o2h discovery is a highly reputed service provider of mg/g scale discovery chemistry. We have partnered with a range of well known pharmaceutical and biotechnology companies from Europe, USA and Japan.
The specialised team at o2h discovery has a broad array of experience in preparing small molecule NCEs with the requisite high quality specifications. It is proficient in utilising perse methodologies, including the synthesis of singles, multi-step, small arrays as well as focused libraries. Our scientific team is also experienced in parallel construction of focused libraries for use in hit-to-lead and lead optimisation projects.
The delivery of all our compounds is accompanied with complete characterisation data including, but not limited to, high-field NMR, mass and purity by LC-MS/HPLC/GC.
o2h discovery has experience of a wide range of chemistry including:
- Chiral chemistry
- Aliphatic, aromatic and heterocyclic chemistry
- Carbohydrate chemistry
- Peptide chemistry
- Steroid chemistry
- Nucleoside chemistry
- Combinatorial chemistry
- Natural product chemistry
- Fragment libraries
- Metabolite/impurity/reference synthesis
- Microwave chemistry
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.
Computational chemists at o2h discovery work at providing stand-alone services to our clients with in silico based screening projects as well as supporting medicinal chemistry projects. Computational chemistry expertise includes molecular modelling, virtual screening and drug designing.
Virtual screening services include target identification, in silico drug-likeness, screening of client/commercial databases to identify focused lead/hit compounds and docking studies to prioritise hits for in vitro studies.
Drug designing to support hit generation and lead optimisation are applied to augment medicinal chemistry design efforts and help guide structural modifications to enhance potency, selectivity and drug-like characteristics. Close cooperation between our molecular modellers and medicinal chemists plays a vital role in this process.
Apart from these, we also support designing target-focused libraries, target modelling, molecular dynamic simulations and developing highly predictive 3D-QSAR models based on target and therapeutic areas.
o2h discovery expanded its capability to support several chemical biology projects to deliver bespoke, high quality tools to positively impact target validation and mechanistic understanding.
This includes cutting edge research to prepare key diverse intermediates alongside developing optimised construction methods to prepare these complex molecules in the most efficient manner. The involvement of our analytical group plays an essential role to ensure these tools are isolated in the most appropriate way to meet the required compound specifications and deliver high quality biological data.
Antibody drug conjugate
Bespoke Intermediates for ADCs
Building on our expertise to support small molecules drug discovery programs, we have now extended our service offering to projects in ADC space as outlined below.
Our service offering includes the synthesis, development and scale-up of bespoke Linker, Linker-Reagent, Reagents, Peptide scaffolds, and associated intermediates to meet our collaborator's specifications for their R&D needs.