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Browsing publications by Professor Mike Waring.

Newcastle AuthorsTitleYearFull text
Melanie Uguen
Gemma Davison
James Hunter
Dr Mathew Martin
Dr Shannon Turberville
et al.
Build–Couple–Transform: A paradigm for lead-like library synthesis with scaffold diversity2022
Professor Mike Waring
Identification and optimization of a novel series of selective PIP5K inhibitors2022
Harriet Stanway-Gordon
Jessica Graham
Professor Mike Waring
On-DNA Transfer Hydrogenolysis and Hydrogenation for the Synthesis of DNA-Encoded Chemical Libraries2022
Duncan Miller
Tristan Reuillon
Dr Lauren Molyneux
Dr Tim Blackburn
Dr Noel Edwards
et al.
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor2022
Isaline Castan
Professor Mike Waring
Scope of on-DNA nucleophilic aromatic substitution on weakly-activated heterocyclic substrates for the synthesis of DNA-encoded libraries2022
Islam Al-Khawaldeh
Dr Christine Basmadjian
Dr Cinzia Bordoni
Dr Suzannah Harnor
Amy Heptinstall
et al.
An alkynylpyrimidine-based covalent inhibitor that targets a unique cysteine in NF-κB-inducing kinase (NIK)2021
Dr Cinzia Bordoni
Daniel Brough
Gemma Davison
James Hunter
Daniel Lopez Fernandez
et al.
Cardiac Ion Channel Inhibition2021
Edwige Picazo
Amy Heptinstall
Dr Celine Cano
Professor Bernard Golding
Professor Mike Waring
et al.
Cyclisations and fragmentations in the alkylation of 6-chloro-5-hydroxy-4-aminopyrimidines with aminoalkyl chlorides2021
James Hunter
Harriet Stanway-Gordon
Professor Mike Waring
Functional group tolerance of a micellar on-DNA Suzuki-Miyaura cross-coupling reaction for DNA-encoded library design2021
James Hunter
Matt Anderson
Isaline Castan
Jessica Graham
Catherine Salvini
et al.
Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries2021
Professor Mike Waring
Micellar Buchwald-Hartwig coupling of aryl and heteroarylamines for the synthesis of DNA-encoded libraries2021
Melanie Uguen
Professor Mike Waring
Microwave-assisted synthesis of 4-oxo-2-butenoic acids by aldol-condensation of glyoxylic acid2021
Isaline Castan
Jessica Graham
Catherine Salvini
Harriet Stanway-Gordon
Professor Mike Waring
et al.
On the design of lead-like DNA-encoded chemical libraries2021
James Hunter
Professor Mike Waring
The maturation of DNA encoded libraries: opportunities for new users2021
Professor Mike Waring
Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors2020
Gemma Davison
Dr Mathew Martin
Professor Martin Noble
Professor Mike Waring
Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease2020
James Hunter
Dr Lisa Prendergast
Professor Mike Waring
High fidelity Suzuki−Miyaura coupling for the synthesis of DNA encoded libraries enabled by micelle forming surfactants2020
Daniel Wood
Daniel Lopez Fernandez
Leanne Knight
Islam Al-Khawaldeh
Dr Conghao Gai
et al.
FragLites - minimal, halogenated fragments displaying pharmacophore doublets. An efficient approach to druggability assessment and hit generation2019
Professor Mike Waring
Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor2019
Professor Mike Waring
Route to Prolonged Residence Time at the Histamine H1 Receptor: Growing from Desloratadine to Rupatadine2019
Professor Mike Waring
A Genetically Selected Cyclic Peptide Inhibitor of BCL6 Homodimerization2018
Professor Mike Waring
Cancer II2018
Professor Mike Waring
Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC to Provide Insight into Small Molecule Targeting of BCL62018
Professor Mike Waring
Practical application of ligand efficiency metrics in lead optimisation2018
Professor Bernard Golding
Professor Mike Waring
The consequences of ‘Brexit’ for drug discovery and development, and the regulatory implications2018
Professor Mike Waring
Discovery of pyrazolo[1,5-a]pyrimidine B-cell lymphoma 6 (BCL6) binders and optimization to high affinity macrocyclic inhibitors2017
Professor Mike Waring
Structure-activity relationships of the sustained effects of adenosine A2A receptor agonists driven by slow dissociation kinetics2017
Professor Mike Waring
Structure-affinity Relationships and Structure-kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists2017
Professor Mike Waring
Tumour regression and improved gastrointestinal tolerability from controlled release of SN-38 from novel polyoxazoline-modified dendrimers2017
Professor Mike Waring
AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies2016
Professor Mike Waring
Enhanced cytocompatibility and functional group content of poly(L-lysine) dendrimers by grafting with poly(oxazolines)2016
Professor Mike Waring
Optimisation of a series of bivalent triazolopyridazine based bromodomain and extraterminal inhibitors: the discovery of (3R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)2016
Professor Mike Waring
Potent and selective bivalent inhibitors of BET bromodomains2016
Professor Mike Waring
Preparation of triazolopyridazine derivatives for use as antiproliferative agents2016
Professor Mike Waring
A safe and scalable synthesis of 2-hydroxy-3-alkoxypropionates by epoxide ring opening2015
Professor Mike Waring
An analysis of the attrition of drug candidates from four major pharmaceutical companies2015
Professor Mike Waring
Duncan Miller
Challenges in the Medicinal Chemical Optimization of Binding Kinetics2015
Professor Mike Waring
Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR402015
Professor Mike Waring
Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα)2015
Professor Mike Waring
An Improved Method for Difluorocyclopropanation of Alkenes2014
Professor Mike Waring
Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor2014
Professor Mike Waring
Dr James Smith
Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β- inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation.2014
Professor Mike Waring
The challenges of increasing drug discovery productivity2014
Professor Mike Waring
A chemistry Wiki to facilitate and enhance chemical design in drug discovery2013
Professor Mike Waring
Lipophilicity in drug discovery.2010