DMPK is a critical component of a successful drug discovery project, and our medicinal chemists have extensive experience in applying discovery DMPK data to optimise the design of compounds, and ultimately to develop the optimal compound for candidate nomination.
That’s why, as part of our tailored, iterative design-make-test approach, we can work with a number of external DMPK partners.
Our DMPK partners provide capabilities and expertise including:
Physicochemical profiling
In vitro ADME (stability, metabolism, permeability and transporters, protein binding, DDIs…)
In vivo pharmacokinetics and bioanalysis
Metabolite identification
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.
Posters & case studies
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.
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. P. McElroy, P. Jones, N. A. Ignatenko, N. Gunkel and A. K. Miller. View case study.
