C
Christian Watson
Researcher at Research Triangle Park
Publications - 4
Citations - 737
Christian Watson is an academic researcher from Research Triangle Park. The author has contributed to research in topics: CCR5 receptor antagonist & Transgene. The author has an hindex of 3, co-authored 4 publications receiving 678 citations.
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Journal ArticleDOI
A simple method for quantifying functional selectivity and agonist bias.
Terry P. Kenakin,Christian Watson,Vanessa Muniz-Medina,Arthur Christopoulos,Steven J. Novick +4 more
TL;DR: A scale based on the Black and Leff operational model that contains the key elements required to describe 7TM agonism, namely, affinity for the receptor and efficacy in activating a particular signaling pathway, can statistically evaluate selective agonist effects in a manner that can theoretically inform structure-activity studies and/or drug candidate selection matrices.
Journal ArticleDOI
The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor
TL;DR: 4-{[4-({(3R)-1-Butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5dioxo-1,4,9-triazaspiro]oxy}benzoic acid hydrochloride (873140) is a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1.
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Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.
Wieslaw M. Kazmierski,Don L. Anderson,Christopher Joseph Aquino,Brian Andrew Chauder,Maosheng Duan,Robert G. Ferris,Terrence Peter Kenakin,Cecilia S. Koble,Dan G. Lang,Maggie S. McIntyre,Jennifer Poole Peckham,Christian Watson,Pat Wheelan,Andrew Spaltenstein,Mary Beth Wire,Angilique Svolto,Michael Youngman +16 more
TL;DR: SAR converting leads 1 and 2 to druglike molecules and the pivotal structural motif enabling this transition was the secondary sulfonamide substituent paved the way to enhancing potency and bioavailability and minimizing hERG inhibition.
Journal ArticleDOI
Pharmacological applications of baculovirus-mediated protein expression in mammalian cells
TL;DR: An example of BacMam‐mediated gene delivery to configure a cell‐based assay for pharmacological assessment of a G protein‐coupled receptor and a protocol is provided to assess the susceptibility of new cell lines to transduction by the virus.