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Linkerology

    Linkers belong to the key component of PROTACs and other heterobifunctional molecules. Numerous scientific studies suggest that the linker’s length, polarity, and rigidity can play a crucial role in the tertiary complex formation, its stability, and the pharmacokinetic (PK) properties of the bifunctional molecules.

    Enamine Germany provides a wide assortment of linker molecules from stock. They can be used for the rapid design and synthesis of different bifunctional molecules.

    Linear Linkers are important to designing and investigating PROTACs, DUBTAGs, and other bifunctional molecules. Enamine offers a diverse collection of building blocks for the construction of linear PEG- and carba-linkers with different lengths, tail functional groups (FGs), and compositions. This collection is continuously enriched with new compounds from our synthesis program.

    Advanced Linkers. More complex linkers, containing strained structures have become popular in the last couple of years. These advanced linkers contain in their structure cycles, spirocycles, double and triple bonds, and multiple heteroatoms. Based on the literature data, we singled out the general structural criteria and selected the corresponding linker Building Blocks from our stock. We can also readily synthesize any other linker molecules upon your request.

Types of Linkers
    Mono-Boc diamines are the most popular Linkers in the design of bifunctional molecules (first of all PROTACs). Various diamine linkers can be found in the structures of the drug candidates such as ARV-110, ARV-471, CFT8634, and FHD‑609. Enamine Germany provides an outstanding collection of diverse diamines (by flexibility/distance/shape/polarity) which are useful for linkerology studies of new bifunctional molecules.
Other Linkers.  Besides diamines, other linkers with diverse end-functional groups are widely used in the design of bifunctional molecules. Enamine provides various linkers with different combinations of functional
groups (e.g., OH/halogen-acetylenes, amino acids, aminoacetylenes, aminoazides). Upon request, we can propose a set of linker Building Blocks according to your criteria.

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