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Unit Head: Steven Harper [Ph. D.]

As a leader in medicinal chemistry research and custom synthesis, we provide partners with compound synthesis options and support across the full spectrum of preclinical drug discovery. Our partners greatly appreciate our pragmatic and results-oriented approach to both synthetic and drug discovery projects, as well as our ability to rapidly solicit multi-disciplinary support within IRBM toward overcoming scientific and practical challenges.

IRBMOur team has a strong synthetic pedigree and experience across a range of structural classes including peptidomimetics, steroids, nucleosides and a vast number of heterocyclic drug scaffolds. Our facilities are state of the art, allowing both single compound and parallel synthesis, employing the most modern transition metal catalysed couplings, organocatalysis and photoredox chemistries.

Our legacy in drug research includes the discovery of three marketed drugs (Isentress®, Grazoprevir® and Zejula®) and over 30 preclinical and clinical development compounds. Our experience across a range of different disease areas continues to expand, and includes oncology, antivirals, diabetes, obesity, cardiovascular and CNS indications.

Our know-how in advancing integrated drug discovery projects adds value to our partner’s research both in the early phases and late stage of preclinical drug discovery.

Unit Capabilities

Custom synthesis

  • mg to kg scale synthesis of key compounds (up to 20L reaction vessels);
  • chemistry route scouting expertise;
  • impurity isolation, identification and de novo synthesis to support process chemistry;
  • stable isotopic labelled compound synthesis;
  • chemical libraries / parallel synthesis;
  • chiral synthesis / separations.

Drug Discovery

  • HTS follow-up and hit to lead chemistries;
  • SAR expansion and lead optimisation;
  • structure-based design and computational chemistry guided approaches;
  • optimisation of molecular properties for CNS penetration;
  • strategic approaches to reduce cycle time.

Support

  • strong integration of NMR support in both compound identification and medicinal chemistry;
  • chiral SFC chromatography;
  • automated compound handling, purification and QC;
  • curated in-house chemical compound collections (c. 350,000 compounds);
  • integrated computational chemistry and IT platforms.