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Enamine’s covalent fragments produce potent and unique hits

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.

Purification capabilities enhanced

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.

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