Capabilities and services

Fragment Screening

Multiple screening formats are available including ligand-detect NMR and SPR. Fluorine NMR is available as an additional detection method. HSQC NMR can be used to validate hits and identify binding sites. Crystallography services are available to initiate a structure-based drug design program using the Australian Synchrotron at Monash.

Assay Development

Screening cascades are tailored for each target. We work with you to determine which primary and secondary screens best suit your target, considering such factors as protein size, stability and production yields and the availability of natural substrates or inhibitors. SPR assay development can be provided as an independent service or to establish conditions prior to fragment screening. MFP can assist with protein production, including isotope labelling for protein-detect NMR. Selective labelling strategies can be designed for protein-detect NMR of large proteins.

Hit optimisation

We offer structure-activity relationships (SAR) by catalogue compound sourcing. And our library is designed such that all compounds in our screening sets have at least 10 analogues available for immediate purchase. This enables us to establish SAR in a rapid and cost-effective manner prior to commencing a chemistry program.

Lead Development

MFP is located within the Monash Institute of Pharmaceutical Sciences, which provides ready access to medicinal chemistry expertise to elaborate fragment hits into higher affinity lead compounds. MFP uses our highly efficient REFiL strategy, enabling the rapid exploration of chemical space without the need for a large chemistry program. By combining the efficiency of parallel chemical synthesis with off-rate screening by SPR we can rapidly synthesize libraries of fragment analogues in plate-format to explore SAR along an expansion vector to identify new binding interactions.

DNA-encoded Libary (DEL) Screening

DNA- encoded library (DEL) screens involve screening millions to billions of compounds that have a DNA tag (barcode) attached. These libraries are built-up by sequential synthetic steps with the addition of a unique piece of DNA for each individual reaction. This enables it to identify every compound within these very large chemical libraries The DEL technology has come to fruition through advances in DNA-compatible reactions, selection methodologies, next-generation sequencing and bioinformatic data analysis. The MFP offers DEL screening as an alternative, cost-effective and efficient method to screen extremely large chemical library sets.

X-Ray Crystallography

We offer a range of X-ray crystallography services to support your fragment or small molecule drug discovery program. These services include: soaking and co-crystallisation development; collection, processing and analysis of X-ray data. The information obtained gives a 3-dimensional picture of how and where a ligand binds with a protein target, which guides the next steps in structure-based drug design.

Custom Surface Plasmon Resonance (SPR)

The MFP has a suite of Biacore SPR instruments (2 × T200 and 1 × S200) and extensive expertise in surface chemistry, assay development and SPR data analysis. The MFP staff will work with clients to develop SPR assays to characterise binding affinity and kinetics of interactions. SPR is a very versatile tool that enables detailed characterisation of interactions across a range of different binding partners including antibody-antigen; protein-protein; small-molecules and peptides with proteins and DNA/RNA targets.

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Commercial clients
Academic clients

Funding Opportunities for FBDD

Therapeutic Innovation Australia
The MFP is a TIA-supported facility. We do assist researchers in preparing funding applications for the TIA’s Pipeline Accelerator scheme.

Innovation Connections
The Australian Government’s Innovation Connections grant scheme is open to commercial partners.

Monash Fragment Platform