ICMRBS Webinar Series

Online

Marta Carneiro, Head of Structural Biology at ZoBio, presented the lecture ‘NMR in target driven drug discovery: why not?’ on Wednesday 25 November 2020. Marta has discussed several examples of how ZoBio uses NMR in various ways to streamline the discovery process and reduce downstream attrition. This talk was a part of the Drug Discovery/Development session of the ICMRBS Early Career Researcher Webinar Series.  The webinars are specifically meant for early researchers working on magnetic resonance in biological systems, but also for more senior scientists that may be interested in information about different NMR approaches in drug discovery.

The ZoBio Fragment Library: Chemically Diverse Starting Points for Drug Discovery

The ZoBio Fragment Library: Chemically Diverse Starting Points for Drug Discovery

ZoBio strives to provide attractive, validated chemical starting points for your drug discovery projects. To achieve this goal, we have been building and maintaining the ZoBio fragment library since 2003. Our fragment library has been screened against more than 100 targets from a large array of target families.

The quality of the ZoBio fragment library rests on three pillars: chemical diversity, properties being aligned with our biophysical screening and validation assays, and synthetic tractability of fragments. In the continuous process of maintaining the collection, these guiding principles are first and foremost in our mind. We have recently finalized a major library revision, further improving the quality and efficiency of fragment screening at ZoBio.

This revision included the replacement of original fragments with new compounds based on our latest medchem insights and analysis of the performance of fragments in a multitude of fragments screens. Compound acquisition and admission to the screening deck was guided by objective cheminformatics and rigorous quality control, using NMR and SPR.

Our fragment library now contains approximately 2.000 fragments that are available for screening, including interesting compounds with pronounced 3-dimensional fingerprints.

Interested in screening a cleverly designed fragment library? Talk to us!

 

NMR in Target Driven Drug Discovery: Why Not?

NMR in Target Driven Drug Discovery: Why Not?

NMR is a powerful and information rich tool that can provide critical information at many stages of the pre-clinical drug discovery process.

In a recent publication ZoBio scientists discuss a number of examples in which relatively simple NMR experiments routinely provided them with data critical to the setup of new programs, interpretation of biophysical and biochemical data and elucidation of structural information describing the protein–small molecule interaction. In this article examples from the very early stages of target preparation and hit discovery are reported, but we also show how NMR offers the potential to observe protein–ligand interactions and thereby contribute structural information in multiple settings.

Our NMR team is ready to make an impact on your drug discovery campaign as well.

 

 

Mirati and ZoBio Collaborate to Advance Targeted Oncology Programs

Mirati and ZoBio Collaborate to Advance Targeted Oncology Programs

Mirati Therapeutics has selected ZoBio to provide fragment-based screening, biophysical compound characterization and structural biology for several oncology targets. In this arrangement, ZoBio screens its fragment library using both its proprietary Target Immobilized NMR Screening and SPR capabilities. Subsequently hit analogs are characterized by a biophysics-based cascade tailored to select molecules with the desired Mode of Action and binding site. Medicinal chemistry decision making is aided by ZoBio’s unique combination of solution NMR and X-ray crystallography that provides structural information earlier, particularly for weakly binding fragment hits and early analogs.

Statement from Matt Marx and Gregg Siegal: “We are excited to be working together to advance Mirati’s preclinical portfolio.  This represents an ideal combination of Mirati’s discovery expertise and approach to target selection and ZoBio’s platform of capabilities and proven track record in hit identification, characterization and target enablement.“