting complex models to experimental data, paying close attention to the quality of fit and overall confidence in kinetic parameter estimates. Sometimes the assay format needs to be modified to accommodate particular kinetic profiles, and we select the appropriate mathematical models for each particular format.
Excellerate was a precursor when it adopted Cisbio’s Tag-lite technology for kinetic binding. The Tag-lite solution has quickly become the industry standard for studying receptor-ligand binding interactions. Our Tag-lite offer continues to demonstrate its effectiveness, as shown below in a list of recent publications:
Nederpelt, Indira, et al. “Characterization of 12 GnRH peptide agonists – a kinetic perspective.” British journal of pharmacology 173.1 (2016): 128-141.
Sykes, David A., and Steven J. Charlton. “Single Step Determination of Unlabeled Compound Kinetics Using a Competition Association Binding Method Employing Time-Resolved FRET.” Rational Drug Design. Humana Press, New York, NY, 2018. 177-194.
Nederpelt, I. Time is of the essence – Investigating kinetic interactions between drug, endogenous neuropeptides and receptor. Diss. 2017.
Excellerate has invested in the latest plate reader technology to maximize the robustness and fidelity of our HTRF assays. Scientists at Excellerate selected the latest in the Pherastar range from BMG Labtech, the FSX, as it has been optimized for use with TR-FRET applications. The signal to noise on this machine is second to none, enabling very rapid acquisition times and therefore high frequency kinetic reads. In addition, the onboard injectors are capable of adding reagent during a read, which means very early time points can be sampled.
The Excellerate facilities are equipped with excellent liquid handling capabilities, including nanolitre dispensing, which enables the medium throughput screening of compound/fragment libraries.
Cisbio and Excellerate share the same philosophy and commitment to excellent service. Regular open communication is at the heart of our ethos; we work closely with our clients to ensure they are involved in decision-making and are happy with the progress made throughout the process. This increases confidence and significantly speeds up the development.
Excellerate are not only experts in kinetic assay development and screening, we also have decades of experience successfully incorporating kinetic data into full drug discovery programs to select candidates with superior clinical efficacy and safety. We can provide consultancy on how to integrate kinetic data into your projects, advising on the optimal kinetic characteristics for a given therapeutic application and how to integrate them into PK/PD analysis.
Better customer support
Do you have a question about your final product? Do you need to discuss what the numbers on the report mean? Automated phone systems infuriate you?
Cisbio and Excellerate guarantee you direct access to the scientists who prepared your drug-target kinetic report.
We do not use automated phone systems or a complex directory. Simply talk to the right person, right away.
Our local team of HTRF experts is ready to make your experience with Cisbio and Excellerate seamless.
Enjoy a collection of expert opinions on kinetic binding
Benefit from Excellerate Bioscience’s expertise combined with Cisbio’s Tag-lite technology to tackle your kinetic binding research.
This application note will provide you a perfect example of what you can expect for your own research project. This document gives you a concrete case study about kinetic adenosine receptor family binding assays. Discover the methods used by Excellerate, including a list of the materials and a complete adenosine kinetic binding characterization regarding human, rat and mouse adenosines A1, A2a, A2b and A3.
Curious about the Excellerate team?
Prof Steven J Charlton, Chief Scientific Officer
Steven has over 16 years experience in industrial drug discovery.
At Novartis, he was the Director of Molecular Pharmacology in Respiratory Diseases, leading an assay development and compound profiling team of 30 scientists and providing expert opinion and support for GPCR, ion channel, and enzyme projects. He has broad drug discovery experience, ranging from target validation to full lead optimisation programmes through to successful clinical proof of concept. In addition to his role as Chief Scientific Officer at Excellerate Bioscience, Steven is also Professor of Molecular Pharmacology and Drug Discovery at the University of Nottingham, where he is interested in all aspects of the quantitative assessment of ligand-receptor interactions, particularly the kinetics of binding and signaling.
Viral Patel, Chief Operations Officer
Viral Patel has over 18 years of global pharmaceutical research experience, contributing to the development of therapeutics in a variety of disease areas. He has successfully built pharmacology and enzymology groups within Novartis and Merck, and has extensive experience in developing and automating screening cascades. Viral has a particular interest in mechanistic enzymology and in understanding how different modes of inhibition influence clinical efficacy. He currently holds an Honorary Industrial Fellowship at the University of Nottingham.
Suky Chahal, Chief Finance Officer
Suky joined Excellerate’s Board of Directors in June 2017 as the Finance Director. Suky held the position of Group Finance Director at Standard Motor Products Europe Ltd in the automotive industry for the previous 11 years and led the European Group through business restructurings and a management buyout. Prior to this, he held various board positions with European and US multinationals, dealing with business acquisitions and disposals. With over 25 years experience in accountancy and business development, he has brought a wealth of experience to Excellerate to assist with its future growth plans. Suky is a Fellow of the Chartered Association of Certified Accountants and holds a BA hons in Finance and Accounting.
Dr Karolina Gherbi, Principle Scientist
Dr Karolina Gherbi is a molecular pharmacologist with 7 years of experience gained in both industry and academia. She has extensive knowledge of detailed GPCR pharmacology focused on defining compound mechanisms of action in biochemical and cellular assays, with particular expertise in advanced microscopy techniques. Dr Gherbi manages a team of research scientists to provide project support for multiple target classes in a range of disease therapeutic areas.
Dr Elizabeth Rosethorne, Principal Scientist
Dr Elizabeth Rosethorne is a cellular pharmacologist with >10 years’ experience in Respiratory Drug Discovery within industry and academia. Her particular expertise lie in the use of phenotypic assays to identify targets for disease therapeutics and functionally characterise novel compounds in primary human cells. Dr Rosethorne has experience in Project Leadership, and has collaborated with diverse research teams to support compounds to Proof of Concept and beyond.
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No matter what the inquiry, our commitment to exceptional service ensures that we will provide you an optimal solution.
Want to know more about our Excellerate offer? Learn about this dynamic and innovative contract research organization built on a worldwide reputation for excellence in the field of molecular and cellular pharmacology.
Two expert companies working together to offer an exceptional drug-target kinetics service.