Search Results - "Jones, Philip S"

The Joint European Compound Library: boosting precompetitive research by Besnard, Jérémy, Jones, Philip S., Hopkins, Andrew L., Pannifer, Andrew D.

“…•New high-throughput screening collection now available at no cost for academic groups and SMEs.•Compounds contributed by seven European pharma…”
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The Discovery of New Inhibitors of Insulin-Regulated Aminopeptidase by a High-Throughput Screening of 400,000 Drug-like Compounds by Gising, Johan, Honarnejad, Saman, Bras, Maaike, Baillie, Gemma L, McElroy, Stuart P, Jones, Philip S, Morrison, Angus, Beveridge, Julia, Hallberg, Mathias, Larhed, Mats

“…With the ambition to identify novel chemical starting points that can be further optimized into small drug-like inhibitors of insulin-regulated aminopeptidase…”
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Biological and Medicinal Chemistry Sector of The Royal Society of Chemistry: Promoting Chemistry Learning, Networking and Excellence for Baby Boomers through to Gen Alpha by Bagal, Sharan K., Giblin, Gerard M. P., Hall, Adrian, Jones, Philip S.

“…The Biological and Medicinal Chemistry Sector (BMCS) is an important interest group within the UK's Royal Society of Chemistry (RSC). Operating through a…”
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Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors by Brem, Jürgen, Panduwawala, Tharindi, Hansen, Jon Ulf, Hewitt, Joanne, Liepins, Edgars, Donets, Pawel, Espina, Laura, Farley, Alistair J. M., Shubin, Kirill, Campillos, Gonzalo Gomez, Kiuru, Paula, Shishodia, Shifali, Krahn, Daniel, Leśniak, Robert K., Schmidt (Adrian), Juliane, Calvopiña, Karina, Turrientes, María-Carmen, Kavanagh, Madeline E., Lubriks, Dmitrijs, Hinchliffe, Philip, Langley, Gareth W., Aboklaish, Ali F., Eneroth, Anders, Backlund, Maria, Baran, Andrei G., Nielsen, Elisabet I., Speake, Michael, Kuka, Janis, Robinson, John, Grinberga, Solveiga, Robinson, Lindsay, McDonough, Michael A., Rydzik, Anna M., Leissing, Thomas M., Jimenez-Castellanos, Juan Carlos, Avison, Matthew B., Da Silva Pinto, Solange, Pannifer, Andrew D., Martjuga, Marina, Widlake, Emma, Priede, Martins, Hopkins Navratilova, Iva, Gniadkowski, Marek, Belfrage, Anna Karin, Brandt, Peter, Yli-Kauhaluoma, Jari, Bacque, Eric, Page, Malcolm G. P., Björkling, Fredrik, Tyrrell, Jonathan M., Spencer, James, Lang, Pauline A., Baranczewski, Pawel, Cantón, Rafael, McElroy, Stuart P., Jones, Philip S., Baquero, Fernando, Suna, Edgars, Morrison, Angus, Walsh, Timothy R., Schofield, Christopher J.

“…Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization…”
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Cell-active small molecule inhibitors validate the SNM1A DNA repair nuclease as a cancer target by Bielinski, Marcin, Henderson, Lucy R, Yosaatmadja, Yuliana, Swift, Lonnie P, Baddock, Hannah T, Bowen, Matthew J, Brem, Jürgen, Jones, Philip S, McElroy, Stuart P, Morrison, Angus, Speake, Michael, van Boeckel, Stan, van Doornmalen, Els, van Groningen, Jan, van den Hurk, Helma, Gileadi, Opher, Newman, Joseph A, McHugh, Peter J, Schofield, Christopher J

“…The three human SNM1 metallo-β-lactamase fold nucleases (SNM1A-C) play key roles in DNA damage repair and in maintaining telomere integrity. Genetic studies…”
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The SULSA Assay Development Fund: accelerating translation of new biology from academia to pharma by McElroy, Stuart P., Jones, Philip S., Barrault, Denise V.

“…•Translating academic science with drug discovery requires high quality assays.•We established a fund and utilised existing infrastructure to address this…”
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The ELF Honest Data Broker: informatics enabling public–private collaboration in a precompetitive arena by Paillard, Guillaume, Cochrane, Philip, Jones, Philip S., van Hoorn, Willem P., Caracoti, Andrei, van Vlijmen, Herman, Pannifer, Andrew D.

