Medicinal chemistry expertise available at o2h discovery includes hit identification, hit-to-lead optimisation, lead generation, and lead optimisation. All of these can be accessed as stand-alones or as a part of an integrated drug discovery project.
Hit identification/lead generation projects have involved ligand design for customer-defined targets, synthesis of homologous or diverse series of compounds, design and generation of structurally related compounds, combinatorial synthesis of general as well as focused libraries and search for surrogates of core chemical scaffolds.
Hit-to-lead projects typically involve confirmation of a genuine structure-activity relationship (SAR) and reducing structural/pharmacological liabilities. o2h discovery has the capability to synthesise small focused arrays of compounds in sufficient quantities to allow clients to rapidly screen these compounds for ADME and in vitro biological activity (primary as well as secondary screenings).
For projects advancing to lead optimisation phase, chemists at o2h discovery work intensively with their biology counterparts to produce compounds which closely match the desired target product profile. Typically, this involves a thorough search of prior art and assuring patentability, generation of back-up series and leading the compounds to in vivo proof-of-concept. Our biologists can assist in generating in vivo experimental models recapitulating a particular human pathological condition, designing and efficiently executing PK/PD, toxicology and other relevant pharmacological studies to advance these compounds further.