|Asinex Building Blocks||27122 Compounds|
|ASINEX’s building block encompasses the legacy of our synthetic know-how and 20+ years of medicinal chemistry expertise with an ultimate goal of delivering novel, valuable chemical monomers for increasingly challenging drug discovery programs.|
In addition to commonly popular functionalities, ASINEX building blocks represent the diversity of other valuable functional groups including alkenes, epoxides, amino alcohols and polyfunctional entities, which are especially useful for template-based generation of compound libraries where a polyfunctional building block can serve as a core scaffolding structure.
ASINEX Building Blocks have been validated for both chemical stability and reactivity. Many of these building blocks have been utilized for the synthesis of our natural product-like and macrocyclic libraries as well as for advancing a number of hit-to-lead optimization projects.
|Asinex Building Blocks |
For DNA-encoded libraries
|DNA-encode libraries (DEL) are a valuable discovery tool for the identification of promising hits against multiple challenging targets. Compounds in DNA encoded libraries are synthesized form chemical building blocks exploiting DNA-compatible combinatorial chemistry. Strategic selection of building blocks helps generate excellent chemical diversity in library generation. Specific polyfunctional monomers provide an additional advantage as they can be flexibly applied to all established DEL enabling strategies: templated synthesis, combinatorial “split-and-pool’’ etc.|
At ASINEX we have created several hundred bi and tri-functional low MW monomers providing flexibility in DNA tagging chemistry and allowing further opportunity for molecule growth and linking.
(+ Macrocyclic Fragments)
|Our “BioDesign” approach incorporates key structural features of known pharmacologically relevant natural products (e.g. alkaloids and other secondary metabolites) into synthetically feasible medicinal chemistry scaffolds. In order to identify the privileged pharmacophores, ring systems and linkers, we have carried out statistical analysis of structural features of natural products, marketed drugs, and drug candidates. Our research shows that saturated fused ring, spiro, and bridged systems with a tendency towards multiple chiral centers are highly privileged among natural products and marketed drugs yet these structures are very poorly represented in commercial libraries. We deliberately introduced these highly privileged elements in the design of novel fragments with a higher level of saturation, multiple chiral centers and a high diversity of natural product-like frameworks.|
|Asinex Fragments||21872 Compounds|
|ASINEX’s fragments encompass tremendous diversity of our scaffold and synthetic handles that allows straightforward progress from fragments to leads. The subsets of fragments suitable for specific biochemical and/or biophysical screening methods are available upon request.|