Publications by authors named "Martin J. Packer"

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AZ14289671 is a highly selective and blood-brain barrier penetrant irreversible TKI that targets EGFRExon20 insertions.
Aisha M Swaih, Sara Talbot, Adriana Savoca, Hannah Thorpe, Vikki Flemington, Martin J Packer

Cell Rep Med· September 2025

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Highly Optimized CNS Penetrant Inhibitors of EGFR Exon20 Insertion Mutations.
William McCoull, Clare Thomson, Erin Braybrooke, Christina Chan, Nicola Colclough, Martin J Packer

J Med Chem· February 2025

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Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}--methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
Jeffrey W Johannes, Amber Y S Balazs, Derek Barratt, Michal Bista, Matthew D Chuba, Martin J Packer

J Med Chem· December 2024

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Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Clare Thomson, Erin Braybrooke, Nicola Colclough, Nichola L Davies, Nicolas Floc'h, Martin J Packer

J Med Chem· September 2024

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Characterisation of high throughput screening outputs for small molecule degrader discovery.
Lillie E Bell, Catherine Bardelle, Martin J Packer, Johanna Kastl, Geoffrey A Holdgate

SLAS Discov· July 2024

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Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer.
Sharan K Bagal, Peter C Astles, Coura Diène, Argyrides Argyrou, Claire Crafter, Martin J Packer

J Med Chem· July 2024

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Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Clare Thomson, Peter Barton, Erin Braybrooke, Nicola Colclough, Zhiqiang Dong, Martin J Packer

J Med Chem· June 2024

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Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice.
Daniel H O' Donovan, David Baker, Giovanni Ciotta, Sébastien L Degorce, Sylvain Demanze, Martin J Packer

Bioorg Med Chem Lett· November 2023

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Bifocal stance theory, the transmission metaphor, and institutional reality.
Martin J Packer, Michael Cole

Behav Brain Sci· November 2022

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Grouping concentration response curves by features of their shape to aid rapid and consistent analysis of large data sets in high throughput screens.
Gareth Davies, John Vincent, Martin J Packer, David Murray

SLAS Discov· June 2022

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NMR Molecular Replacement Provides New Insights into Binding Modes to Bromodomains of BRD4 and TRIM24.
Felix Torres, Reto Walser, Janina Kaderli, Emanuele Rossi, Romel Bobby, Martin J Packer

J Med Chem· April 2022

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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}--methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Jeffrey W Johannes, Amber Balazs, Derek Barratt, Michal Bista, Matthew D Chuba, Martin J Packer

J Med Chem· October 2021

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Nuclear magnetic resonance free ligand conformations and atomic resolution dynamics.
Amber Y S Balazs, Nichola L Davies, David Longmire, Martin J Packer, Elisabetta Chiarparin

Magn Reson (Gott)· June 2021

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Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
Daniel H O' Donovan, Clare Gregson, Martin J Packer, Ryan Greenwood, Kurt G Pike

Bioorg Med Chem Lett· May 2021

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Correction to "Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles".
Amber Y S Balazs, Rodrigo J Carbajo, Nichola L Davies, Yu Dong, Alexander W Hird, Martin J Packer

J Med Chem· March 2021

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Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors.
Erica Banks, Michael Grondine, Deepa Bhavsar, Evan Barry, Jason G Kettle, Martin J Packer

Sci Transl Med· April 2020

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Utilizing Grand Canonical Monte Carlo Methods in Drug Discovery.
Michael S Bodnarchuk, Martin J Packer, Alexe Haywood

ACS Med Chem Lett· January 2020

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IMPRESSION - prediction of NMR parameters for 3-dimensional chemical structures using machine learning with near quantum chemical accuracy.
Will Gerrard, Lars A Bratholm, Martin J Packer, Adrian J Mulholland, David R Glowacki

Chem Sci· January 2020

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Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles.
Amber Y S Balazs, Rodrigo J Carbajo, Nichola L Davies, Yu Dong, Alexander W Hird, Martin J Packer

J Med Chem· November 2019

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PELE-MSM: A Monte Carlo Based Protocol for the Estimation of Absolute Binding Free Energies.
Joan F Gilabert, Christoph Grebner, Daniel Soler, Daniel Lecina, Martí Municoy, Martin J Packer

J Chem Theory Comput· November 2019

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Alignment-Free Molecular Shape Comparison Using Spectral Geometry: The Framework.
Matthew P Seddon, David A Cosgrove, Martin J Packer, Valerie J Gillet

J Chem Inf Model· January 2019

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Experimental free ligand conformations: a missing link in structure-based drug discovery.
Elisabetta Chiarparin, Martin J Packer, David M Wilson

Future Med Chem· January 2019

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Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
Adriana E Tron, Matthew A Belmonte, Ammar Adam, Brian M Aquila, Lawrence H Boise, Martin J Packer

Nat Commun· December 2018

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Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Jason G Kettle, Rana Anjum, Evan Barry, Deepa Bhavsar, Crystal Brown, Martin J Packer

J Med Chem· October 2018

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Correction to "Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors".
Jeffrey W Johannes, Stephanie Bates, Carl Beigie, Matthew A Belmonte, John Breen, Martin J Packer

ACS Med Chem Lett· November 2017

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