Not logged in Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode Southall, Stacey M.; Banerjee, Joydeep; Brown, Jason; Butkovic, Kristina; Cansfield, Andrew D.; Cansfield, Julie E.; Congreve, Miles S.; Cseke, Gabriella; Deflorian, Francesca; Hunjadi, Martina Petrovic; Hutinec, Antun; Inturi, Trinadh Kumar; Rupcic, Renata; Saxty, Gordon; Watson, Stephen P. Share Save
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes Cansfield, Andrew D.; Ator, Mark A.; Banerjee, Joydeep; Bestwick, Michael; Bortolato, Andrea; Brown, Giles A.; Brown, Jason; Butkovic, Kristina; Cansfield, Julie E.; Christopher, John A.; Congreve, Miles; Cseke, Gabriella; Deflorian, Francesca; Dugan, Benjamin; Hunjadi, Martina Petrovic; Hutinec, Antun; Inturi, Trinadh Kumar; Landek, Goran; Mason, Jonathan; O'Brien, Alistair; Ott, Gregory R.; Rupcic, Renata; Saxty, Gordon; Southall, Stacey M.; Zadravec, Rahela; Watson, Stephen P. Share Save
A phase 1b/2a multicenter study of the safety and preliminary pharmacodynamic effects of selective muscarinic M1 receptor agonist HTL0018318 in patients with mild-to-moderate Alzheimer's disease Nathan, Pradeep. J. J.; Millais, S. Babli; Godwood, Alex; Dewit, Odile; Cross, David. M. M.; Liptrot, Janet; Ruparelia, Bharat; Jones, Stephen Paul; Bakker, Geor; Maruff, Paul. T. T.; Light, Gregory. A. A.; Brown, Alastair J. H.; Weir, Malcolm Peter; Congreve, Miles; Tasker, Tim Share Save
Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits (Sep, 10.1038/s41467-021-25280-5, 2021) Palacios-Filardo, Jon; Udakis, Matt; Brown, Giles A.; Tehan, Benjamin G.; Congreve, Miles S.; Nathan, Pradeep J.; Brown, Alastair J. H.; Mellor, Jack R. Share Save
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Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M1-acetylcholine receptor agonist: A randomized cross-over trial Bakker, Charlotte; Prins, Samantha; Liptrot, Jan; Hart, Ellen P.; Klaassen, Erica S.; Brown, Giles A.; Brown, Alastair; Congreve, Miles; Weir, Malcolm; Marshall, Fiona H.; Stevens, Jasper; Cross, David M.; Tasker, Tim; Nathan, Pradeep J.; Groeneveld, Geert Jan Share Save
Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study Bakker, Charlotte; Tasker, Tim; Liptrot, Jan; Hart, Ellen P.; Klaassen, Erica S.; Doll, Robert Jan; Brown, Giles A.; Brown, Alastair; Congreve, Miles; Weir, Malcolm; Marshall, Fiona H.; Cross, David M.; Groeneveld, Geert Jan; Nathan, Pradeep J. Share Save
First-in-man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1-receptor partial agonist for the treatment of dementias Bakker, Charlotte; Tasker, Tim; Liptrot, Jan; Hart, Ellen P.; Klaassen, Erica S.; Prins, Samantha; Doef, Thalia F.; Brown, Giles A.; Brown, Alastair; Congreve, Miles; Weir, Malcolm; Marshall, Fiona H.; Cross, David M.; Groeneveld, Geert Jan; Nathan, Pradeep J. Share Save
X-Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists Jespers, Willem; Verdon, Gregory; Azuaje, Jhonny; Majellaro, Maria; Keranen, Henrik; Garcia-Mera, Xerardo; Congreve, Miles; Deflorian, Francesca; de Graaf, Chris; Zhukov, Andrei; Dore, Andrew S.; Mason, Jonathan S.; Aqvist, Johan; Cooke, Robert M.; Sotelo, Eddy; Gutierrez-de-Teran, Hugo Share Save
Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine Bucknell, Sarah J.; Ator, Mark A.; Brown, Alastair J. H.; Brown, Jason; Cansfield, Andrew D.; Cansfield, Julie E.; Christopher, John A.; Congreve, Miles; Cseke, Gabriella; Deflorian, Francesca; Jones, Christopher R.; Mason, Jonathan S.; O'Brien, M. Alistair; Ott, Gregory R.; Pickworth, Mark; Southall, Stacey M. Share Save
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Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis Rappas, Mathieu; Ali, Ammar A. E.; Bennett, Kirstie A.; Brown, Jason D.; Bucknell, Sarah J.; Congreve, Miles; Cooke, Robert M.; Cseke, Gabriella; de Graaf, Chris; Dore, Andrew S.; Errey, James C.; Jazayeri, Ali; Marshall, Fiona H.; Mason, Jonathan S.; Mould, Richard; Patel, Jayesh C.; Tehan, Benjamin G.; Weir, Malcolm; Christopher, John A. Share Save
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Inhibition of A2AR by AZD4635 induces anti-tumor immunity alone and in combination with anti-PD-L1 in preclinical models Borodovsky, Alexandra; Wang, Yanjun; Ye, Minwei; Shaw, Joseph C.; Sachsenmeier, Kris; Deng, Nanhua; Goodwin, Kelly; Clarke, James D.; Goodwin, Richard; Strittmatter, Nicole; Hay, Carl; Sah, Vasu; Deborah, Lawson; Reimer, Corinne; Congreve, Miles; Mason, Jonathan; Marshall, Fiona; Lyne, Paul; Woessner, Richard Share Save
Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGIu5) X-ray Structures Christopher, John A.; Orgovan, Zoltan; Congreve, Miles; Dore, Andrew S.; Errey, James C.; Marshall, Fiona H.; Mason, Jonathan S.; Okrasa, Krzysztof; Rucktooa, Prakash; Serrano-Vega, Maria J.; Ferenczy, Gyorgy G.; Keseru, Gyorgy M. Share Save
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AZD4635 A2A receptor occupancy in cynomolgus monkey using PET and its application to an oncology clinical development program Johnstrom, Peter; Gutierrez, Pablo Morentin; Varnas, Katarina; Schou, Magnus; Takano, Akihiro; Jones, Lorraine; Mugundu, Ganesh; McCoon, Patricia; Lyne, Paul; Infante, Jeffrey; Falchook, Gerald; Patel, Manish; Karlix, Janet; Merchant, Melinda; Clarke, James; Cross, Alan; Seneca, Nicholas; Farde, Lars; Congreve, Miles; Mason, Jon S.; Marshall, Fiona H. Share Save
Preclinical pharmacodynamics and antitumor activity of AZD4635, a novel adenosine 2A receptor inhibitor that reverses adenosine mediated T cell suppression Borodovsky, Alexandra; Wang, Yanjun; Ye, Minwei; Shaw, Joseph C.; Sachsenmeier, Kris F.; Deng, Nanhua; DelSignore, Kelly J.; Fretland, Adrian J.; Clarke, James D.; Goodwin, Richard J.; Strittmatter, Nicole; Hay, Carl; Sah, Vasu R.; Lawson, Deborah; Reimer, Corinne; Congreve, Miles; Mason, Jonathan S.; Marshall, Fiona H.; Lyne, Paul; Woessner, Richard Share Save
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