“…•A novel HTS triage and management application to enable a large precompetitive hit discovery consortium.•Scientific functionality and IP safeguards for…”
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IMI European Lead Factory — democratizing access to high-throughput screening by Jones, Philip S., Boucharens, Sylviane, McElroy, Stuart P., Morrison, Angus, Honarnejad, Saman, van Boeckel, Stan, van den Hurk, Helma, Basting, Daniel, Hüser, Jörg, Jaroch, Stefan, Ottow, Eckhard, Benningshof, Jorg, Folmer, Rutger H. A., Leemhuis, Frank, Kramer-Verhulst, Patricia M., Nies, Vera J. M., Orrling, Kristina M., Rijnders, Ton, Pfander, Claudia, Engkvist, Ola, Pairaudeau, Garry, Simpson, Peter B., Ortholand, Jean-Yves, Roche, Didier, Dömling, Alexander, Kühnert, Sven M., Roevens, Peter W. M., van Vlijmen, Herman, van Wanrooij, Eva J. A., Verbruggen, Christophe, Nussbaumer, Peter, Ovaa, Huib, van der Stelt, Mario, Simonsen, Klaus Baek, Tagmose, Lena, Waldmann, Herbert, Duffy, James, Finsinger, Dirk, Jurzak, Mirek, Burgess-Brown, Nicola A., Lee, Wen H., Rutjes, Floris P. J. T., Haag, Hubert, Kallus, Christopher, Mors, Hartmut, Dorval, Thierry, Lesur, Brigitte, Ramon Olayo, Fernando, Hamza, Daniel, Jones, Geraint, Pearce, Christopher, Piechot, Alexander, Tzalis, Dimitrios, Clausen, Mads H., Davis, Jeremy, Derouane, Daphné, Vermeiren, Céline, Kaiser, Markus, Stockman, Robert A., Barrault, Denise V., Pannifer, Andrew D., Swedlow, Jason R., Nelson, Adam S., Orru, Romano V. A., Ruijter, Eelco, van Helden, Steven P., Li, Volkhart M., Vries, Ton, de Vlieger, Jon S. B.

“…The European Lead Factory combines assets and experience from major pharma with innovation and agility of academia and SMEs in a collaborative platform to…”
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The enantiospecific synthesis of (+)-monomorine I using a 5-endo-trig cyclisation strategy by Berry, Malcolm B, Craig, Donald, Jones, Philip S, Rowlands, Gareth J

“…We have developed a general strategy for the synthesis of 2,5-syn disubstituted pyrrolidines that is based on the multi-faceted reactivity of the sulfone…”
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In Vitro Assay Development and HTS of Small-Molecule Human ABAD/17β-HSD10 Inhibitors as Therapeutics in Alzheimer's Disease by Aitken, Laura, Baillie, Gemma, Pannifer, Andrew, Morrison, Angus, Jones, Philip S, Smith, Terry K, McElroy, Stuart P, Gunn-Moore, Frank J

“…A major hallmark of Alzheimer's disease (AD) is the formation of neurotoxic aggregates composed of the amyloid-β peptide (Aβ). Aβ has been recognized to…”
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Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors by Cai, Jiaqiang, Robinson, John, Belshaw, Simone, Everett, Kathryn, Fradera, Xavier, van Zeeland, Mario, van Berkom, Leon, van Rijnsbergen, Peter, Popplestone, Lucy, Baugh, Mark, Dempster, Maureen, Bruin, John, Hamilton, William, Kinghorn, Emma, Westwood, Paul, Kerr, Jennifer, Rankovic, Zoran, Arbuckle, Wullie, Bennett, D. Jonathan, Jones, Philip S., Long, Clive, Martin, Iain, Uitdehaag, Joost C.M., Meulemans, Tommi

“…By using a small atom (Cl, F, or Me) to increase the torsion angle between the phenyl ring and the attached secondary amide, trifluoromethylphenyl motif was…”
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Structure–activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties by Palin, Ronald, Clark, John K., Evans, Louise, Houghton, Andrea K., Jones, Philip S., Prosser, Alan, Wishart, Grant, Yoshiizumi, Kazuya

