Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics

por Hothersall, J. Daniel, Guo, Dong, Sarda, Sunil, Sheppard, Robert J., Chen, Hongming, Keur, Wesley, Waring, Michael J., IJzerman, Adriaan P., Hill, Stephen J., Dale, Ian L., Rawlins, Philip B.
Publicado 2017

Structure–Affinity Relationships and Structure–Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists

por Xia, Lizi, de Vries, Henk, Lenselink, Eelke B., Louvel, Julien, Waring, Michael J., Cheng, Leifeng, Pahlén, Sara, Petersson, Maria J., Schell, Peter, Olsson, Roine I., Heitman, Laura H., Sheppard, Robert J., IJzerman, Adriaan P.
Publicado 2017

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor

por Bosma, Reggie, Stoddart, Leigh A., Georgi, Victoria, Bouzo-Lorenzo, Monica, Bushby, Nick, Inkoom, Loretta, Waring, Michael J., Briddon, Stephen J., Vischer, Henry F., Sheppard, Robert J., Fernández-Montalván, Amaury, Hill, Stephen J., Leurs, Rob
Publicado 2019

Route to Prolonged Residence Time at the Histamine H(1) Receptor: Growing from Desloratadine to Rupatadine

por Bosma, Reggie, Wang, Zhiyong, Kooistra, Albert J., Bushby, Nick, Kuhne, Sebastiaan, van den Bor, Jelle, Waring, Michael J., de Graaf, Chris, de Esch, Iwan J., Vischer, Henry F., Sheppard, Robert J., Wijtmans, Maikel, Leurs, Rob
Publicado 2019

Biocatalysis in Drug Design: Engineered Reductive Aminases (RedAms) Are Used to Access Chiral Building Blocks with Multiple Stereocenters

por Casamajo, Arnau Rué, Yu, Yuqi, Schnepel, Christian, Morrill, Charlotte, Barker, Rhys, Levy, Colin W., Finnigan, James, Spelling, Victor, Westerlund, Kristina, Petchey, Mark, Sheppard, Robert J., Lewis, Richard J., Falcioni, Francesco, Hayes, Martin A., Turner, Nicholas J.
Publicado 2023

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

por Bamborough, Paul, Barnett, Heather A., Becher, Isabelle, Bird, Mark J., Chung, Chun-wa, Craggs, Peter D., Demont, Emmanuel H., Diallo, Hawa, Fallon, David J., Gordon, Laurie J., Grandi, Paola, Hobbs, Clare I., Hooper-Greenhill, Edward, Jones, Emma J., Law, Robert P., Le Gall, Armelle, Lugo, David, Michon, Anne-Marie, Mitchell, Darren J., Prinjha, Rab K., Sheppard, Robert J., Watson, Allan J. B., Watson, Robert J.
Publicado 2016

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation

por Lewis, Huw D., Liddle, John, Coote, Jim E., Atkinson, Stephen J., Barker, Michael D., Bax, Benjamin, D., Bicker, Kevin L., Bingham, Ryan P., Campbell, Matthew, Chen, Yu Hua, Chung, Chun-wa, Craggs, Peter D., Davis, Rob P., Eberhard, Dirk, Joberty, Gerard, Lind, Kenneth E., Locke, Kelly, Maller, Claire, Martinod, Kimberly, Patten, Chris, Polyakova, Oxana, Rise, Cecil E., Rüdiger, Martin, Sheppard, Robert J., Slade, Daniel J., Thomas, Pamela, Thorpe, Jim, Yao, Gang, Drewes, Gerard, Wagner, Denisa D., Thompson, Paul R., Prinjha, Rab K., Wilson, David M.
Publicado 2015