02 December 2014
Drug Discovery collaboration with BioVersys AG extended
Collaboration with BioVersys AG aiming at discovery of novel treatments against bacterial infections has been extended for the 4th consecutive year.
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02 December 2014
Collaboration with BioVersys AG aiming at discovery of novel treatments against bacterial infections has been extended for the 4th consecutive year.
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28 March 2014
Controlling Biological Activity with Light: Diarylethene-Containing Cyclic Peptidomimetics
Oleg Babii, Sergii Afonin, Marina Berditsch, Sabine Reisser, Pavel K. Mykhailiuk, Vladimir S. Kubyshkin, Thomas Steinbrecher, Anne S. Ulrich and Igor V. Komarov
Angewandte Chemie International Edition 2014 53 (13), 3392–3395
Enamine scientists in collaboration with research at Karlsruhe Institute of Technology (KIT, Germany) published a study on antibiotics activated by light. It deals with synthesis of analogues of the antimicrobial peptide gramicidin S which conformations can be switched by light. This property was rendered by incorporation in its structure of an amino acid designed based on a photoisomerizable diarylethene scaffold. The biological activity of the resulting peptidomimetics can be reversibly controlled by ultraviolet/visible light.
Success of Enamine’s innovative product pipeline and service portfolio is based on the commitment of the company to the scientific research. Enamine caries out and supports research projects within the company as well as off-site in collaboration with many academic centers in Ukraine and abroad. About 30 scientific papers were published by Enamine scientists in renowned scientific journals in 2013.
02 March 2014
With development of on-line chemical directories acquiring necessary reagents and building blocks for day-to-day research activity has become a technical routine. Many thousands of building blocks are now available in the market and sub-structure search can efficiently provide a selection of reagents to buy. However, this approach might be limited. With over 80,000 building blocks synthesized and now available from our stock we are a recognized leader in the market. Our catalog features versatile building block classes and adds 1,000 products each month. Although they all are available for purchase through EnamineStore and many public or corporate chemical databases we wanted to gather together the most interesting and recently prepared building blocks to provide a series of useful guides to a novel and innovative chemistry. First five brochures have been published to highlight our rich collections of Advanced Morpholine Analogues, Bicyclic Aliphatic Amines, Fluorinated Aliphatic Amines, Isocyanates, Isothiocyanates, and Trifluoroethyl Carbamates, and Sulfonyl Chlorides and other Sulfonylating Agents.
23 September 2013
Axxam S.p.A., a contract research and discovery company, announced today that an entirely new generation screening collection is now available for drug discovery programs: AXXDIV2.0 made up with 240 000 carefully selected small molecules.
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03 June 2013
Enamine and Exquiron are announcing a multi-year collaboration wherby Exquiron is acquiring a large screening compounds libraries from Enamine.
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06 June 2012
A collaboration agreement has been signed between Enamine, the Medical Research Council Laboratory of Molecular Biology (MRC LMB), Cambridge, UK, and the Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic (IOCB), Prague, Czech Republic. The new alliance is aimed at discovering novel Rhomboid Protease inhibitors as potential drugs to treat infectious, parasitic, oncological, immune and cardiovascular diseases. Enamine will provide the MRC LMB and IOCB with access to its integrated drug discovery capabilities, including Molecular Modeling, Compound Library, Screening Assays, Hit Finding and Characterization, Hit to Lead Chemistry and ADMET. The three parties will seek to partner the small molecule inhibitors generated with pharmaceutical companies for onward clinical development. The collaboration agreement was negotiated by MRC Technology on behalf of MRC LMB.
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18 April 2012
Enamine and UkrOrgSynthesis Ltd (UORSY), a leading Ukrainian supplier of chemical building blocks and compounds for high-throughput screening, announced they have signed a collaboration agreement to offer chemical building blocks to the drug discovery industry cooperatively. By combining their catalogues, the companies become the largest global manufacturer and seller of building blocks, with 60 000 products available from stock for immediate delivery and an array of ca. 8 million tangible building blocks deliverable with synthetic success rate of 80%.
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31 January 2012
Enamine Ltd, a leading provider of screening compounds and chemical building blocks, today announced it has extended its long-standing relationship with BioFocus, with the acquisition by BioFocus of a large new compound screening library. The library will be available to BioFocus HTS collaborators in early 2012.
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25 January 2012
Enamine is planning to change the numbering of products offered through screening collections in 2012. To facilitate compound tracking in different offerings and allow transparent identification of structures by their unique ID throughout various databases, the old identification method utilizing lot-related T-numbers will be ceased. According to the new identification system all structures referring to compounds offered by Enamine for screening will have unique Z-codes familiar to those who worked with REAL Database before. Existing T-codes will be supported for ordering purposes.
29 September 2011
Over 51,000 low molecular weight reagents are now available from our stock. To the best of our knowledge, with this amount of substances the company has become the world’s largest supplier of physically available building blocks. The considerable improvement of synthetic technologies at Enamine is pushing the limits of the stock update rate. Currently over 1,000 building blocks are added to the stock every month.
28 April 2014
Mykhailiuk, P. K. Generation of C2F5CHN2 In Situ and Its First Reaction: [3+2] Cycloaddition with Alkenes Chem. Eur. J. 2014, 17, 5168. (Back Cover Picture)
Ritter, S. K. Diazoalkane Expands Fluorine Focus On Ethyl Groups Chemical & Engineering News, 92 (17), 2014.
