Our research and development platform spans the full range of technologies required to discover small molecule hits and develop them to clinical candidates. Critically, each of our novel drug discovery projects is underpinned by leading medical researchers with cutting edge expertise in the target biology.
High Throughput Screening
We access three established HTS facilities in Australia, taking advantage of their 30-plus years of combined operating experience. These facilities specialise in developing and miniaturising molecular, cell based and high content assays and together have prosecuted more than 100 HTS campaigns, many in collaboration with large pharmaceutical companies. CTx uses a purpose-built compound management facility with state of the art storage equipment and dispensing technology. CTx also draws on proven fragment screening expertise to identify high quality starting points for our medicinal chemists.
The CTx medicinal chemistry leadership team has more than 50 years of large pharma experience with a proven track record of delivering clinical candidates against a range of therapeutic targets including GPCRs, ion channels and enzymes. With extensive in-house expertise in HTS triage, lead generation and lead optimisation, CTx medicinal chemistry has all the necessary skills to identify and optimise lead series to deliver clinical candidates.
Recombinant Protein Production
We have expertise in the production, purification and characterisation of recombinant proteins expressed from bacterial, insect and/or mammalian cell lines in quantities appropriate for high throughput screening and structural studies. All proteins are characterised by mass spectrometry, N-terminal sequencing, thermal denaturation curves and dynamic light scattering to ensure consistent quality. To date, more than 100 proteins have been produced successfully for CTx projects.
The CTx structural biology team draws on 50-plus years of protein crystallography knowledge and has successfully determined the structures of several CTx target proteins and protein/inhibitor complexes. As well as high quality in-house crystallization labs, CTx has access to multiple X-ray facilities (Rigaku MicroMax 007HF with RAXIS4++ area detector and cryocooling) and to the Australian Synchrotron. CTx uses a Linux cluster of 120 processors and associated software for its computational structure-based drug design.
Through the Centre for Drug Candidate Optimisation (CDCO), CTx is highly proficient in physical and preformulation chemistry, pharmacokinetics, drug metabolism and bioanalysis. Profiling of compounds routinely includes analysis of physicochemical properties, permeability, metabolism and metabolite profiling, metabolic drug-drug interactions, in vivo pharmacokinetics, stability testing and impurity profiling. CDCO also provides expertise in preclinical formulation development, solid-state characterisation and salt selection for lead compounds. Since 2003 CDCO has worked on more than 50 collaborative drug discovery programs, and contributed to more than 15 novel candidates moving into clinical development.
Translational Cancer Biology
Our pre-clinical development of proprietary drug candidates is advanced by project-specific relationships with clinicians and scientists from Australia’s leading medical research institutions and hospitals. The CTx translational research group develops, validates and performs target-specific functional bioassays, biomarker assays, in vivo models and imaging strategies for the evaluation of novel compounds From bench to bedside – our expertise in cancer biology, translational research and clinical practice ensures that all our projects will have the best possible chance of transitioning seamlessly from preclinical to clinical development.