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Target Validation

We use advanced cellular and molecular biology techniques on our automated platform to validate novel targets. Our approach is driven by our team’s scientific rigor and expertise coupled with technical excellence in fully automated experiment execution and data analysis, leading to faster progression into the next development stage.

  • Target expression and target half-live by quantifying protein turnover and route to degradation
  • Target function by investigating changes in phenotype, pathways, and gene expression using gene silencing and gene knockdown/ CRISPR-Cas9 coupled with various cell-based and molecular readouts such as imaging, cell health assays, metabolic assays, qRT-PCR & dPCR, RNA-Seq/ Tempo-Seq, and others
  • Advanced insights into effects of target modulation by employing complex models such as organoids and other 3D cell models

Hit Finding

We deploy both the latest in silico and well-established in vitro screening approaches to identify novel developable drug-like matter. This unique pairing of computational techniques (virtual screens, ML-guided molecule selection) and wet lab automation generates high quality hits faster and more efficiently compared to conventional approaches.

  • Machine learning guided screening set selection and hit evolution with enhanced hit rates
  • In silico screening, docking and molecular dynamics 
  • In vitro screening and profiling from as few as 5 molecules (for deep mechanistic studies) to full HTS (100k+ compounds)
  • Curated and focused libraries (fragments, diversity, natural products, therapeutic areas/ signalling pathways focused)
  • Compatibility and management of third-party and custom libraries
  • Biophysical screening/ profiling and fragment based drug discovery (FBDD)
  • Phenotypic screening by single molecule & synergy matrix screens, cell panels, and cell viability/ cytotoxicity assays

Hit-to-lead

We deliver rigorous validation and profiling of hits, with Ulysses enabling rich and detailed, quantitative structure-activity relationship (QSAR) mapping, as well as selectivity, kinetic and mechanism of action studies. Our platform returns a comprehensive evaluation of hits, enabling effective and reliable prioritization for progression to lead series.

  • Rapid synthetic hit expansion and diversification
  • Advanced medicinal and computer-aided drug design (CADD)
  • Ultra high definition kinetic and mechanistic biochemistry/ enzymology
  • Binary and ternary complex formation
  • Biophysical quantitation of target engagement energetics and kinetics (association/ dissociation)
  • Selectivity/ liability profiling and off-target binding
  • Bespoke screening cascades and functional cellular assays
  • Protein science and (co)crystallography for structure-based drug discovery (SBDD)

Lead optimization

Ulysses delivers accelerated lead optimization by drastically shortening the DMTA cycle time. High reliability precision data generated on our platform drives confident iteration through to candidate selection in a fraction of the time usually required. We continuously develop our library of pragmatic and elucidating assay cascades, leading to superior drug design and enhanced success rates. 

  • Rapid biochemical profiling, kinetics, selectivity, mechanism of action
  • Isolated and in-cell target engagement: Lumit/ NanoBRET, and healthy vs disease specificity using sets of cell-based assays
  • Cellular mode of action via generation of EC50s, elucidation of pathway modulation, and confirmation of on-target/ off-target effect
  • Medicinal and synthetic chemistry (optimising SAR/ SPR/ STR)
  • We integrate synthetic, medicinal and computational chemistry, as well as in vivo ADMET for late-stage lead optimization

Preclinical

En route to IND, comprehensive pharmacokinetics and pharmacodynamics studies and safety/ toxicology assessments are conducted. These involve both in vitro and in vivo studies, conducted in full compliance with all necessary regulatory requirements – bringing better drugs to patients sooner.

  • Pharmacokinetics and pharmacodynamics (PK/ PD) and safety pharmacology
  • In-depth pharmacokinetics, including ADME, drug-drug interactions, metabolite profiling, concentration time profiles
  • Comprehensive acute toxicology assessment, incl. single dose and repeated dose to determine MTD and NOAEL
  • Additional toxicology studies (including reproductive and developmental toxicity, immunotoxicity, genotoxicity, etc.)