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Reach out to new chemical space breaking the availability bias:
11 000 000 000 molecules and beyond

REAL compounds

The world’s largest collection of building blocks in stock:
169 144 and counting

New Building Blocks

Run HTS directly at Enamine or have your copy from
Ever-expanding collection of 3 million compounds

Screening Libraries & HTS

120 000 Fragment compounds
including 10 000 covalent binders

Fragments

A broad test panel to support lead discovery
Integrated projects or a-la-carte service

ADME/T & in-vivo PK

Scientific research and development of techniques for the synthesis of organic compounds

High Fidelity Fragments

High Fidelity Library

Fragments of high MedChem tractability  

REAL Database

The largest enumerated database of synthetically feasible molecules

Functional Compounds

Impurity Reference Standards
 

Covalent Fragments

Covalent Fragments

Diverse covalent warheads with balanced reactivity

2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from May 2019

Recent News

  • 26 March 2019   Press Releases

    Enamine extends multi-year drug discovery collaboration with Lundbeck

    Enamine and H. Lundbeck A/S (Lundbeck) announced the expansion of their research collaboration. Enamine will support Lundbeck’s in-house discovery chemistry competencies with three principal assets enabling Lundbeck to optimally identify and develop hit series in its multiple research programs. A large diverse library of 100 000 new screening compounds was done for hit finding activities on numerous therapeutic targets. Enamine’s make-on-demand REAL compounds are for efficient access to billions of novel chemical compounds. Enamine FTE increased dedicated team of chemists to effectively support Lundbeck on all hit related follow-up activities backed by immediate access to over 170 000 building blocks in Enamine’s inventory.

    Read press release

  • 12 February 2019   News

    Enamine to Support Large-scale Hit Discovery Programs via New ...

    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.

  • 05 February 2019   News

    Horizon 2020 Project PELICO, Coordinated by Enamine, Achieves Promising ...

    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.

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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