Implexsys Therapeutics

Precision medicines for intractable targets

A transformational small-molecule platform for rapid hit discovery and optimization against difficult-to-drug targets, taking fragments rapidly to development candidates.

The challenge

Compelling but difficult-to-drug targets

Many compelling, disease-relevant drug targets have resisted traditional small-molecule drug discovery approaches.

Two kinds of target

Oral small-molecule therapeutic opportunities

A

Novel, difficult-to-drug targets

Promising new biology that conventional small-molecule approaches have not been able to address.

B

Targets already validated by biologics

Biology already proven by antibodies and other biologics, but still lacking a small-molecule medicine.

Both often share the same hurdles

  • No obvious druggable binding pocket
  • Flat or dynamic surfaces, such as protein–protein interactions
  • Highly conserved orthosteric binding sites, which make selectivity difficult
What it takes

The common bottleneck

Finding functional starting points, and turning them efficiently into development candidates.

Platform overview

Rapid hit to development candidate

A transformational small-molecule platform for rapid hit discovery and optimization against difficult-to-drug targets. It overcomes two longstanding challenges in fragment-based drug discovery (FBDD): dependence on biophysical screening, and the risk, time and cost required to transform weak binders into potent, functionally active leads.

  • 1
    Removes dependence on biophysical screening

    Breakthrough technology for functional screening of fragments combined with an AI-assisted SMART fragment library.

  • 2
    Vastly accelerated path from fragment hit to DC

    An automated, integrated chem-bio platform rapidly generates large, high-quality SAR data sets, with AI-enabled iterative data analysis and optimization.

  • 3
    Orthosteric and allosteric

    Highly effective for both orthosteric and allosteric modulators of difficult-to-drug targets.

Potency (Kd / Ki / IC50) vs. molecular weight (Da). Traditional fragment elaboration (purple) compared with the Implexsys platform (orange). LE = ligand efficiency.
Our pipeline

Implexsys is developing a pipeline of small-molecule therapeutics against difficult-to-drug targets, with an initial focus on oncology and immunology.

OncologyImmunology