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. 

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.

• KLK6: Synthesis and structure-activity relationship of N-(4-benzamidino)-oxazolidinones-potent and selective inhibitors of kallikrein-related peptidase 6. View case study, view paper.

“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

Key expertise

Our Experts

Publications

• Cell-active small molecule inhibitors validate the SNM1A DNA repair nuclease as a cancer target. M. Bielinski, L. R. Henderson, Y. Yosaatmadja, L. P. Swift, H. T. Baddock, M. J. Bowen, J. Brem, P. S. Jones, S. P. McElroy, A. Morrison, M. Speake, S. van Boeckel, E. van Doornmalen, J. van Groningen, H. van den Hurk, O. Gileadi, J. A. Newman, P. J. McHugh,  C. J. Schofield. View paper.

• Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists. A. Mahindra, L. Jenkins, S. Marsango, M. Huggett, M. Huggett, L. Robinson, J. Gillespie, M. Rajamanickam, A. Morrison, S. McElroy, I. G. Tikhonova, G. Milligan, A. G. Jamieson. View paper.

• The identification and characterisation of autophagy inhibitors from the published kinase inhibitor sets. M Zachari, J. Rainard, G. Pandarakalam, L. Robinson, J. Gillespie, M. Rajamanickam, V. Hamon, A. Morrison, I. Ganley, S. McElroy. View paper.

• Identification of a novel class of benzofuran oxoacetic acid-derived ligands that selectively activate cellular EPAC; Cells; 8(11); 1425; 2019. E. Beck, E. Parnell, A. Cowley, A. Porter J. Gillespie, J. Robinson, L. Robinson, A. Pannifer, V. Hamon, P. Jones, A. Morrison, S. McElroy, M. Timmerman, H. Rutjes, P. Mahajan, J. Wiejak, U. Luchowska-Stańska, D. Morgan, G. Barker, H. Rehmann and S. Yarwood. View paper.

• Synthesis and structure–activity relationships of N-(4-benzamidino)-oxazolidinones–potent and selective inhibitors of kallikrein-related peptidase 6; chemRxiv DOI: 10.26434/chemrxiv.9788276, 2019. E. De Vita, N. Smits, H. van den Hurk, E. Beck, J. Hewitt, G. Baillie, E. Russell, A. Pannifer, V. Hamon, A.Morrison, S. McElroy, P. Jones, N. Ignatenko, N. Gunkel and A. Miller. View paper. 

• Abstract LB-B17: Characterization of small molecule inhibitors of the Nrf2-Keap1 interaction using MicroScale Thermophoresis. Molecular Cancer Therapeutics 17 (1 Supplement), LB-B17-LB-B1. J. Rainard, A. Morrison, A. Pannifer, P. Jones, R. Mead, S. McElroy. View paper. 

• Comprehensive Medicinal Chemistry III, Chapter 1.18, 505-519; Eds. S. Chackalamannil, D. Rotella, S. Ward; Oxford: Elsevier; 2017. European Lead Factory; F. Giordanetto, P. Jones, A. Nelson, J. Benningshof, G. Muller, A. Pannifer, S. van Boeckel and D. Tzalis. View paper.

• The importance of triaging in determining the quality of output from high-throughput screening. Future Medicinal Chemistry, 2015, Vol. 7, No. 14, Pages 1847-1852. P. Jones, S. McElroy, A. Morrison, A. Pannifer. View paper. 

• The Joint European Compound Library: boosting precompetitive research. Drug Discovery Today; 20, 181, 2015. J. Besnard, P. Jones, A. Hopkins and A. Pannifer. View paper.

Posters & case studies

• Lead generation: discovery of novel KLK6 Inhibitors as novel anti-cancer drugs. E. De Vita, N. Smits, H. van den Hurk, E. M. Beck, J. Hewitt, G. Baillie, E. Russell, A. Pannifer, V. Hamon, A. Morrison, S. McElroy, P. Jones, N. Ignatenko, N. Gunkel, A. K. Miller. View case study.

• Using a library of Pan-Assay Interference (PAINS) small molecules to understand and improve HTS outcomes. G. Baillie, A. Morrison, A. Pannifer, S. McElroy. Download PDF.

• Characterization of small molecule inhibitors of the Nrf2-Keap1 interaction using MicroScale Thermophoresis. J. Rainard, M. Matheson, J. Gemmell, A. Morrison, A. Pannifer, P. Jones, R. Mead, S. McElroy. Download PDF.

• The European Lead Factory: A Collaborative Approach to Drug Discovery. ESC Chemistry: F. MacLeod, A. Morrison, E. Beck, P. Jones, J. Hewitt, M. Matheson, J. Schulz, J. Robinson, L. Robinson, J. Gillespie, M. Huggett, M. Rajamanickam; ESC CMC: A. Pannifer, V. Hamon; ESC Biology: S. McElroy, M. Speake, G. Baillie, E. Russell, J. Rainard, A. Porter, G. Pandarakalam, N. Clark, D. Tegazzini. PPSC: H. Rutjes, C.A.A. van Boeckel, N. Smits, E. van Doornmalen, T. W. Lam, M. Bras, C. S. Schofield; J. J. Brem; M. A. McDonough, M. Van der Stelt, F. J. Janssen, P.P. Geurink, H. Ovaa, H. S. Overkleeft, A. C. M. van Esbroeck, M. P. Baggelaar, H. den Dulk. Download PDF.