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.
Scientists at the UCSF, together with colleagues at the UNC, created the largest “docking-friendly” database of molecules, based on the Readily Accessible (REAL) compounds from Enamine. Practical validation of the new database was recently published in Nature magazine, demonstrating that it is capable of identifying extremely powerful and synthetically available new hits.
Horizon 2020 Project PELICO, Coordinated by Enamine, Achieves Promising Results in Peptidomimetics Synthesis
EU-funded project PELICO, under Enamine’s coordination, reports promising results in synthesis of peptides, their pharmacokinetic and toxicity studies, and coupling with photo-controlled building blocks to yield new photo-controlled peptidomimetics.
The demand for library synthesis at Enamine driven by the on-site access to the world’s largest and most reputable stock of building block has multiplied in 2018. We keep developing our preparative chromatography capabilities to sustain the drastically increasing number of compounds produced.
Enamine's chemists and biologists from Bienta just published an article in ACS Comb. Sci. describing design and synthesis of a new sulfonyl-fluoride-based covalent fragment library. The library was validated by screening against a model protease, trypsin, and some fragment hits were identified. See ACS website for more details.