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Reach out to new chemical space breaking the availability bias:
14 000 000 000 molecules and beyond

REAL compounds

NEWS

Feb 20, 2020

Feb 20, 2020

New chemotypes from virtual libraries: screening of Enamine REAL Database reveals in vivo hits

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. Read More >

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Ever-expanding collection of 3 million compounds

Screening Libraries & HTS

NEWS

Dec 12, 2019

Dec 12, 2019

New RNA targeted library has been created!

“The number of targets, the number of diseases that one could go after by targeting RNA, is almost unimaginable,” says Matt Disney, a chemist at the Scripps Research Institute.

In response to growing interest and recent advancements in targeting RNA our experts designed dedicated library of small molecules predicted to bind to RNA targets. In contrast to the classical protein targets and disease treatment, drugging RNA reveals absolutely new way to treat and prevent different disorders.

Our freshly-made library is ready for fast shipment within a week in various custom formats.

RNA Library contains 8 960 compounds. Read more>>

120 000 Fragment compounds
including 10 000 covalent binders

Fragments

NEWS

June 25, 2019

June 25, 2019

Enamine’s covalent fragments
produce potent and unique hits

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.

A refined library used in the research with a few frequent hitters and excessively reactive fragments removed is available from Enamine on request >

Ref.: J. Am. Chem. Soc. 2019, 141, 8951−8968

The world’s largest collection of building blocks in stock:
184 345 and counting

New Building Blocks

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

EDF在线老虎机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 January 2020

Recent News

  • 20 February 2020   News

    New chemotypes from virtual libraries: screening of Enamine REAL ...

    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.

  • 19 November 2019   Press Releases

    Optibrium collaborates with Enamine and BioSolveIT to add REAL ...

    Optibrium™, BioSolveIT™ and Enamine™ today announce a three-way collaboration enabling efficient search of Enamine’s REAL Space directly from within Optibrium’s StarDrop™ software. This extension to StarDrop is powered by BioSolveIT’s proprietary Feature Trees (FTrees) technology, to search a gigantic chemical space of over 11 billion readily accessible compounds and identify novel compounds that are similar to a query structure of interest. The resulting chemical structures and data are pre-formatted and ready to evaluate using StarDrop’s comprehensive suite of integrated software for small molecule design, optimisation and data analysis.

    EDF在线老虎机Read press release

  • 05 November 2019   Press Releases

    Cyclica Collaborates With Enamine to Use REAL Technology in ...

    EDF在线老虎机Cyclica, Inc. announced a collaboration with Enamine Ltd. to explore its huge readily accessible chemical space using Cyclica’s state-of-the-art AI-driven Ligand Design™ platform. The companies aim to empower Cyclica’s patented, evolutionary algorithm with new design options based on the 73,000 Enamine’s in-stock building blocks and 171 thoroughly validated synthesis procedures. The joint effort is expected to enable Cyclica’s Ligand Design™ to identify novel molecules with desired polypharmacological properties out of over 11 billion REAL™ (readily accessible) compounds. At least 80% of these compounds will be synthesized by Enamine within only 3-4 weeks.

    Read press release

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J. Fluorine Chem. , 2013, 152 136-143

DOI: 10.1016/j.jfluchem.2013.03.002

Kubyshkin V. S.; Mykhailiuk P. K.; Afonin S.; Grage S. L.; Komarov I. V.; Ulrich A. S.

Trans-4,5-Difluoromethano-proline was incorporated into the cyclic antimicrobial peptide gramicidin S in place of a native proline residue. Introduction of this intrinsically unstable amino acid into the polypeptide backbone was achieved using a dipeptide strategy. The stable dipeptide building block with the N-acylated 4,5-difluoromethano-proline fragment was obtained by direct difluorocyclopropanation of an unsaturated precursor. The influence of the unnatural amino acid on the conformation and function of gramicidin S was evaluated using circular dichroism and biological assays. The application of trans-4,5-difluoromethano-proline as a new label for solid state 19F NMR structure analysis of membrane-active peptides was tested on gramicidin S and compared with previous labeling schemes.

Incorporation of labile trans-4,5-difluoromethanoproline into a peptide as a stable label for 19F NMR structure analysis

Kubyshkin V. S.; Mykhailiuk P. K.; Afonin S.; Grage S. L.; Komarov I. V.; Ulrich A. S.
J. Fluorine Chem. 2013, 152 136-143
EDF在线老虎机 DOI: 10.1016/j.jfluchem.2013.03.002

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