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.“

 

Axxam and ZoBio Form a Strategic Alliance Integrating their Drug Discovery Services Platforms

Axxam and ZoBio Form a Strategic Alliance Integrating their Drug Discovery Services Platforms

MILAN, IT, AND LEIDEN, NL

Axxam and ZoBio have initiated a strategic alliance to provide a combination of integrated discovery services spanning all phases from gene to fully optimized leads.

This alliance provides access to a synergistic, industry-leading, integrated toolbox of protein production and engineering technologies and screening methods using cellular, biochemical, high content and biophysical assays. These capabilities are used to probe our innovative small molecule and fragment libraries for ideally behaved hits. The hits can subsequently be evolved with our focused medicinal chemistry expertise supported by NMR and X-ray crystallography-based structural biology, all under a single, seamless contractual arrangement. The Axxam and ZoBio collaboration brings together decades of experience with unbeatable technology to help you to overcome your greatest drug discovery challenges.

Stefan Lohmer, co-founder and Chief Executive Officer of Axxam, commented, “We are very pleased to announce this strategic alliance with ZoBio. Both Axxam and ZoBio share a common philosophy based on excellence and creativity in biology. Axxam is a biology-driven company with a deep understanding of targets, assay development and high throughput screening, with a culture of scientific excellence and the attention to delivering the quality results our clients need and expect.

The complementary technical skillsets between Axxam and ZoBio provide a seamless suite of options to our clients looking to interrogate pharmacologically challenging drug targets with a variety of complementary platforms.”

Gregg Siegal, Chief Executive Officer of ZoBio added, “Fundamentally, HTS and fragments offer tremendous complementarity with the result being a far more robust drug discovery campaign. Our biophysical approach allows us to select for molecules with the desired mode of action whereas Axxam’s cellular and biochemical expertise selects molecules with the desired biological activity. While the science of our two companies is orthogonal, we share a deep commitment to excellence, which is why this is the perfect collaboration.”

Gotham Therapeutics and ZoBio Achieve Significant Milestone in Epitranscriptomic Drug Discovery Collaboration

Gotham Therapeutics and ZoBio Achieve Significant Milestone in Epitranscriptomic Drug Discovery Collaboration

NEW YORK, NY, USA AND LEIDEN, NL

Gotham Therapeutics has selected ZoBio to initiate a collaboration on the development of small molecules targeting epitranscriptomic targets. This collaboration has now resulted in several lead candidates for the METTL3/METTL14 complex.

With 15 years of experience, ZoBio is the proven partner for biophysics driven, fragment based drug discovery. We are dedicated to achieving the best science and highest level of transparency.

Our integrated discovery engine progresses projects from gene-to-lead. High throughput protein engineering and production, diverse, novel fragment libraries, proprietary biophysical screening technologies and complementary structural biology approaches have been tailored to provide validated data at every step of the process. The right combination of these various disciplines generates actionable medicinal chemistry hypotheses for small molecule modulators of a great variety of pharmacological targets, including those that have previously been out of reach.

‘In a sector that is still in its infancy, we have made tangible progress with our partner ZoBio to develop small molecule leads against a portfolio of epitranscriptomic targets just 14 months after initiation of the project,’ commented Dr. Lee Babiss, Chief Executive Officer of Gotham Therapeutics. ‘Today’s news is also a validation of the semi-virtual model we use and the productivity of our network with best-in-class CROs.’

‘With METTL3/METTL14 being among the more obvious approaches in epitranscriptomics, the quality of the hit matter pursued is going to be a key differentiating factor,’ added Dr, Gerhard Müller, Chief Scientific Officer of Gotham Therapeutics. ‘Together with ZoBio, we have not just successfully identified the initial candidates for Gotham’s first pipeline program but also established a robust process from gene to lead as a platform for additional projects to come.’