Ready-to-use sets to support your discoveries
We at Enamine are constantly working on creating novel molecules and innovative synthetic pathways for the Drug Discovery Community. We carefully designed and synthesized a series of E3 binders with attached linkers of different lengths and natures to support Degrader Research and Development. One of our recent focuses is the derivatization of the von Hippel-Lindau (VHL) Cullin RING E3 ligase binders.
Our kits provide a robust selection of pre-synthesized VHL ligands (VHL 032, Me-VHL 032, VHL 101-phenol, and VHL 285-phenol) conjugated to linkers with varying lengths and compositions. This comprehensive offer goes beyond standard PEG- and Carba-linkers, including rigid/cyclic linkers proven effective in bifunctional molecule design.
Linker’s terminal functional groups can be easily modified through the most straightforward reactions – amide coupling or click-chemistry.
Product catalog
Product name
VHL Amine Kit-1
Amine-1-227
Description
VHL 032 and Me-VHL 032 derivatized with most comprehensive and diverse linkers of variable length from 2 to 18 heavy atoms in a chain with terminal amine functional group
Key features
- Easy access, ready for delivery in plates as 20 mM solutions in DMSO
- Variation VHL ligand
- Variable in length from 4 up to 18 heavy atoms
- Well-balanced composition including PEG-, Carba- and Rigid-linkers
Screening collections play a pivotal role in early-stage drug discovery, providing a flexible platform compatible with many advanced methods. Our collaboration with UORSY has led to the creation of a joint collection of screening compounds named 'Legacy', reflecting the rich scientific heritage of Ukrainian suppliers. This collection has resulted from our 15 years of efforts in supporting drug discovery through high-throughput screening and comprises over 1.76 million in-stock screening compounds.
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We provide compounds synthesized from in-house synthesized building blocks using meticulously developed and optimized reactions. More than 50% of our compounds have drug-like physicochemical properties, and over 40% - lead-like profiles.
Key features:
- 11.2% shaped molecules (9.3% disc & 1.9% sphere)
- 4.9% high QED (QED=0.9)
- 3.7% PAINS
- 2.7% fragment-like compounds
- 0.8% natural-like compounds
- 100% affordable prices
Availability, packaging, and quality control
The compounds are available in milligram amounts, typically 1-20 mg, sufficient for a fast re-supply of the hits. The samples are mainly stored as dry powders and can be supplied either neat or as DMSO solutions in virtually any applicable format. All Enamine compounds undergo rigorous quality control with LCMS and/or 1H NMR to meet the standard of at least 90% purity.
Selecting the right compounds for your project
Our experienced team of Medicinal & Computational chemistry team is ready to assist you choose a hit-finding strategy tailored to your specific needs.
Discover the Legacy Screening Collection on , where you can explore compounds using text, substructure, and similarity enaminestore.com queries.
Molecular properties
6 692 compounds in stock
1 360 pre-plated compounds
Vinyl sulfones and sulfonamides are among the most common and efficient Michael acceptors and are good alternatives to acrylamides. This class of covalent binders attracted much attention with several representatives being in different stages of clinical trials. The recent investigation described by Adam Gilbert and co-workers using N-acetyl lysine and glutathione showed that vinyl sulfonyl derivatives in general are more reactive than acrylamides and sulfones are more active over sulfonamides. Last but not least vinyl sulfone and vinyl sulfonamide warheads displayed some selectivity toward Lys over cysteine residue if compared to popular acrylamide electrophiles.
Several recent examples of successful application of vinyl sulfones in drug discovery include irreversible protease inhibitor K11777 targeting noncatalytic Cys25, the first irreversible ATP-competitive inhibitor of CDK2 NU6300 targeting Lys89, FT827 potent covalent inhibitor of USP7 and promising SARS-CoV-2 Main protease inhibitor which covalently binds to Cys145.
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6 692 compounds for cherry-picking
Plated libraries in stock:
Version: 9 January 2024
320 pre-plated compounds
sublibrary of LYS-1600
Examples of vinyl sulfones and sulfonamides in pre-plated sets
Promising and more stable isosteres of acrylamides
724 compounds in stock 320 pre-plated compounds
Bicyclo[1.1.0]butane carboxylic amides emerged as a new class of Cys-focused electrophiles. They are considered as bioisosters of acrylamides, but their increased stability and unique reactivity can result in the development of new selective covalent binders.
We offer over 700 compounds from stock and continuously work on the synthesis of new derivatives. You can select from our growing REAL Array of currently 1 million strained bicyclobutanes and be the first to try them on your target. Synthesis of hundreds of compounds will take us a few weeks only.
New Bioisosteres of Acrylamides readily available through custom parallel synthesis and from our REAL Array
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The chemistry of bicyclo[1.1.0]butane (BCB) derivatives is vividly developing. Strained hydrocarbons (e.g., EN300-298918) were proposed by Baran as suitable candidates for selective covalent labeling of Cys-residues in polypeptides. In his study, the reactivity of bicyclo[1.1.0]butyl aryl sulfones was similar to that of acrylamides in GSH-assay. Recently, Ojida introduced BCB-amide as a covalent warhead, targeting cysteine residue. These molecules are easy to synthesize from BCB-carboxylic acid and diverse amines. Importantly, BCB-amides were tested in Ramos cells, which shows their compatibility with biological systems.
BCBs represent a novel perspective area for developing new selective covalent inhibitors. We are continuously working on the enumeration and synthesis of new strained bicyclobutane derivatives.
Examples of Bicyclobutane amides in stock
Ready-to-use sets to support your discoveries
The field of bifunctional molecules is experiencing explosive growth. To address this, Enamine has prioritized the preparation of ligand-linker conjugates as intermediates. These pre-designed building blocks significantly simplify research by enabling the rapid and efficient synthesis of bifunctional molecule libraries.
