Hit Identification and Lead Generation in Pancreatic Cancer

Alfa Cytology is a full-scale preclinical research service provider with extensive experience. Based on state-of-the-art platforms and resources, our experienced scientists will work with you to determine the optimal strategy to advance your hit finding and hit-to-lead research. Here, we provide hit identification and lead generation service, part of our integrated small molecule drug development for pancreatic cancer (PC).

Introduction to Hit Identification and Lead Generation

Drug identification and lead compound generation play a crucial role in the early stages of drug discovery. Furthermore, lead compound optimization is required.

• Target Compound Identification (Hit ID): This is the process of identifying compounds with an established biological target activity. It is usually achieved by high-throughput screening (HTS), in which many compounds are tested for their ability to interact with a specific target.
• Lead compound generation: Once a promising drug has been identified, the goal is to generate lead compounds, molecules with superior properties such as potency, selectivity, and manageable toxicity. This is known as the lead compound generation (H2L) stage. The ultimate goal is to identify drug candidates that balance these properties best.

Fig. 1 Lead compound generation represents a critical stage in drug discovery. (Holenz J, Stoy P.; 2018)

Our Services

Our small molecule drug discovery project team uses hit identification approaches that mix design and screening elements. To get as many accurate hits as possible, our team's design hit strategy begins with the goal of carefully reviewing and evaluating what appropriate methods will be followed. With a range of orthogonal methods, we are able to deliver high-quality, validated hit compounds to our customers.

• High-Throughput Screening (HTS)

High throughput screening (HTS) is an effective tool for the rapid identification of promising compounds. As a relatively unbiased approach, HTS can identify compounds with novel binding modes. Our platform integrates comprehensive HTS screening technology, as well as proven HTS assay design and execution. We have the capability to screen for the identification of hit compounds using our own libraries or libraries provided to us by our customers for HTS screening in drug discovery.

• Fragment Discovery

Fragment screening, also known as fragment-based drug discovery (FBDD) is another type of screening. Compared to HTS, only a limited number of compounds (typically 1000) are screened in FBDD with a relatively low molecular weight of (<300), aiming to identify weak effective fragment hits (~100 μM). Using this approach, we can help researchers obtain effective small molecule inhibitors whenever possible.

• Virtual Screening

Virtual screening is a method for selecting compounds from large databases using computational tools and millions of compounds can thus be analyzed by this method. Virtual screening offers significant advantages over physical screening, including faster, less resource-intensive screening, and even screening for unavailable compounds. We can offer structure-based and ligand-based drug design and virtual screening. Using advanced modeling techniques and data analysis methods, we can support small molecule inhibitor discovery for PC therapy from hit identification to lead optimization.

• Compound Libraries

We have a diverse compound library that is constantly being expanded. A variety of compounds with more relaxed structures are suitable for a wide range of targets. Fragment compound libraries consist of approximately 2,400 fragments with optimized properties for fragment screening. Notably, we also offer compound library design services. Customized screening libraries are based on customer requirements, time, and budgets.

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If you are interested in our services, please contact us for more details. You can get in touch with our staff directly and receive professional, reliable, and fast feedback.

Reference

1. Holenz J, Stoy P. Advances in Lead Generation. Bioorg Med Chem Lett. 2019;29(4):517-524. doi:10.1016/j.bmcl.2018.12.001