Technology

LCGC established a powerful, automated molecular-diversity server called the NanoTube Automated Repository Server (NARS) with a dynamic storage capacity of 10-million samples in a frozen, dehumidified environment with a cherry-picking throughput of 10,000 samples per day. The NARS stores replicate ‘single-shot’ aliquots of up to 50 uL per individually-addressable storage container. NARS provides unparalleled, ultra-rapid access to the largest chemical libraries, without freeze-thawing, thereby preserving the integrity of the entire collection indefinitely.

For a brochure of our NARS system, click here.

In addition to the NARS repository, LCGC has acquired a unique compound library of 120,000 members. We have powder reserves of 10 mg each. The file was acquired with a unique computational and ‘medicinal bias’ that differs from a typical approach. These compounds pass all Lipinski and drug reactivity filters typically used in pharma to qualify drug-like libraries for high throughput screening (HTS). Creation of focused libraries is easily accomplished for thousands of compounds in days, rather than weeks, drug discovery research.

For a brochure of our HTS library, click here.

The LCGC library was formatted by a method allowing for abbreviated HTS, referred to as orthogonal compression of compound libraries (OCL), that enables five-fold improvement in lead-finding ability compared to present practice in HTS. The approach pools the compounds contained on 100 microtiter plates into ten plates, distributed across two independent dimensional arrays orthogonal to each other, yielding a total of only 20 plates. Each compound is represented twice, surrounded by nine different molecules in each well. Our approach is to prepare OCL on a set of five (5) 384-well plates containing 8,000 compounds. This OCL methods extends the capacity of large scale screening enterprises and provides an entry point for smaller labs to complete HTS without large technology budgets. Published studies support that when properly applied, OCL can markedly reduce the resources required for successful HTS (Motlekar N, et al., Assay. Drug. Dev. Technol. (2008) 395-405; Ferrand S, et al., Assay Drug. Dev. Technol. (2005) 395-405).

In collaboration with Chip Allee of CeuticalSoft we have developed innovative software that extracts maximum value from the OCL method. The 10XY module can be run as stand-alone workbook with all the plate and compound data embedded for a single set of mixture plates or it can be run as a fully integrated database application with full access to large mixture plate collections.

In essence, what LCGC has put in place a multi-million dollar drug discovery infrastructure and to make it affordably available. Enhancing HTS efficiency to discover novel drug leadsquickly and reliably could represent a transformative contribution to the drug discovery field, especially for smaller laboratories at biotechnology startups and throughout academia.