Christopher Daley
Merck & Co.
5 Papers
70 Citations
Christopher Daley is an academic researcher from Merck & Co.. The author has contributed to research in topics: Medicine & Ligand efficiency. The author has an hindex of 3, co-authored 5 publications.
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Papers
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice
Anthony J. Roecker,Melissa Egbertson,Kristen L.G. Jones,Robert Gomez,Richard L. Kraus,Yuxing Li,Amy Jo Koser,Mark O. Urban,Rebecca M. Klein,Michelle K. Clements,Jacqueline Panigel,Christopher Daley,Jixin Wang,Eleftheria N. Finger,John Majercak,Vincent P. Santarelli,Irene Gregan,Matthew J. Cato,Tracey Filzen,Aneta Jovanovska,Ying-Hong Wang,Deping Wang,Leo A. Joyce,Edward C. Sherer,Xuanjia Peng,Xiu Wang,Haiyan Sun,Paul J. Coleman,Andrea K. Houghton,Mark E. Layton +29 more
TL;DR: A novel series of orally bioavailable arylsulfonamideNav1.7 inhibitors with high levels of selectivity over Nav1.5, the Nav isoform responsible for cardiovascular side effects, are discovered through judicious use of parallel medicinal chemistry and physicochemical property optimization.
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Benzoxazolinone aryl sulfonamides as potent, selective Na v 1.7 inhibitors with in vivo efficacy in a preclinical pain model
Joseph E. Pero,Michael A. Rossi,Hannah D. G. F. Lehman,Michael J. Kelly,James Mulhearn,Scott E. Wolkenberg,Matthew J. Cato,Michelle K. Clements,Christopher Daley,Tracey Filzen,Eleftheria N. Finger,Yun Gregan,Darrell A. Henze,Aneta Jovanovska,Rebecca M. Klein,Richard L. Kraus,Yuxing Li,Annie Liang,John Majercak,Jacqueline Panigel,Mark O. Urban,Jixin Wang,Ying-Hong Wang,Andrea K. Houghton,Mark E. Layton +24 more
TL;DR: Novel, peripherally-restricted benzoxazolinone aryl sulfonamides are reported as potentNav1.7 inhibitors with excellent selectivity against the Nav1.5 isoform, which is expressed in the heart muscle.
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Pharmacological Characterization of the Novel and Selective α7 Nicotinic Acetylcholine Receptor-Positive Allosteric Modulator BNC375.
Xiaohai Wang,Christopher Daley,Vanita Gakhar,Henry S. Lange,Joshua D. Vardigan,Michelle Pearson,Xiaoping Zhou,Lee Warren,Corin O. Miller,Michelle Belden,Andrew John Harvey,Anton A. Grishin,Carolyn J. Coles,Sue O'connor,Fiona Thomson,Joseph L. Duffy,Ian M. Bell,Jason M. Uslaner +17 more
TL;DR: Systemic administration of BNC375 reverses scopolamine-induced cognitive deficits in rat novel object recognition and rhesus monkey object retrieval detour task over a wide range of exposures, showing no evidence of an inverted U-shaped dose-effect curve and suggesting that α7 nAChR PAMs have therapeutic potential in central nervous system diseases with cognitive impairments.
15
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Anthony J. Roecker,Mark E. Layton,Joseph E. Pero,Michael J. Kelly,Thomas J. Greshock,Richard L. Kraus,Yuxing Li,Rebecca M. Klein,Michelle K. Clements,Christopher Daley,Aneta Jovanovska,Jeanine E. Ballard,Deping Wang,Fuqiang Zhao,Andrew Brunskill,Xuanjia Peng,Xiu Wang,Haiyan Sun,Andrea K. Houghton,Christopher S. Burgey +19 more
TL;DR: In this article, a series of arylsulfonamide Nav1.7 inhibitors were optimized to achieve improved selectivity over Nav 1.6 while maintaining rodent oral bioavailability through the use of a novel multiparameter optimization paradigm.
9
Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays
Richard L. Kraus,Fuqiang Zhao,Parul S. Pall,Dan Zhou,Joshua D. Vardigan,Andrew Danziger,Yuxing Li,Christopher Daley,Jeanine E. Ballard,Michelle K. Clements,Rebecca M. Klein,Marie A. Holahan,Thomas J. Greshock,Ronald M. Kim,Mark E. Layton,Christopher S. Burgey,Jordi Serra,Darrell A. Henze,Andrea K. Houghton +18 more
TL;DR: In this paper, the authors developed rhesus macaque models of action potential propagation, nociception, and olfaction, to measure Nav1.7 target modulation in vivo.