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M. Congreve · SciRah

Researcher profile · Semantic Scholar

M. Congreve

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M. Congreve — researcher profile on SciRah

h-index: 41
Works: 189
Citations: 9,649

Most-cited papers

Impact of GPCR Structures on Drug Discovery.
M. Congreve, C. de Graaf, N. Swain, C. G. Tate
2020Cell306 citations Open access
Semantic Scholar
Intracellular allosteric antagonism of the CCR9 receptor
C. Oswald, M. Rappas, J. Kean, A. S. Doré +9 more
2016Nature233 citations
Semantic Scholar
Crystal structure of the GLP-1 receptor bound to a peptide agonist
A. Jazayeri, M. Rappas, Alastair J. H. Brown, J. Kean +13 more
2017Nature177 citations
Semantic Scholar
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
J. Christopher, S. J. Aves, K. Bennett, A. S. Doré +8 more
2015Journal of Medicinal Chemistry159 citations Open access
Semantic Scholar
Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity
A. Borodovsky, Christine M. Barbon, Yanjun Wang, M. Ye +20 more
2020Journal for ImmunoTherapy of Cancer109 citations Open access
Semantic Scholar
Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs.
M. Congreve, C. Oswald, F. Marshall
2017TIPS - Trends in Pharmacological Sciences107 citations
Semantic Scholar
Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.
J. Christopher, Z. Orgován, M. Congreve, A. S. Doré +8 more
2018Journal of Medicinal Chemistry81 citations
Semantic Scholar
From structure to clinic: Design of a muscarinic M1 receptor agonist with the potential to treat Alzheimer’s disease
Alastair J. H. Brown, Sophie J. Bradley, F. Marshall, Giles A. Brown +44 more
2021Cell75 citations Open access
Semantic Scholar
Structure-based drug design for G protein-coupled receptors.
M. Congreve, João M. Dias, F. Marshall
2014Progress in Medicinal Chemistry74 citations
Semantic Scholar
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis
M. Rappas, Ammar A. E. Ali, K. Bennett, Jason Brown +15 more
2019Journal of Medicinal Chemistry71 citations Open access
Semantic Scholar
Accurate Prediction of GPCR Ligand Binding Affinity with Free Energy Perturbation
Francesca Deflorian, L. Pérez-Benito, E. B. Lenselink, M. Congreve +4 more
2020Journal of Chemical Information and Modeling60 citations Open access
Semantic Scholar
Targeting adenosine A2A receptor antagonism for treatment of cancer
M. Congreve, Giles A. Brown, A. Borodovsky, M. Lamb
2018Expert Opinion on Drug Discovery52 citations
Semantic Scholar
Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors.
Rie Suzuki, Giles A. Brown, J. Christopher, Conor C. G. Scully +1 more
2020Journal of Medicinal Chemistry49 citations Open access
Semantic Scholar
Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits
Jon Palacios-Filardo, Matt Udakis, Giles A. Brown, B. Tehan +4 more
2020Nature Communications39 citations Open access
Semantic Scholar
Crystal Structure of Human Soluble Adenylate Cyclase Reveals a Distinct, Highly Flexible Allosteric Bicarbonate Binding Pocket
Susanne M. Saalau-Bethell, V. Berdini, A. Cleasby, M. Congreve +9 more
2014ChemMedChem38 citations Open access
Semantic Scholar
Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol–Bound β1-Adrenergic Receptor
Tomomi Sato, J. Baker, T. Warne, Giles A. Brown +3 more
2015Molecular Pharmacology34 citations Open access
Semantic Scholar
X‐Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists
W. Jespers, G. Verdon, J. Azuaje, Maria Majellaro +12 more
2019Angewandte Chemie32 citations Open access
Semantic Scholar
Structure-based drug design of chromone antagonists of the adenosine A2A receptor
S. P. Andrews, J. Mason, Edward Hurrell, M. Congreve
201421 citations
Semantic Scholar
Abstract 5580: Preclinical pharmacodynamics and antitumor activity of AZD4635, a novel adenosine 2A receptor inhibitor that reverses adenosine mediated T cell suppression
A. Borodovsky, Yanjun Wang, M. Ye, J. Shaw +16 more
201717 citations
Semantic Scholar
Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties
J. Christopher, S. J. Aves, Jason Brown, J. Errey +9 more
201517 citations
Semantic Scholar
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 Pepti
S. J. Bucknell, M. Ator, Alastair J. H. Brown, Jason Brown +12 more
2020Journal of Medicinal Chemistry16 citations Open access
Semantic Scholar
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
C. Bakker, T. Tasker, J. Liptrot, E. Hart +10 more
2021Alzheimer's Research & Therapy14 citations Open access
Semantic Scholar
First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1‐receptor partial agonist for the treatment of dementias
C. Bakker, T. Tasker, J. Liptrot, E. Hart +11 more
2020British Journal of Clinical Pharmacology13 citations Open access
Semantic Scholar
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
P. Nathan, S. B. Millais, A. Godwood, O. Dewit +11 more
2022Alzheimer's & Dementia10 citations Open access
