Medicinal & Synthetic Chemistry

Hypothesis driven compound design and synthesis

INTRODUCTION

BioAscent’s medicinal chemistry CRO services are provided by our highly talented team of chemists, who have extensive experience of prosecuting successful drug discovery programmes gained within leading pharmaceutical and biotechnology companies. We understand the importance of making the right compound, not any compound, and that delivering a successful molecule with the appropriate biological, ADME and safety profile is set at the design stage.

Working in close partnership with you to understand your approach and project needs we can design and synthesise the optimal ligands for your project at all phases of the discovery process (Hit generation, Hit to Lead, Lead Optimisation). We assess and interpret the information from testing and rapidly incorporate it into the next design cycle thereby ensuring rapid progress. With our wealth of knowledge as drug hunters we can quickly and efficiently take your programme to success.

Our synthetic chemistry capabilities include multi-step synthesis of complex molecules, asymmetric synthesis, route design, building block synthesis, parallel synthesis of ligand arrays and reference molecules.

The synthetic chemistry team is supported by a range of in-house analytical techniques to ensure the quality of the output both for bespoke synthetic chemistry and for the compound library. These include: 400MHz NMR with multi-nuclei probe and variable temperature capability, LCMS analysis including UPLC, supercritical fluid chromatography to provide access to chiral analysis and preparative enantiomer separations.

MEDICINAL CHEMISTRY CASE STUDY

Working in collaboration with partners at the German Cancer Research Center within the European Lead Factory project (ELF), BioAscent scientists helped discover potent and selective inhibitors of enzymes associated with the development of some cancers and neurodegenerative diseases.  This work has been published in ChemMedChem.

“More importantly, the scientists who were involved in the hit development stage, were fully committed to the success of the project, bringing their own ideas and solutions, which made my role as project owner very comfortable. I would be very happy to work with them again.”

Dr Aubry Miller, Cancer Drug Discovery/Wirkstoffforschung Group Leader, German Cancer Research Center (DKFZ)

Target Class Expertise

Our chemistry team have worked on a broad range of target and ligand classes including:

Enzymes

Hydrolases, proteases (including serine, cysteine proteases), kinases (including protein, sugar kinases), phosphodiesterases, ligases, polymerases, helicases, nucleases, demethylases, deacetylases, methyltransferase, decarboxylases, dehydrogenases, oxygenases, reductases

GPCRs
Ion channels

Voltage and ligand-gated

Nuclear receptors
Protein-protein, protein-RNA & protein-DNA interactions
Others

Including splicing factors, chaperones, transporters

Key expertise

Hypothesis driven compound design and synthesis
Design and synthesis of building blocks and intermediates
Synthesis of focused arrays and SAR seeking libraries
Multiparameter optimisation
Project management
Establish strategy for intellectual property protection
Analytical chemistry

Equipment

To support our talented team we have a comprehensive range of equipment, including:

NMR

Bruker Avance III 400 MHz NMR with multinuclear probe and 120-position carousel sample changer

LCMS

Agilent 1200 and 1290 analytical LCMS systems with CTC autosamplers capable of both plate and vial-based sampling

SFC

Waters and Berger analytical/semi-prep SFC systems capable of achiral/chiral method development and separation with automated sample management

HPLC Purification

Waters fully automated semi-prep HPLC systems with diode array detection

Flash Chromatography

Biotage Isolera automated purification systems with either dual wavelength or diode array detection

Evaporation

Genevac centrifuges with plate, vial and tube capability

Microwave Assisted Synthesis

Biotage Initiators with up to 60-sample capacity

Hydrogenation

Thales Nano H-Cube

Flow synthesis

Uniqsis Flowsyn Multi-X with high and low temperature capability

Parallel Synthesis

Extensive array of parallel synthesis equipment

New Technologies

ElectraSyn 2.0, Merck Photoreactor M1

Secure Data Analysis

In an industry standard, secure Dotmatics database

Our Experts

Director of Chemistry

Dr Angus Morrison

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Associate Director of Chemistry

Dr Duncan McArthur

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Chief Scientific Advisor

Dr Phil Jones

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Publications

Posters & case studies

Integrated Drug Discovery


Science-led drug discovery

Get in Touch

Let's talk about how we can maximise your drug discovery success.

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