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Building Block Catalogue

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Building Blocks

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2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from March 2021

Recent News

  • 05 April 2021   News

    Open positions for Postdocs and Research Scientists

    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.”

    Start: any time.
    Please, send the application documents (motivation letter, CV, list of publications, recommendation letters) to Pavel.MykhailiukATmail.enamine.net

  • 01 March 2021   News

    Lumobiotics GmbH is part of an European consortial Project

    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.

  • 24 February 2021   Press Releases

    Enamine extend collaboration with prominent Swiss Biotech

    A new multi-year drug discovery agreement will focus on CNS drug discovery

    Kyiv, Ukraine, February 24 2021 - Enamine Ltd. a provider of drug discovery services empowered with the world’s largest collections of building blocks, fragments and screening compounds announced today that it has extended its long-standing research collaboration with Addex Therapeutics Ltd (SIX: ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical company specialized in allosteric modulation-based drug discovery and development. Enamine is providing Addex with its integrated capability in medicinal chemistry, pharmacology and ADME/PK (Absorption, Distribution, Metabolism, Excretion/Pharmacokinetics) to efficiently support Addex’ small molecule CNS drug discovery programs.

    Read press release

Upcoming events

Wnt/sFRP-1 Interaction Inhibitors Library

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1 346 compounds

This selection of small molecules takes into consideration Wnt/sFRP-1 (Secreted Frizzled Related Proteins) interaction. sFRP-1 family of proteins include endogenous molecules that bind both Wnt ligands and Fz receptors.

Fig. 1.Epigenetic inactivation of negative regulators of WNT signaling. (a) In cancer cells, epigenetic inactivation of SFRP and DKK enables β-catenin to translocate to the nucleus, which leads to activation of WNT signaling. (b) In normal cells, SFRP and DKK are associated with key WNT signaling molecules such as WNT ligands and LRP5/6, which prevent translocation of β-catenin to the nucleus (from Tohoku J. Exp. Med. 2010, 221, 11–17).

It is believed that inhibition of sFRP-1 would result in vicarious activation of Wnt signaling. In adition, WAY-316606 is a sFRP-1 inhibitor (K i= 80 nM) that was described to increase total bone area in a murine calvarial organ culture assay at < 1 nM concentration. It is also reported to be antiosteoporotic agent. WAY-262611 is a Wnt pathway agonist that increases bone formation rate with EC 50 of 0.63 uM in TCF-Luciferase assay. WAY-262611 exhibits good pharmacokinetic properties and a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration. Specific attention needs to be paid to monitoring specific organ toxicity associated with a long-term perturbation of Wnt pathway including neoplasia(s), although recent data suggest otherwise. Current (sub)library size is 1 346 compounds.

Fig. 2.(a) Pharmacophore model based on WAY-316606; orange – aromatic/heteroaromatic groups, green-hydrophobic pharmacophore (halogen, CF 3, CHF 2, Me, Et, iPr etc.), blue-positively charged moiety ( +NH 3Alk, +NH 2Alk 2, +NHAlk 3etc.); (b) Superposition of WAY-316606 and our pharmacophore construct used in (sub)library design.

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