Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool

Duncan C. Miller; Tristan Reuillon; Lauren Molyneux; Timothy J. Blackburn; Simon  Cook; Noel Edwards; Jane A. Endicott; Bernard T. Golding; Roger J. Griffin; Ian R. Hardcastle; Amy B. Heptinstall; Pamela Lochhead; Mathew P. Martin; Nick Martin; Stephanie M. Myers; David R. Newell; Richard Noble; Laurent J.M. Rigoreau; Huw Thomas; Julie Ann Tucker; Lan-Zhen Wang; Michael J. Waring; Ai-Ching Wong; Stephen Wedge; Martin Noble; Celine Cano

doi:10.1021/acs.jmedchem.1c01756

Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool

Duncan C. Miller, Tristan Reuillon, Lauren Molyneux, Timothy J. Blackburn, Simon Cook, Noel Edwards, Jane A. Endicott, Bernard T. Golding, Roger J. Griffin, Ian R. Hardcastle, Amy B. Heptinstall, Pamela Lochhead, Mathew P. Martin, Nick Martin, Stephanie M. Myers, David R. Newell, Richard Noble, Laurent J.M. Rigoreau, Huw Thomas, Julie Ann TuckerLan-Zhen Wang, Michael J. Waring, Ai-Ching Wong, Stephen Wedge, Martin Noble, Celine Cano

Biology

Research output: Contribution to journal › Article › peer-review

Original language	English
Pages (from-to)	6513-6540
Number of pages	27
Journal	JOURNAL OF MEDICINAL CHEMISTRY
Volume	65
Issue number	9
Early online date	25 Apr 2022
DOIs	https://doi.org/10.1021/acs.jmedchem.1c01756
Publication status	E-pub ahead of print - 25 Apr 2022

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10.1021/acs.jmedchem.1c01756Licence: CC BY

acs.jmedchem.1c01756
© 2022 The Authors. Published by American Chemical Society
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Cite this

Miller, D. C., Reuillon, T., Molyneux, L., Blackburn, T. J., Cook, S., Edwards, N., Endicott, J. A., Golding, B. T., Griffin, R. J., Hardcastle, I. R., Heptinstall, A. B., Lochhead, P., Martin, M. P., Martin, N., Myers, S. M., Newell, D. R., Noble, R., Rigoreau, L. J. M., Thomas, H., ... Cano, C. (2022). Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool. JOURNAL OF MEDICINAL CHEMISTRY, 65(9), 6513-6540. Advance online publication. https://doi.org/10.1021/acs.jmedchem.1c01756

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title = "Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool",

author = "Miller, {Duncan C.} and Tristan Reuillon and Lauren Molyneux and Blackburn, {Timothy J.} and Simon Cook and Noel Edwards and Endicott, {Jane A.} and Golding, {Bernard T.} and Griffin, {Roger J.} and Hardcastle, {Ian R.} and Heptinstall, {Amy B.} and Pamela Lochhead and Martin, {Mathew P.} and Nick Martin and Myers, {Stephanie M.} and Newell, {David R.} and Richard Noble and Rigoreau, {Laurent J.M.} and Huw Thomas and Tucker, {Julie Ann} and Lan-Zhen Wang and Waring, {Michael J.} and Ai-Ching Wong and Stephen Wedge and Martin Noble and Celine Cano",

note = "{\textcopyright} 2022 The Authors. Published by American Chemical Society ",

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Miller, DC, Reuillon, T, Molyneux, L, Blackburn, TJ, Cook, S, Edwards, N, Endicott, JA, Golding, BT, Griffin, RJ, Hardcastle, IR, Heptinstall, AB, Lochhead, P, Martin, MP, Martin, N, Myers, SM, Newell, DR, Noble, R, Rigoreau, LJM, Thomas, H, Tucker, JA, Wang, L-Z, Waring, MJ, Wong, A-C, Wedge, S, Noble, M & Cano, C 2022, 'Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool', JOURNAL OF MEDICINAL CHEMISTRY, vol. 65, no. 9, pp. 6513-6540. https://doi.org/10.1021/acs.jmedchem.1c01756

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T1 - Parallel Optimisation of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Chemical Tool

AU - Miller, Duncan C.

AU - Reuillon, Tristan

AU - Molyneux, Lauren

AU - Blackburn, Timothy J.

AU - Cook, Simon

AU - Edwards, Noel

AU - Endicott, Jane A.

AU - Golding, Bernard T.

AU - Griffin, Roger J.

AU - Hardcastle, Ian R.

AU - Heptinstall, Amy B.

AU - Lochhead, Pamela

AU - Martin, Mathew P.

AU - Martin, Nick

AU - Myers, Stephanie M.

AU - Newell, David R.

AU - Noble, Richard

AU - Rigoreau, Laurent J.M.

AU - Thomas, Huw

AU - Tucker, Julie Ann

AU - Wang, Lan-Zhen

AU - Waring, Michael J.

AU - Wong, Ai-Ching

AU - Wedge, Stephen

AU - Noble, Martin

AU - Cano, Celine

PY - 2022/4/25

Y1 - 2022/4/25

U2 - 10.1021/acs.jmedchem.1c01756

DO - 10.1021/acs.jmedchem.1c01756

M3 - Article

SN - 0022-2623

VL - 65

SP - 6513

EP - 6540

JO - JOURNAL OF MEDICINAL CHEMISTRY

JF - JOURNAL OF MEDICINAL CHEMISTRY

IS - 9

ER -