Capabilities - Lead to Candidate

Sareum optimises multiple compound series through consecutive iterations of synthesis, biochemical assays and ligand-protein structure solution. Our medicinal chemists make use of high quality structural information during lead optimisation to generate novel, potent, selective drug candidates with optimised pharmacokinetic and pharmacodynamic properties that meet the precise biological characteristics required in a drug discovery programme.

lead to candidate

Automated Medicinal Chemistry

We use our industry-leading automated medicinal chemistry platform, in addition to more standard medicinal chemistry techniques, in order to rapidly generate focused chemical libraries which are usually based around several different chemical series. The process is accelerated using members of our in-house template libraries which are biased towards compounds tractable to further chemistry iteration. This approach allows the rapid optimisation of both lead and backup series compounds to match the desired project criteria. The use of modelled or experimentally derived protein structures allows us to identify and fully characterise ligand binding site(s). Using this information, and working closely with our medicinal chemistry team, our computational chemists propose key features required by novel small molecule inhibitors, or key modifications to existing molecules to improve potency, selectivity and/or ADME properties.

Hit to lead to candidate

Compound Biological Profile

Sareum is very experienced in using medicinal chemistry to create compounds that have the desired pharmacological effects in vivo. The chemistry lead optimisation process is coupled closely with key biochemical and biological assays in order to ensure the ideal drug criteria are selected during the chemistry evolution process. Critical to this success is the ability to respond quickly to assay results by having regular chemistry refocusing. This process is greatly enhanced by the use of rapidly generated structural data which can provide key data necessary for pharmacokinetic or target selectivity modification.