Developing new methods for introducing fluorine into complex organic molecules has been all the rage during the past few years. Researchers preparing drug candidates and crop-protection chemicals typically seek to add a single fluorine atom or trifluoromethyl group and now have myriad ways to do so. But methods for adding longer, more lipophilic perfluoroalkyl groups, such as pentafluoroethyl, –C2F5, to complex molecules are relatively scarce. The approaches tend to be direct additions of C2F5 using organometallic transfer reagents and don’t utilize C2F5-containing building blocks.
Enamine scientists have developed a new building block for introducing C2F5 group into organic molecules. Pavel Mykhailiuk and colleagues safely generated the fluorinated diazoalkane, C2F5CHN2, in situ from C2F5CH2NH2•HCl and NaNO2. Authors demonstrated the utility of the reagent by using it in [3 + 2]-cycloadditions with mono- and disubstituted alkenes at room temperature to prepare perfluoroethylated pyrazolines with better than 95% conversion rates. Authors believe the diazofluoroalkane will also be as useful as other diazoalkanes for cyclopropanations, carbene insertions, and alkyne cycloadditions.
14 March 2014
336 Azides and alkynes have been selected from Enamine’s catalog of over 90 000 Building Blocks. Their structures have been published in the Selected Building Block series. This brochure, the sixth in series, provides a useful guide to novel and innovative chemistry developed at Enamine that can find multiple applications in drug design. Cycloaddition reaction of azides and alkynes has been shown to smoothly provide excellent yields of 1,2,3-triazoles. It has been recognized as an outstanding example of “click chemistry” This reaction can be used to selectively synthesize both 1,4- and 1,5-substituted triazoles. Besides reaction with azides alkynes undergo many other cycloaddition reactions.
15 January 2014
The new version of EnamineStore provides enhanced functionality to quickly search and purchase from catalogs of Enamine and UORSY (collectively over 10 million compounds). The following improvements have been realized besides changes in general form layouts:
Search functionality
Catalog
Cart
07 August 2013
Four Ukrainian students won respectively three Gold medals and one Bronze medal at the 45th Chemistry Olympiad held in Moscow on July 15-24, 2013.
The Ukrainian Team competed against 291 students from 73 countries.
Members of Ukrainian Olympic team:
Andriy Stelmakh, Lviv Physics and Mathematics Lyceum – Gold Medal
Oleksandr Vyhivsky, Kharkiv school # 47 – Gold Medal
Mykyta Onizhuk, Kharkiv technical school # 173 – Gold Medal
Khrystofor Khokhlov, Kiev school # 145 – Bronze Medal
Enamine is continuously aiming towards excellence, in its organization, products & services. The company is proud of the achievement of the Ukrainian team and to have sponsored its national team. Sponsoring such event is a natural initiative from Enamine and we would like to warmly congratulate the four students for their results.
Source: Korresponsent.net
15 October 2012
3D Diversity Set from Enamine, containg 50 000 drug-like compounds, has been selected by ChanTest for their dicovery services using powerful HTS of Ion Channels, GPCRs and Transporters in partnership with pharma and biotech companies.
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05 June 2012
Recently several new features were made available to users of EnamineStore:
06 February 2012
Enamine Ltd concluded an agreement with Legend Star International Co., to further promote products offered by Enamine to Taiwan drug discovery market. It is expected, that Taiwanese customers will be getting all relevant information on Enamine compounds and services from the local distributor and will benefit from improved service. Clients from Taiwan are encouraged to contact Legend Star International Co., Ltd. for all questions related to purchase of Enamine products:
1F., No.166, Fuxing 3rd St.,
Taishan Township, Taipei, Taiwan,
Mr. Chen Tsung-Ting
Tel: 886-2-29003199 (Ext 20)
Fax: 886-2-29009912
E-mail: This email address is being protected from spambots. You need JavaScript enabled to view it.
30 January 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.
Integration of the newly created contract biology lab with Enamine’s internationally renowned synthetic chemistry powerhouse and the vast screening compound repository creates a perfect combination for providing efficient and cost-competitive drug discovery services to the international pharmaceutical and biotech industry.
18 October 2011
Solid-Phase Peptide Synthesis was launched by Enamine with a new PS3 Peptide synthesizer (Protein Technologies, Inc.). Small linear and cyclic peptides comprising 2 to 25 amino acid residues of both natural and unnatural origin can be prepared on 1-30 mg scale in a highly pure form (>95%). A large collection of proprietary unnatural amino acids including many conformationally constrained ones as well as ones containing fluorine substituents can be used to expand the variety of peptides. The example structures of peptides prepared with our new peptide synthesizer are listed below.
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CF3-Labeled Gramicidin-S analogue ( Angew.Chem., Int. Ed. Engl . 2006 , 45 , 5659-5661) |
Cell-penetrating peptide SAP-E ( ChemBioChem 2011, 12 , 896-903) |
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CF3-Labeled SAP analogue ( Angew. Chem. Int. Ed. 2008 , 47 , 5765 –5767 ) |
26 September 2011
Recently Enamine has further improved the high-throughput synthesis workflow used for preparation of compounds offered through the REAL Database. Removal of production bottlenecks, application of optimized technological solutions and expansion of high performance preparative flash chromatography unit allowed us to shorten entire production cycle to 12-14 days. Currently we are able to produce up to 2,000 samples per month using this optimized procedure. 90% feasibility rate can be achieved after a single production cycle for typical compound sets. Compounds synthesized via the enhanced scheme can be delivered within 3 weeks after acceptance of an order.