Please join us for a webinar "Hit Discovery for GPCRs: HTS or Virtual Screens?” presented by Guest Speaker, Carleton Sage, PhD, Vice President of Computational Sciences at Eurofins, Beacon Discovery on Thursday, June 24, 2021
We still have several funded Postdoc positions in organic chemistry to work at Enamine Ltd. (Ukraine, Kyiv) on a ERC-project “Saturated bioisosteres of benzene.”
We are happy to announce the start of Project ALISE supported by European Commission under Horizon 2020 MSCA-RISE. As the coordinator of the Project, Enamine is involved in the development of light-controllable antibody peptide conjugates pushing the boundaries of photopharmacology towards clinical applications.
We have several Postdoc positions in organic chemistry to work at Enamine Ltd. (Ukraine, Kyiv) on a ERC-project “Saturated bioisosteres of benzene.” Start: 1 April 2021 (or later).
Congratulations to Pavel Mykhailiuk, Chief Scientific Officer at Enamine, for receiving ERC Consolidator Grant funding for the Project: BENOVELTY - Saturated bioisosteres of benzene and their application in drug design.
The research will be carried out at Enamine Ltd in Ukraine, a global provider of chemical and biological services to biotech companies, academic institutions and research organisations.
Enamine will provide chemical synthesis support for a global nonprofit research initiative OpenPandemics COVID-19, organized by Scripps Research and IBM, and aimed at rapidly identifying efficient new drugs against the coronavirus SARS-CoV-2. Enamine will be synthesizing any promising hits identified by the research team at OpenPandemics COVID-19 via large scale docking experiments.
An international group of scientists from academia and industry, including Enamine, is trying to help combat COVID-19. This effort began when Chinese scientists worked rapidly to determine the structure of the novel SARS‑CoV‑2 main protease (Mpro), which triggered a massive crystal-based fragment screen at the XChem facility at UK’s Diamond Light Source. For more details, please visit https://www.diamond.ac.uk/covid-19. With the same urgency, the scientists are now trying to progress these data towards what is desperately needed: effective, easy-to-make anti-COVID drugs https://covid.postera.ai/covid.
We are delighted to announce another application of Enamine REAL database recently published in Nature. This paper is a result of the collaborative effort of scientists from Enamine and the leading academic institutions from the USA and Germany.
Melatonin (MT) receptors are established drug targets for aligning circadian phase in disorders of sleep and depression. But there are only a few in vivo hits reported to date. Enamine scientists along with the scientists from UCSF, UNC, USC, and other institutions participated in the research study aimed to fill the gap in therapeutics of these receptors.
Meet our delegates at International Symposium on DEL in Zurich to learn on our approaches in selecting DEL-compatible building blocks and on our advances in intriguing designs of novel chemotypes >>>
In continuation of our efforts to make affordable screening libraries that can quickly be supplied for screening, we have plated two new targeted libraries designed to bring high quality and novelty to your hit finding program. Both freshly-made libraries are ready for fast shipment within only one week in various formats including assay-ready plates.
In a recent JACS paper several academic groups collaborated on discovery of novel covalent inhibitors using a library of 993 acrylamides and chloroacetamides sourced from Enamine’s covalent fragment collection. The design was focusing on mild electrophiles that were supposed to overcome the selectivity challenge. The library was characterized by a new high-throughput thiol-reactivity assay and screened against 10 cysteine-containing proteins. Potent and unique primary hits have been found in the majority (7 out of 10) of cases.
Scientists at the UCSF, together with colleagues at the UNC, created the largest “docking-friendly” database of molecules, based on the Readily Accessible (REAL) compounds from Enamine. Practical validation of the new database was recently published in Nature magazine, demonstrating that it is capable of identifying extremely powerful and synthetically available new hits.
Horizon 2020 Project PELICO, Coordinated by Enamine, Achieves Promising Results in Peptidomimetics Synthesis
EU-funded project PELICO, under Enamine’s coordination, reports promising results in synthesis of peptides, their pharmacokinetic and toxicity studies, and coupling with photo-controlled building blocks to yield new photo-controlled peptidomimetics.
The demand for library synthesis at Enamine driven by the on-site access to the world’s largest and most reputable stock of building block has multiplied in 2018. We keep developing our preparative chromatography capabilities to sustain the drastically increasing number of compounds produced.
Enamine's chemists and biologists from Bienta just published an article in ACS Comb. Sci. describing design and synthesis of a new sulfonyl-fluoride-based covalent fragment library. The library was validated by screening against a model protease, trypsin, and some fragment hits were identified. See ACS website for more details.
Our compound management team at Enamine is excited about the recent acquisition of the Echo® 550 Liquid Handler from Labcyte. This robotic superhero is expected to significantly speed up and notably precise compound handling, which is exactly an option needed for 2.5 Million+ compounds in stock. Screening libraries at Enamine are now more accessible, more customized and assay-ready to meet your exact needs in compound screening.
680 million new compounds: REAL Database doubled its size in the new release and offers 20% off for the selections of analogues made online at EnamineStore.com.
Accessing new chemistry for drug discovery has been recently facilitated by the approach developed by John Irwin et al. (DOI: 10.1021/acs.jcim.7b00316). Combination of Similarity Ensemble Approach (SEA) with the maximum Tanimoto similarity to the nearest bioactive was found to provide efficient prediction for all 400 million commercially available compounds in ZINC database including 340 million Enamine’s REAL compounds. You can access the files at https://zinc15.docking.org and http://files.docking.org/catalogs/20/enamine-v/. REAL compounds will be synthesized at Enamine on your request in less than 3 weeks with over 85% success rate!
A New Synthetic Route Reported For 1-(Trimethylsilyl)vinyl MIDA boronate, A Suitable Trifunctional Building Block
Recent publicationby our chemists describes gram-scale synthesis and some chemical transformations of novel trifunctional C 2building blocks – MIDA boronate shown below.