Understanding Allosteric Modulation and Functional Selectivity at G Protein-Coupled Receptors

Scammells, Peter (Primary Chief Investigator (PCI))
Christopoulos, Arthur (Chief Investigator (CI))

Project: Research

8 Article

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2022

Structural Features of Iperoxo-BQCA Muscarinic Acetylcholine Receptor Hybrid Ligands Determining Subtype Selectivity and Efficacy
Wakeham, M. C. L., Davie, B. J., Chalmers, D. K., Christopoulos, A., Capuano, B., Valant, C. & Scammells, P. J., 5 Jan 2022, In: ACS Chemical Neuroscience. 13, 1, p. 97-111 15 p.
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2021

Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M₁ Muscarinic Acetylcholine Receptor
Jörg, M., Khajehali, E., van der Westhuizen, E. T., C. Choy, K. H., Shackleford, D. M., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., Christopoulos, A. & Scammells, P. J., 8 Jan 2021, In: ChemMedChem. 16, 1, p. 216-233 18 p.
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Open Access

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2018

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M₁ Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles
Dallagnol, J. C. C., Khajehali, E., Van Der Westhuizen, E. T., Jörg, M., Valant, C., Gonçalves, A. G., Capuano, B., Christopoulos, A. & Scammells, P. J., 12 Apr 2018, In: Journal of Medicinal Chemistry. 61, 7, p. 2875-2894 20 p.
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2016

4-phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M₁ muscarinic acetylcholine receptor
Mistry, S. N., Jorg, M., Lim, H., Vinh, N. B., Sexton, P. M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 14 Jan 2016, In: Journal of Medicinal Chemistry. 59, 1, p. 388-409 22 p.
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Novel fused arylpyrimidinone based allosteric modulators of the M₁ muscarinic acetylcholine receptor
Mistry, S. N., Lim, H., Jorg, M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 18 May 2016, In: ACS Chemical Neuroscience. 7, 5, p. 647-661 15 p.
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Prediction of loops in G protein-coupled receptor homology models: effect of imprecise surroundings and constraints
Arora, B., Coudrat, T., Wootten, D., Christopoulos, A., Noronha, S. B. & Sexton, P. M., 25 Apr 2016, In: Journal of Chemical Information and Modeling. 56, 4, p. 671-686 16 p.
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2015

Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand
Mistry, S. N., Shonberg, J., Draper-Joyce, C. J., Klein Herenbrink, C., Michino, M., Shi, L., Christopoulos, A., Capuano, B., Scammells, P. J. & Lane, J. R. D., 2015, In: Journal of Medicinal Chemistry. 58, 17, p. 6819-6843 25 p.
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Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor
Shonberg, J., Draper-Joyce, C. J., Mistry, S. N., Christopoulos, A., Scammells, P. J., Lane, J. R. D. & Capuano, B., 2015, In: Journal of Medicinal Chemistry. 58, 13, p. 5287 - 5307 21 p.
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