Publications by authors named "Sam Hoare"

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Potentiation of GPCR signaling by ATP and sugar monophosphates.
Sam R J Hoare

Trends Pharmacol Sci· October 2025

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Quantifying the Kinetics of Signaling and Arrestin Recruitment by Nervous System G-Protein Coupled Receptors.
Sam R J Hoare, Paul H Tewson, Shivani Sachdev, Mark Connor, Thomas E Hughes

Front Cell Neurosci· January 2022

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The Problems of Applying Classical Pharmacology Analysis to Modern In Vitro Drug Discovery Assays: Slow Binding Kinetics and High Target Concentration.
Sam R J Hoare

SLAS Discov· August 2021

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Pharmacological characterisation of novel adenosine A receptor antagonists.
Kerry Barkan, Panagiotis Lagarias, Margarita Stampelou, Dimitrios Stamatis, Sam Hoare

Sci Rep· November 2020

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Analyzing kinetic signaling data for G-protein-coupled receptors.
Sam R J Hoare, Paul H Tewson, Anne Marie Quinn, Thomas E Hughes, Lloyd J Bridge

Sci Rep· July 2020

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A kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework.
Sam R J Hoare, Paul H Tewson, Anne Marie Quinn, Thomas E Hughes

Sci Rep· February 2020

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The importance of target binding kinetics for measuring target binding affinity in drug discovery: a case study from a CRF receptor antagonist program.
Sam R J Hoare, Beth A Fleck, John P Williams, Dimitri E Grigoriadis

Drug Discov Today· January 2020

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Receptor binding kinetics equations: Derivation using the Laplace transform method.
Sam R J Hoare

J Pharmacol Toxicol Methods· July 2018

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Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites.
Dimitri E Grigoriadis, Evan Smith, Sam R J Hoare, Ajay Madan, Haig Bozigian

J Pharmacol Exp Ther· June 2017

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Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.
Beth A Fleck, Sam R J Hoare, Rebecca R Pick, Margaret J Bradbury, Dimitri E Grigoriadis

J Pharmacol Exp Ther· May 2012

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Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.
John E Tellew, Marion Lanier, Manisha Moorjani, Emily Lin, Zhiyong Luo, Sam R J Hoare

Bioorg Med Chem Lett· December 2010

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Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors.
Siobhan Malany, Lisa M Hernandez, William F Smith, Paul D Crowe, Sam R J Hoare

J Recept Signal Transduct Res· August 2009

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Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation.
Sam R J Hoare, Beth A Fleck, Raymond S Gross, Paul D Crowe, John P Williams

Mol Pharmacol· May 2008

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Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen Chen, Fabio C Tucci, Wanlong Jiang, Joe A Tran, Beth A Fleck, Sam R Hoare

Bioorg Med Chem· May 2008

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Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Chen Chen, Wanlong Jiang, Joe A Tran, Fabio C Tucci, Beth A Fleck, Sam R Hoare

Bioorg Med Chem Lett· January 2008

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Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.
Wanlong Jiang, Joe A Tran, Fabio C Tucci, Beth A Fleck, Sam R Hoare

Bioorg Med Chem Lett· December 2007

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Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Joe A Tran, Wanlong Jiang, Fabio C Tucci, Beth A Fleck, Jenny Wen, Sam R Hoare

J Med Chem· December 2007

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Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Chen Chen, Wanlong Jiang, Fabio Tucci, Joe A Tran, Beth A Fleck, Sam R Hoare

J Med Chem· November 2007

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Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Wanlong Jiang, Fabio C Tucci, Joe A Tran, Beth A Fleck, Jenny Wen, Sam R Hoare

Bioorg Med Chem Lett· October 2007

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Allosteric modulators of class B G-protein-coupled receptors.
Sam R J Hoare

Curr Neuropharmacol· September 2007

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Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Joe A Tran, Fabio C Tucci, Wanlong Jiang, Dragan Marinkovic, Caroline W Chen, Sam R Hoare

Bioorg Med Chem· August 2007

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Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism.
Susan K Sullivan, Sam R J Hoare, Beth A Fleck, Yun-Fei Zhu, Christopher E Heise

Biochem Pharmacol· September 2006

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Single amino acid residue determinants of non-peptide antagonist binding to the corticotropin-releasing factor1 (CRF1) receptor.
Sam R J Hoare, Brock T Brown, Mark A Santos, Siobhan Malany, Stephen F Betz

Biochem Pharmacol· July 2006

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