Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Jon T. Seal"'
Autor:
Anne-Marie Michon, Rab K. Prinjha, Alex Preston, Laurie J. Gordon, Inmaculada Rioja, Pierre Thesmar, Emmanuel Hubert Demont, James Michael Woolven, Stephen John Atkinson, Jon T. Seal, Cassie Messenger, Lee Andrew Harrison, Paola Grandi, Darren Jason Mitchell, Robert J. Watson, Simon Taylor, Chun-wa Chung, James Gray, Antonia J. Lewis, Ian D. Wall, Dave Lugo, Paul Bamborough
Publikováno v:
ACS Med Chem Lett
[Image: see text] Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a25fcee7700cf48b3d9393a0adacecd2
https://doi.org/10.1021/acsmedchemlett.0c00247
https://doi.org/10.1021/acsmedchemlett.0c00247
Autor:
Jenifer Powles, Neil Upton, Kim Winborn, Nigel Deeks, Christopher N. Johnson, Tania Buck, Mahmood Ahmed, Brenda K. Trail, Darren Jason Mitchell, Mervyn Thompson, Vicky Holland, Laurie J. Gordon, Michael A. Briggs, Jon T. Seal, Stephen Moss, Ashley Garner, David R. Witty, Steven Mark Bromidge, Lorraine Campbell, Andrew D. Medhurst, Tania O. Stean, Geoffrey Stemp, Dieter Hamprecht
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4867-4871
Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::235a4ea32a843eeea24f410f2584c393
https://doi.org/10.1016/j.bmcl.2005.06.107
https://doi.org/10.1016/j.bmcl.2005.06.107
Autor:
Jonathan M. Barford, Victoria J. Bolton, Geoffrey Stemp, Shiyam Mohamed, Stephen Christopher Martin Fell, Christopher N. Johnson, Gareth J. Sanger, David MacPherson, Samantha Louisa Brown, Chermaine Cluff, Darren Jason Mitchell, Sadhia R. Mahmood, Fiona McKay, Beverley Smith, Jon T. Seal, James Myatt, Alison I. Muir, Mervyn Thompson, Kim L. Matthews, Kirk Lawless, Steven J. Stanway, Emma M. Jarvie, Alexander J. Stevens, Susan Marie Westaway
Publikováno v:
Journal of medicinal chemistry. 52(4)
N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8857cec1d323c56eea1c718edc45757b
https://pubmed.ncbi.nlm.nih.gov/19191554
https://pubmed.ncbi.nlm.nih.gov/19191554
Autor:
Andrea Colombo, Izzy Boyfield, Christopher N. Johnson, Alessandra Consonni, Emma M. Jarvie, Victoria J. Bolton, Darren Jason Mitchell, Paolo Celestini, Michael A. Briggs, Sharon C Stratton, James Myatt, Geoffrey Stemp, David MacPherson, Alexander J. Stevens, Jon T. Seal, Stefania Gagliardi, Steven J. Stanway, Macdonald Gregor James, Mauro Riccaboni, Kate Lapsley, Susan Marie Westaway, Silvano Ronzoni, Gareth J. Sanger, Tom D. Heightman, Kim L. Matthews, Samantha Louisa Brown, Mervyn Thompson, Elizabeth Conway
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(24)
Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2cf8a53bdb66c538b47ff91cc8129e4
https://pubmed.ncbi.nlm.nih.gov/19006669
https://pubmed.ncbi.nlm.nih.gov/19006669
Autor:
Stephen J. Medhurst, Sandra Arpino, James Wright, Darren Jason Mitchell, Alexander J. Stevens, James Biggs, Kim Winborn, Susan Marie Westaway, John B. Davis, Jeffrey C. Jerman, Vicky Holland, Tanya Coleman, Jennifer E. Cryan, Geoffrey Stemp, Sarah C. Lappin, Jon T. Seal, Harshad Kantilal Rami, Leontine Saskia Trouw, Mervyn Thompson, Martin J. Gunthorpe
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87b365ea545812a5b73fbe175229b22f
https://pubmed.ncbi.nlm.nih.gov/18809327
https://pubmed.ncbi.nlm.nih.gov/18809327
Autor:
Neil Upton, Vicky Holland, Andrew D. Medhurst, Geoffrey Stemp, Michael A. Briggs, Ashley Garner, Kim Winborn, Mervyn Thompson, Tania Buck, Steven Mark Bromidge, Dieter Hamprecht, Mahmood Ahmed, Stephen Moss, Lorraine Campbell, Nigel Deeks, Tania O. Stean, David R. Witty, Jenifer Powles, Christopher N. Johnson, Brenda K. Trail, Darren Jason Mitchell, Laurie J. Gordon, Jon T. Seal
Publikováno v:
Bioorganic & Medicinal Chemistry.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6e74e53f8e5756eaf7bf0cf9c8b1a3c6
https://doi.org/10.1016/j.bmc.2005.06.017
https://doi.org/10.1016/j.bmc.2005.06.017
Autor:
Susan M. Westaway, Samantha L. Brown, Stephen C. M. Fell, Christopher N. Johnson, David T. MacPherson, Darren J. Mitchell, James W. Myatt, Steven J. Stanway, Jon T. Seal, Geoffrey Stemp, Mervyn Thompson, Kirk Lawless, Fiona McKay, Alison I. Muir, Jonathan M. Barford, Chermaine Cluff, Sadhia R. Mahmood, Kim L. Matthews, Shiyam Mohamed, Beverley Smith
Publikováno v:
Journal of Medicinal Chemistry; Feb2009, Vol. 52 Issue 4, p1180-1189, 10p