In developing its proprietary CMRT (“smart,” Customized Macrocycles for Recognition of Topologies) Technology, the Cyclenium team focussed on the correction of deficiencies, in particular relating to drug-likeness, in earlier approaches, and designed the QUEST Library to possess the following key attributes:

  • Broad spatial coverage and superior topological diversity
  • Unique structures outside existing patents in macrocycle space
  • Congruent with drug-likeness criteria of Lipinsky and Veber
  • In-line with current industry standards for physicochemical properties and stability of classical small molecules
  • Displaying preferred structural elements for protein-protein interactions and brain penetration
  • Minimal off-target activity and superior safety
  • Amenable for use in any HTS system
  • Modular assembly that enables rapid solid-phase synthesis and high-throughput optimization
  • Easy scalability in solution, reasonable manufacturing costs
  • Amenable to standard formulation approaches

Cyclenium CMRT Technology Advantages

  • Alternative to biological drugs (antibodies, proteins, peptides, oligonucleotides)
  • Orally bioavailable and blood-brain-barrier (BBB) penetrating compounds
  • Compounds that behave like traditional small molecules regarding stability, PK/PD properties, development
  • Well suited to track historically poorly accessible drug targets in broad range of therapeutic areas
  • Offers an underexplored chemical class as an attractive alternative to the typical heterocyclic small molecules that dominate current pharmaceutical compound collections.
brown and black round beads

Macrocyclic Drug Discovery

  • Covers unexploited molecular space between traditional small molecules and large bio-molecules
  • Cyclic chemical structures with ring sizes of generally >12 atoms
  • Captures pharmacological properties of larger peptides/proteins in metabolically stable small molecules
  • Offers excellent target fit, high potency and exquisite selectivity similar to biologics due to constrained and preorganized conformation
  • Potential to modulate complex drug targets with simple agents
  • Proven on broad range of target classes