James McGee
Eli Lilly and Company
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Featured researches published by James McGee.
Bioorganic & Medicinal Chemistry Letters | 2016
Steven L. Kuklish; Stephen Antonysamy; Shobha N. Bhattachar; Srinivasan Chandrasekhar; Matthew Joseph Fisher; Adrian J. Fretland; Karen M. Gooding; Anita Harvey; Norman E. Hughes; John G. Luz; Peter Rudolph Manninen; James McGee; Antonio Navarro; Bryan H. Norman; Katherine Marie Partridge; Steven J. Quimby; Matthew A. Schiffler; Ashley V. Sloan; Alan M. Warshawsky; Jeremy Schulenburg York; Xiao-Peng Yu
Here we report on novel, potent 3,3-dimethyl substituted N-aryl piperidine inhibitors of microsomal prostaglandin E synthases-1(mPGES-1). Example 14 potently inhibited PGE2 synthesis in an ex vivo human whole blood (HWB) assay with an IC50 of 7nM. In addition, 14 had no activity in human COX-1 or COX-2 assays at 30μM, and failed to inhibit human mPGES-2 at 62.5μM in a microsomal prep assay. These data are consistent with selective mPGES-1-mediated reduction of PGE2. In dog, 14 had oral bioavailability (74%), clearance (3.62mL/(min*kg)) and volume of distribution (Vd,ss=1.6L/kg) values within our target ranges. For these reasons, 14 was selected for further study.
Bioorganic & Medicinal Chemistry Letters | 2017
Katherine Marie Partridge; Stephen Antonysamy; Shobha N. Bhattachar; Srinivasan Chandrasekhar; Matthew Joseph Fisher; Adrian J. Fretland; Karen M. Gooding; Anita Harvey; Norman E. Hughes; Steven L. Kuklish; John G. Luz; Peter Rudolph Manninen; James McGee; Daniel R. Mudra; Antonio Navarro; Bryan H. Norman; Steven J. Quimby; Matthew A. Schiffler; Ashley V. Sloan; Alan M. Warshawsky; Jennifer Weller; Jeremy Schulenburg York; Xiao-Peng Yu
We describe a novel class of acidic mPGES-1 inhibitors with nanomolar enzymatic and human whole blood (HWB) potency. Rational design in conjunction with structure-based design led initially to the identification of anthranilic acid 5, an mPGES-1 inhibitor with micromolar HWB potency. Structural modifications of 5 improved HWB potency by over 1000×, reduced CYP2C9 single point inhibition, and improved rat clearance, which led to the selection of [(cyclopentyl)ethyl]benzoic acid compound 16 for clinical studies. Compound 16 showed an IC80 of 24nM for inhibition of PGE2 formation in vitro in LPS-stimulated HWB. A single oral dose resulted in plasma concentrations of 16 that exceeded its HWB IC80 in both rat (5mg/kg) and dog (3mg/kg) for over twelve hours.
Clinical and Translational Science | 2018
Nathan P. Coussens; G. Sitta Sittampalam; Rajarshi Guha; Kyle R. Brimacombe; Abigail Grossman; Thomas Dy Chung; Jeffrey R. Weidner; Terry Riss; O. Joseph Trask; Douglas S. Auld; Jayme L. Dahlin; Viswanath Devanaryan; Timothy L. Foley; James McGee; Steven D. Kahl; Stephen C. Kales; Michelle R. Arkin; Jonathan B. Baell; Bruce Bejcek; Neely Gal‐Edd; Marcie A. Glicksman; Joseph Haas; Philip W. Iversen; Marilu Hoeppner; Stacy Lathrop; Eric W. Sayers; Hanguan Liu; Bart Trawick; Julie McVey; Vance Lemmon
The Assay Guidance Manual (AGM) is an eBook of best practices for the design, development, and implementation of robust assays for early drug discovery. Initiated by pharmaceutical company scientists, the manual provides guidance for designing a “testing funnel” of assays to identify genuine hits using high‐throughput screening (HTS) and advancing them through preclinical development. Combined with a workshop/tutorial component, the overall goal of the AGM is to provide a valuable resource for training translational scientists.
Archive | 2004
G. Sitta Sittampalam; Nathan P. Coussens; Henrike Nelson; Michelle R. Arkin; Douglas S. Auld; Christopher M. Austin; Bruce Bejcek; Marcie A. Glicksman; James Inglese; Philip W. Iversen; Zhuyin Li; James McGee; Owen McManus; Lisa Minor; Andrew D. Napper; John M. Peltier; Terry Riss; O. Joseph Trask; Jeffrey R. Weidner
Bioorganic & Medicinal Chemistry Letters | 2003
Jingdan Hu; Cynthia L. Cwi; David L. Smiley; David E. Timm; Jon A. Erickson; James McGee; Hsiu-Chiung Yang; David Mendel; Patrick C. May; Mike Shapiro; James R. McCarthy
Bioorganic & Medicinal Chemistry Letters | 2004
Jason Lamar; Jingdan Hu; Ana B. Bueno; Hsiu-Chiung Yang; Deqi Guo; James Densmore Copp; James McGee; Bruce D. Gitter; David E. Timm; Patrick C. May; James R. McCarthy; Shu-Hui Chen
Bioorganic & Medicinal Chemistry Letters | 2004
Shu-Hui Chen; Jason Lamar; Deqi Guo; Todd J. Kohn; Hsiu-Chiung Yang; James McGee; David E. Timm; Jon A. Erickson; Yvonne Yip; Patrick C. May; James R. McCarthy
Archive | 2012
John Strelow; Walthere Dewe; Phillip W Iversen; Harold B Brooks; Jeffrey A Radding; James McGee; Jeffrey R. Weidner
Plasmid | 2001
James McGee; Bruce Bejcek
Experimental Cell Research | 2000
Ali Jazayeri; James McGee; Takeshi Shimamura; Scott B. Cross; Bruce Bejcek