“…The N-3 position of a series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues was optimised using the predictive power of a CoMFA model. The model…”
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1H-Imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: Separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pkₐ by Arbuckle, Wullie, Baugh, Mark, Belshaw, Simone, Bennett, D. Jonathan, Bruin, John, Cai, Jiaqiang, Cameron, Kenneth S, Claxton, Chris, Dempster, Maureen, Everett, Kathryn, Fradera, Xavier, Hamilton, William, Jones, Philip S, Kinghorn, Emma, Long, Clive, Martin, Iain, Robinson, John, Westwood, Paul

“…Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pkₐ of basic nitrogen containing cathepsin S inhibitors, a set of…”
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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors by Cai, Jiaqiang, Baugh, Mark, Black, Darcey, Long, Clive, Jonathan Bennett, D., Dempster, Maureen, Fradera, Xavier, Gillespie, Jonathan, Andrews, Fiona, Boucharens, Sylviane, Bruin, John, Cameron, Kenneth S., Cumming, Iain, Hamilton, William, Jones, Philip S., Kaptein, Allard, Kinghorn, Emma, Maidment, Maurice, Martin, Iain, Mitchell, Ann, Rankovic, Zoran, Robinson, John, Scullion, Paul, Uitdehaag, Joost C.M., Vink, Paul, Westwood, Paul, van Zeeland, Mario, van Berkom, Leon, Bastiani, Martijn, Meulemans, Tommi

“…6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives were identified as selective human cathepsin S inhibitors with a stable thiol trapping nitrile…”
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The Hypnotic, Electroencephalographic, and Antinociceptive Properties of Nonpeptide ORL1 Receptor Agonists After Intravenous Injection in Rodents by Byford, Alan J., Anderson, Alison, Jones, Philip S., Palin, Ronald, Houghton, Andrea K.

“…Agonists at the opioid receptor-like receptor 1 (ORL1) induce motor impairment, sedation, and loss of righting reflex (LRR) in rodents. This receptor may…”
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Cardiorenal outcomes, kidney function, and other safety outcomes with ertugliflozin in older adults with type 2 diabetes (VERTIS CV): secondary analyses from a randomised, double-blind trial by Pratley, Richard E, Cannon, Christopher P, Cherney, David Z I, Cosentino, Francesco, McGuire, Darren K, Essex, Margaret Noyes, Lawrence, David, Jones, Philip L S, Liu, Jie, Adamsons, Ingrid, Dagogo-Jack, Samuel

“…VERTIS CV was a randomised, double-blind, placebo-controlled, parallel-group, multicentre cardiovascular outcomes trial that evaluated the cardiovascular…”
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Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties by Palin, Ronald, Bom, Anton, Clark, John K., Evans, Louise, Feilden, Helen, Houghton, Andrea K., Jones, Philip S., Montgomery, Brian, Weston, Mark A., Wishart, Grant

“…A series of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues were prepared and evaluated as NOP agonists. The selective NOP agonist (+)-…”
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Discovery of novel low molecular weight inhibitors of IMPDH via virtual needle screening by Pickett, Stephen D, Sherborne, Bradley S, Wilkinson, Trevor, Bennett, James, Borkakoti, Neera, Broadhurst, Michael, Hurst, David, Kilford, Ian, McKinnell, Murray, Jones, Philip S

“…Novel, low molecular weight inhibitors of IMPDH have been discovered through the application of a validated virtual screening protocol. A series of 21 IMPDH…”
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Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity by Guertin, Kevin R., Setti, Lina, Qi, Lida, Dunsdon, Rachel M., Dymock, Brian W., Jones, Philip S., Overton, Hilary, Taylor, Mathew, Williams, Glyn, Sergi, Joseph A., Wang, Karen, Peng, Ying, Renzetti, Marcia, Boyce, Rogely, Falcioni, Fiorenza, Garippa, Ralph, Olivier, Andrée R.

“…A novel series of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents have been identified. These compounds show non-selective…”
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Rapid access towards follow-up NOP receptor agonists using a knowledge based approach by Palin, Ronald, Clark, John K., Evans, Louise, Feilden, Helen, Fletcher, Dan, Hamilton, Niall M., Houghton, Andrea K., Jones, Philip S., McArthur, Duncan, Montgomery, Brian, Ratcliffe, Paul D., Smith, Alasdair R.C., Sutherland, Aaron, Weston, Mark A., Wishart, Grant

“…A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one…”
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