Semantic Scholar
Faculty Opinions recommendation of α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment.
M. Congreve, M. Pickworth
20209 citations
Semantic Scholar
Abstract 3751: Inhibition of A2AR by AZD4635 induces anti-tumor immunity alone and in combination with anti-PD-L1 in preclinical models
A. Borodovsky, Yanjun Wang, M. Ye, J. Shaw +15 more
2018Immunology9 citations
Semantic Scholar
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
Andrew D Cansfield, M. Ator, J. Banerjee, M. Bestwick +22 more
2022ACS Chemical Neuroscience6 citations
Semantic Scholar
Engineering G Protein-Coupled Receptors for Drug Design
M. Congreve, A. S. Doré, A. Jazayeri, Rebecca Nonoo
20155 citations
Semantic Scholar
TEMPORARY REMOVAL: Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design.
A. O'Brien, S. Andrews, Asma Baig, A. Bortolato +19 more
2019Bioorganic & Medicinal Chemistry Letters4 citations
Semantic Scholar
Allosteric binding: structures reveal new ways to tame G protein-coupled receptors.
R. Cooke, M. Congreve
2016Future Medicinal Chemistry4 citations Open access
Semantic Scholar
Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M1‐acetylcholine receptor agonist: A randomized cross‐over trial
C. Bakker, Samantha Prins, J. Liptrot, E. Hart +11 more
2021British Journal of Clinical Pharmacology3 citations Open access
Semantic Scholar
Modeling and Design for Membrane Protein Targets
M. Congreve, A. Bortolato, Giles A. Brown, R. Cooke
20173 citations
Semantic Scholar
Corrigendum: Crystal structure of the GLP-1 receptor bound to a peptide agonist
A. Jazayeri, M. Rappas, Alastair J. H. Brown, J. Kean +13 more
2017Nature3 citations Open access
Semantic Scholar
Perspective in Medicinal Chemistry: Structure-Based Drug Design.
M. Congreve, S. Andrews
2016Current Topics in Medicinal Chemistry3 citations
Semantic Scholar
Author Correction: Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits
Jon Palacios-Filardo, Matt Udakis, Giles A. Brown, B. Tehan +4 more
2021Nature Communications2 citations Open access
Semantic Scholar
Fragment Screening in Complex Systems
M. Congreve, J. Christopher
20162 citations
Semantic Scholar
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
S. Southall, J. Banerjee, Jason Brown, K. Butković +11 more
2022ACS Medicinal Chemistry Letters1 citations Open access
Semantic Scholar
Faculty Opinions recommendation of Palladium-Catalyzed Decarbonylative Difluoromethylation of Acid Chlorides at Room Temperature.
M. Congreve, M. Pickworth
2019Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature1 citations
Semantic Scholar
Advances and Insights from CNS G Protein-Coupled Receptor Crystallography
J. Christopher, M. Congreve, Francesca Deflorian, F. Marshall
20171 citations
Semantic Scholar
Crystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with vercirnon
C. Oswald, M. Rappas, J. Kean, A. S. Doré +9 more
20161 citations
Semantic Scholar
CHAPTER 5:Fragment Screening of G Protein-Coupled Receptors
M. Congreve, R. Cooke
20151 citations
Semantic Scholar
Faculty Opinions recommendation of Strategies to prepare and use functionalized organometallic reagents.
M. Congreve, M. Pickworth
20141 citations
Semantic Scholar
Structure‐Based Drug Design for G Protein‐Coupled Receptors
M. Congreve, J. Christopher, Chris de Graaf
20210 citations
Semantic Scholar
Faculty Opinions recommendation of Discovery of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization.
M. Congreve, M. Pickworth
2021Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature0 citations
Semantic Scholar
Faculty Opinions recommendation of Addressing a Trapped High-Energy Water: Design and Synthesis of Highly Potent Pyrimidoindole-Based Glycogen Synthase Kinase-3β Inhibitors.
M. Congreve, M. Pickworth
2021Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature0 citations
Semantic Scholar
Faculty Opinions recommendation of Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
M. Congreve, M. Pickworth
2021Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature0 citations
Semantic Scholar
Faculty Opinions recommendation of Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H).
M. Congreve, M. Pickworth
2021Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature0 citations
Semantic Scholar
Faculty Opinions recommendation of Discovery of pemigatinib: A potent and selective fibroblast growth factor receptor (FGFR) inhibitor.
M. Congreve, M. Pickworth
2021Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature0 citations
Semantic Scholar
Crystal structure of the Orexin-1 receptor in complex with Compound 14
M. Rappas, A. Ali, K. Bennett, J. Brown +15 more
20200 citations
Semantic Scholar
Supporting Information X-Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists**
W. Jespers, J. Azuaje, Maria Majellaro, M. Congreve +8 more
20200 citations
Semantic Scholar

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