Enamine, EMBL Agree to Library Synthesis and Drug Discovery Services Collaboration

Enamine and the European Molecular Biology Laboratory (EMBL) agreed to a collaboration through which Enamine will provide library synthesis, medicinal chemistry, and biological services for EMBL’s small-molecule cancer drug discovery programs. Enamine will establish a team of full-time equivalent medicinal chemists to work on the project, which is focused on the development of cancer therapeutics with novel mechanisms of action, the organizations state.

EMBL has an existing relationship with Enamine. “We have been working with Enamine for several years, primarily to enhance the chemical space of our internal screening library,” explained Joe Lewis, Ph.D., head of Chemical Biology Core Facility at EMBL. “We realized quickly that their 2 million plus compound collection provides quality compounds allowing an increase in the chemical diversity of our screening deck.”

David Will, Ph.D., head of Medicinal Chemistry at EMBL, added, “This collaboration with Enamine will be pivotal for the success of our project for identifying targets from phenotypic screens and synthesizing and triaging new patentable preclinical compounds. Their agility and flexibility with access to the world’s largest collection of building blocks in stock at Enamine and integration of chemistry with a comprehensive biology service portfolio perfectly fit our goal of nominating a preclinical development candidate by 2018.”

Source

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Emerging Technologies: the Nanolive 3D Cell Explorer

From 16.08.2016 to 16.09.2016, Bienta was honoured to host Dr. Alain Géloën, a visiting scientist from University of Lyon, CarMeN Laboratory, INSA de Lyon, France, under the two ongoing Horizon 2020 projects,  Peptidomimetics with photocontrolled biological activity, and Carbon-based nano-materials for theranostic application.  Alain performed an exciting research using a novel tomographic Nanolive 3D Cell Explorer microscope . Using the microscope, Alain managed to track the fate of carbon-based nanoparticles in cancer cell cultures, as well as made real-time observations of the cell response to the action of the photocontrolled antibiotics. This unprecedented new technology allowes to look into the live cells without damaging them, enabling marker-free and real-time imaging on single cells, cell cultures, cell multilayers and tissue slices.

 

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European Horizon 2020 project at Bienta

Enamine/Bienta is participating in EU Horizon 2020 grant-funded program“Peptidomimetics with photocontrolled biological activity” headed by research teams from Karlsruhe Institute of Technology, University of Cambridge, Latvian Institute of Organic Synthesis and Enamine. Bienta’s preclinical biology team is supporting characterization of a photodynamic cancer drug candidate by DMPK and animal efficacy studies. In April 2016, Bienta’s researchers co-authored a prestigious paper on the subject (Babii et al., Angew.Chem.Int.Ed., 2016; 55: 5493-6).

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Metabolite identification

Knowing specific sites and pathways of metabolic transformations is useful for guiding synthetic optimization of lead compounds to overcome stability or toxicity issues commonly occurring in drug discovery. Over the last few years, Bienta’s ADME/mass-spectrometry team has accumulated substantial experience in running efficient and affordably priced Metabolite ID projects to help tackling the challenges of synthetic optimization for Enamine’s clients.

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HitLocator Library for efficient HTS campaigns at Bienta

Since the end of 2015, we are offering HitLocator Library (HLL) consisting of 511,360 compounds for contractual HTS campaigns at Bienta.
HLL is a carefully selected representation of the whole Enamine’s collection of more than 2,000,000 chemical compounds. HLL compounds were selected by applying chemical diversity and drug-likeness criteria and using extensive medchem filtering. HLL has an intelligently clustered design consisting of 5 “core” and 12 “radial” sets of 30,080 compounds each, which allows implementing screening strategies customized to the needs and budgets of any academic or industrial client. Bienta has already carried out productive hit finding campaigns on both the subsets and the whole HitLocator Library. HLL hits can be rapidly transformed to leads via hit expansion using the entire 2+ million off-the-shelf compounds, as well as multiple parallel synthesis from Enamine’s RealDatabase and focused Enamine-specific synthetic chemistry.

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New animal facility for in vivo studies launched at BIENTA

Bienta has just launched on-site laboratory for in vivo studies in rodents. This new animal facility allows us to continue expanding our services in preclinical toxicology and animal efficacy models, in addition to pharmacokinetics studies in mice and rats that Bienta was successfully offering for the last several years. Our immediate plans include setting up rodent efficacy models for the therapeutic areas of anti-infectives, inflammation and pain.

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YES Kinase Targeted Library Contest

Bienta has recently supported molecular modeling assessment project ran at Tokyo Institute of Technology, Japan. YES tyrosine kinase targeted library created by 10 competing in silico molecular modeling teams organized by Initiative for Parallel Bioinformatics ( IPAB) was successfully screened by Bienta to identify hits. The library consisting of 600 compounds was selected from Enamine’s  Screening Compounds Collection of close to 2,000,000 compounds.  Bienta enjoys unlimited and immediate access to the vast Enamine compound repository, allowing prompt and efficient high-throughput screening, hit verification “from powders” and hit expansion follow-ups.

The project report was published in NATURE Scientific Reports on 26 November 2015 and can be accessed here (open access).

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Bienta at MIPTEC 2014

Bienta will be participating at MIPTEC 2014 conference, September 23-25, Basel, Switzerland. Meet us there!
Our team member, Ihor Zahanich, will be presenting a poster “Pharmacological characterization of potent and selective Free Fatty Acid Receptor 1 (FFA1/GPR40) agonists for the treatment of type 2 diabetes”.  Author list: Ihor Zahanich, Olexandr Vasylchenko, Yuri Kheylik, Yulia Tokareva, Roman Moriev, Maxim Platonov, Vladimir Iurchenko, Sergey Zozulya.  Poster Session (Poster Area) to be held on Wednesday, 24 September 2014 between 17:00h and 18:00h.

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Differential Scanning Fluorimetry technology is now at Bienta

Introducing a new technology which is planned to be extensively used for screening projects at Bienta. Differential Scanning Fluorimetry (DSF, TSA) is a powerful biophysical method based on detecting the shifts in protein denaturation temperature upon ligand binding as reported by fluorescent dye interacting with protein core exposed by heat denaturation. DSF is a simple, label-free HTS technology applicable to most soluble proteins, irrespectively of their functions and activities. Now Bienta can provide on-site recombinant target protein production to support DSF-based screening projects.

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ASMC 2013

Feb 14, 2013  You are welcome to visit our booth and meet representatives of Enamine&Bienta Sales team at ASMC 2013 (5 – 8 May) (more…)

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Enamine launches preclinical biology laboratory

Jan 13, 2012 Enamine announces opening of contract biology laboratory at its main research site in Kyiv, Ukraine. Enamine’s BioLab will be providing ADMET (absorption, distribution, metabolism, excretion and toxicity) and biomolecular screening services to expand Enamine’s chemistry-driven CRO capabilities into the biological support of early phase drug discovery projects. (more…)

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