X-Chem, Inc., a privately held biotechnology company focused on applying its powerful product engine to the generation of novel small molecule therapeutics, today announced that the company has created the first biotech-owned screening library of DNA-encoded small molecules to ever surpass 100 billion compounds. Its size now far exceeds that of even the largest conventional small molecule screening libraries by 10,000-fold, and its diversity is unprecedented. The library was created using the company’s cutting-edge and proprietary DNA-encoded platform. As described in a recent publication authored by X-Chem scientists ((Litovchick A, Clark MA, Keefe AD. Universal strategies for the DNA-encoding of libraries of small molecules using the chemical ligation of oligonucleotide tags. Artificial DNA: PNA & XNA 2014; vol.5, number 1)) a key advancement is a library synthesis process that enables the addition of a DNA tag using chemical methods.

X-Chem’s vision is to continuously increase the size and diversity of the library to enable identification of small molecules with the safety and efficacy profile of drug candidates directly out of the primary screen. To interrogate a library of such magnitude, the company has built a state-of-the-art screening platform designed to optimize detection and a suite of advanced bioinformatics tools capable of maximizing the signal-to-noise ratio when processing the massive quantities of data generated in the course of each screen.

“DNA-encoded library technology has achieved significant momentum in the drug discovery world. At X-Chem, we have pushed this technology to a new level, uniquely enabling the virtually unlimited expansion of our library and the ability to productively screen such a large number of compounds,” said Richard W. Wagner, Ph.D., Chief Executive Officer of X-Chem.

“Size and diversity of the library can radically improve the rate of lead discovery and also drive expansion of the universe of ‘druggable’ targets. This has the potential to dramatically increase the proportion of lead compounds that will result in safe, effective, and innovative medicines not conceivable previously and to accelerate the drug development process while also reducing its overall cost.” “We have licensed to our partners multiple novel, potent and selective compounds that target notoriously difficult-to-drug targets including, among others, protein:protein interaction (PPI) targets, ubiquitin ligases, antibacterial enzymes, and proteins involved in epigenetic processes,” said Diala Ezzeddine, Ph.D., Chief Business Officer of X-Chem.“Access to our game-changing drug discovery capabilities continues to enable breakthroughs for X-Chem’s partners on targets of high therapeutic value for which no ‘progressable’ small molecule had previously been identified.”