09.30.2013 – ChemDiv Launches MacroLead (TM) Platform

Title: ChemDiv’s MacroLead (TM) Platform: A Novel Approach to Drug Discovery


In the field of drug discovery, the search for new and effective therapies is an ongoing challenge. To advance the discovery and development of novel drugs, biopharmaceutical companies continue to develop innovative technology platforms and novel approaches. In this blog, we will focus on ChemDiv’s MacroLead (TM) platform, launched in 2013, and its potential for revolutionizing drug discovery.

Key Points:

  1. The Drug Discovery Landscape:
    The drug discovery process involves identifying potential therapeutic targets, screening compounds for activity, and optimizing lead compounds for efficacy, selectivity, and safety. Despite significant progress in this field, developing new drugs remains a complex and resource-intensive endeavor, with a high failure rate.
  2. Introduction to MacroLead (TM):
    MacroLead (TM) is a proprietary technology platform developed by ChemDiv, a leading provider of discovery chemistry services and compounds. The platform involves a macrocycle-based drug discovery approach, where macrocycles, cyclic peptides or small molecules, are used to inhibit or modulate protein-protein interactions (PPIs).
  3. Challenges in Developing PPI Inhibitors:
    Protein-protein interactions represent a significant class of drug targets, with potential therapeutic applications across multiple diseases. However, developing potent and selective PPI inhibitors is challenging due to the large interfacial surfaces and flexibility of proteins involved. Macrocycles, with their unique structural features, offer an alternative approach to targeting PPIs.
  4. Advantages of MacroLead (TM):
    ChemDiv’s MacroLead (TM) platform offers several advantages over traditional drug discovery approaches. Macrocycles, with their larger size, increased conformational rigidity, and favorable pharmacokinetic properties, can overcome the limitations of small molecules in inhibiting PPIs. MacroLead (TM) enables rapid identification and optimization of macrocycles, potentially reducing the time and cost associated with drug discovery.
  5. Applications in Drug Development:
    The MacroLead (TM) platform has broad potential applications in drug development, particularly in oncology and immunology. PPIs play a crucial role in cancer and immune system signaling pathways, and inhibiting or modulating these interactions can offer potential therapeutic benefits. ChemDiv’s MacroLead (TM) can aid in developing potent and selective PPI inhibitors for these indications, opening doors for tailored therapies with improved patient outcomes.
  6. Collaborative Approach to Drug Discovery:
    ChemDiv’s MacroLead (TM) platform offers a collaborative approach to drug discovery. The platform is accessible to biopharmaceutical companies seeking novel drug targets and discovery chemistry services. The MacroLead (TM) platform enables researchers to leverage ChemDiv’s chemical library, expertise, and advanced screening capabilities to identify and optimize macrocycles with potent PPI inhibition properties.
  7. Importance of Technology Platforms in Drug Discovery:
    Innovative technology platforms like MacroLead (TM) have the potential to expedite drug discovery, reduce costs, and improve overall treatment outcomes. By providing a novel approach to targeting PPIs, MacroLead (TM) offers potential therapeutic benefits over traditional drug discovery approaches.
  8. Future Directions:
    The launch of MacroLead (TM) represents a significant milestone in ChemDiv’s mission to advance drug discovery through innovative technology platforms. Ongoing research and development are necessary to identify additional macrocyclic compounds with unique properties and develop optimized PPI inhibitors for clinical use.


ChemDiv’s MacroLead (TM) platform offers a novel approach to drug discovery, leveraging the unique properties of macrocycles to target protein-protein interactions. This platform has the potential to accelerate the drug discovery process, reduce costs, and improve patient outcomes. As innovative technology platforms continue to pave the way for more effective therapies, the MacroLead (TM) platform highlights the importance of collaborative research efforts in advancing drug discovery. With continued research and development, the MacroLead (TM) platform offers significant promise for the discovery and development of new drugs with potential therapeutic applications across multiple indications.