Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor

Author:

Miller Duncan C.1ORCID,Reuillon Tristan1,Molyneux Lauren1,Blackburn Timothy1,Cook Simon J.2,Edwards Noel3,Endicott Jane A.3,Golding Bernard T.1ORCID,Griffin Roger J.1,Hardcastle Ian1,Harnor Suzannah J.1ORCID,Heptinstall Amy1,Lochhead Pamela2,Martin Mathew P.3,Martin Nick C.1,Myers Stephanie1,Newell David R.3,Noble Richard A.3,Phillips Nicole3,Rigoreau Laurent4,Thomas Huw3,Tucker Julie A.3,Wang Lan-Zhen3,Waring Michael J.1ORCID,Wong Ai-Ching5,Wedge Stephen R.3,Noble Martin E. M.3,Cano Celine1ORCID

Affiliation:

1. Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K.

2. Signalling Laboratory, The Babraham Institute, Babraham Research Campus, Cambridge CB22 3AT, U.K.

3. Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O’Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K.

4. Cancer Research UK Therapeutic Discovery Laboratories, Jonas Webb Building, Babraham Campus, Babraham, Cambridgeshire CB22 3AT, U.K.

5. Cancer Research UK Therapeutic Discovery Laboratories, London Bioscience Innovation Centre, 2 Royal College Street, London NW1 0NH, U.K.

Funder

Astex Pharmaceuticals

Medical Research Council

Cancer Research UK

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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