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pro vyhledávání: '"Stephen L. Garland"'
Autor:
Stephen L. Garland
Publikováno v:
Future Medicinal Chemistry. 6:729-732
Autor:
David M. Andrews, Richard Kidd, Paul J. Edwards, Stephen L. Garland, David N. A. Fox, Timothy Gallagher, Laura M. Broad, Joseph B. Sweeney
Publikováno v:
Andrews, D, Broad, L M, Edwards, P, Fox, D, Gallagher, T, Garland, S, Kidd, R & Sweeney, J 2016, ' The creation and characterisation of a National Compound Collection : the Royal Society of Chemistry pilot ', Chemical Science, vol. 7, no. 6, pp. 3869-3878 . https://doi.org/10.1039/C6SC00264A
Chemical Science
Chemical Science
We report the extraction of compound data from historical literature, making it chemically searchable. Evaluation by drug discovery groups reveals the utility of this approach.
We present a summary of the National Compound Collection (NCC) pilot
We present a summary of the National Compound Collection (NCC) pilot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d7674c4943bd870faaca550bf86a35a
https://research-information.bris.ac.uk/en/publications/dea9b0b3-6d2c-4a09-8df6-741d443a7fe4
https://research-information.bris.ac.uk/en/publications/dea9b0b3-6d2c-4a09-8df6-741d443a7fe4
Autor:
Frank E. Blaney, Stephen L. Garland
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery
G-protein-coupled receptors (GPCRs) are a very important class of proteins for drug discovery. Exciting progress has been made recently in the determination of X-ray crystal structures. However, despite this, structural coverage of the receptor famil
Autor:
Stephen L. Garland, Magalie Rocheville
Publikováno v:
Drug Discovery Today: Technologies. 7:e87-e94
Positive allosteric modulation is an innovative strategy for the discovery of drugs acting at 7-transmembrane receptors. Screening has led to the identification of numerous starting points for medicinal chemistry typified by novel mechanisms of actio
Autor:
David R. Witty, Jonathan Brand, Ho Y. Li, Paul Goldsmith, Michael Stott, Robert W. Ward, Jennifer Farge, Fiona Nimmo, Nicola Shuker, Sanjeet Singh Sehmi, Mathilde D’Angeli, Ian R. Kilford, Rio Hutchings, Jennifer Sweeting, Andrew K. Takle, John Skidmore, Hasmi Tajuddin, Michael A. Briggs, Giancarlo Trani, David Matthew Wilson, Francis Dominic Sanderson, Paula L. Nichols, David MacPherson, Stephen L. Garland, Ian D. Wall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1368-1372
A pharmacophore model was built, based on known CGRP receptor antagonists, and this was used to aid the identification of novel leads. Analogues were designed, modelled and synthesised which incorporated alternative 'LHS' fragments linked via either
Autor:
Stephen P. Watson, Adelheid Roth, Anna Sava, Greg J. Osborne, David John Nash, Paloma Perez, Ben Powney, Corrado Corti, Magalie Rocheville, Paul W. Smith, Clive Leslie Branch, Federica Bianchi, Pier D’Alessandro, Emma Koppe, Maite de los Frailes, Jesús Ángel de la Fuente, Annarosa Ugolini, Dino Montanari, Stephen L. Garland
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:759-762
The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure-activity relationships, attenuation of dopamine
Publikováno v:
Journal of Medicinal Chemistry. 52:4429-4442
Recent advances in structural biology for G-protein-coupled receptors (GPCRs) have provided new opportunities to improve the definition of the transmembrane binding pocket. Here a reference set of 44 residue positions accessible for ligand binding wa
Autor:
Alison I. Muir, William J. Coates, Adrian Hall, Stephen L. Garland, Neville Hubert Nicholson, Graham D Smith, Mark Wigglesworth, Shahzad Sharooq Rahman, Philip G. Szekeres, Berthold Wroblowski, Jag Paul Heer
Publikováno v:
Journal of Medicinal Chemistry. 52:818-825
The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small molecule agonist and initial dock
Autor:
James T. Townsend, Alessandra Gaiba, David Kendall Jung, Christopher A. Parr, John D. Harling, David Matthew Wilson, Mark James Bamford, Stephen L. Garland, Susannah Davies, Nicholas Bailey, Jason Witherington, Michael J. Alberti, Andrew K. Takle, David Kenneth Dean, Jon Graham Anthony Steadman, Terence A. Panchal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3402-3406
A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3-ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
Autor:
Stephen L, Garland
Publikováno v:
Future medicinal chemistry. 6(7)