|Poster: Designing PAMPA Permeable Macrocycles: Exploring Promising Directions in Early Drug Discovery Research|
Anna Rzepiela, Mark Parisi, Roman Kombarov, Ramon Moreno, Victor Tatarsky
April 23-27, 2017 - 12th Annual Drug Discovery Chemistry, San Diego, CA USA
|Signature Libraries||4800 compounds|
|ASINEX's cutting edge chemistry combined with in silico and in vitro screening validation. Favorable results are packaged in an easy to use, one plate format (80 compounds). For more information, please download >>>|
List of all "Signature Libraries" pleaseclick here.
|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 Glycomimetics||2048 compounds|
|Macrocyclic glycomimetics are an extremely interesting class of glycomimetics as they occupy space between small and macro molecules. Macrocyclic glycomimetics are mostly represented by naturally occurring molecules derived from marine microorganisms and bacterial or fungal metabolites. For more information, please download >>>|
|ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel and have allowed us to generate tremendously diverse, medchem-relevant, macrocyclic frameworks. Many of our macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay. For more information, please download >>>|