R. Nagilla

发表

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Michelle C. Schaeffer, Carol A. Capriotti, P. A. Harris, 2017, Journal of medicinal chemistry.

Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.

N. Aiyar, D. Behm, S. Douglas, 2008, Bioorganic & medicinal chemistry letters.

Nasal route for direct delivery of solutes to the central nervous system: fact or fiction?

U. Kompella, R. Nagilla, S. Mathison, 1998, Journal of drug targeting.

Optimization of a Series of RIPK2 PROTACs.

Aditya R. Thawani, I. E. Smith, R. Nagilla, 2021, Journal of medicinal chemistry.

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[ d]thiazol-5-ylamino)-6-( tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

J. Bertin, K. Erhard, M. Convery, 2019, Journal of medicinal chemistry.

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Michelle C. Schaeffer, Carol A. Capriotti, Paul E. Lamoureux, 2019, Journal of medicinal chemistry.

Identification of an antibody‐based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues

P. A. Harris, J. Bertin, N. Campobasso, 2017, Pharmacology research & perspectives.

Characterization of GSK′963: a structurally distinct, potent and selective inhibitor of RIP1 kinase

Michelle C. Schaeffer, Carol A. Capriotti, J. Bertin, 2015, Cell Death Discovery.

Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.

Dwight M. Morrow, A. Sulpizio, R. Nagilla, 2009, Bioorganic & medicinal chemistry letters.

Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.

Baoguang Zhao, M. Head, N. Laping, 2009, Bioorganic & medicinal chemistry letters.

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.

Michelle C. Schaeffer, Carol A. Capriotti, P. A. Harris, 2013, ACS medicinal chemistry letters.

Cassette dosing for pharmacokinetic screening in drug discovery: comparison of clearance, volume of distribution, half-life, mean residence time, and oral bioavailability obtained by cassette and discrete dosing in rats.

R. Nagilla, M. Nord, L. Jolivette, 2011, Journal of pharmaceutical sciences.

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Deepak Bandyopadhyay, Lauren Dare, Michelle C. Schaeffer, 2016, Journal of medicinal chemistry.

EXTRAPOLATION OF PRECLINICAL PHARMACOKINETICS AND MOLECULAR FEATURE ANALYSIS OF “DISCOVERY-LIKE” MOLECULES TO PREDICT HUMAN PHARMACOKINETICS

Christopher A Evans, Keith W Ward, K. Ward, 2006, Drug Metabolism and Disposition.

Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human

K. Ward, R. Nagilla, L. Jolivette, 2005, Xenobiotica; the fate of foreign compounds in biological systems.

A comprehensive analysis of the role of correction factors in the allometric predictivity of clearance from rat, dog, and monkey to humans.

Keith W Ward, K. Ward, R. Nagilla, 2004, Journal of pharmaceutical sciences.

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

J. Bertin, K. Erhard, D. Lipshutz, 2019 .

The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.

Carol A. Capriotti, J. Bertin, M. Convery, 2016, Journal of medicinal chemistry.

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.

J. Bertin, M. Convery, D. Lipshutz, 2018, ACS medicinal chemistry letters.

AMTB , a TRPM 8 channel blocker : evidence in rats for activity in overactive bladder and painful bladder syndrome

J. Hieble, N. Laping, R. Nagilla, 2008 .

Effect of once weekly treatment with 3,4-methylenedioxymethamphetamine on schedule-controlled behavior in rats.

M. C. Newland, R. Nagilla, M. Bronson, 1998, European Journal of Pharmacology.

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer

P. A. Harris, J. Bertin, M. Mahajan, 2019, ACS medicinal chemistry letters.

AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome.

J. Hieble, N. Laping, R. Nagilla, 2008, American journal of physiology. Renal physiology.

Effect of dodecylmaltoside (DDM) on uptake of BCS III compounds, tiludronate and cromolyn, in Caco-2 cells and rat intestine model

G. Betageri, R. Nagilla, W. Ravis, 2010, Drug delivery.

Investigation of the utility of published in vitro intrinsic clearance data for prediction of in vivo clearance.

Keith W Ward, K. Ward, R. Nagilla, 2006, Journal of pharmacological and toxicological methods.

Stereoselective pharmacokinetics of ketorolac in calves after a single intravenous and oral dose.

R. Nagilla, W. Ravis, S. Duran, 2007, Journal of veterinary pharmacology and therapeutics.

Pharmacokinetics of phenylbutazone in llamas following single intravenous and oral doses.

Alex Simpkins, R. Nagilla, D. Pugh, 2001, Journal of veterinary pharmacology and therapeutics.

Improving the developability profile of pyrrolidine progesterone receptor partial agonists.

C. Duraiswami, N. Laping, Shawn P. Williams, 2010, Bioorganic & medicinal chemistry letters.

Development of potent and selective small-molecule human Urotensin-II antagonists.

N. Aiyar, D. Behm, S. Douglas, 2008, Bioorganic & medicinal chemistry letters.

Stereoselective pharmacokinetics of ketoprofen in llamas following intravenous administration.

R. Nagilla, D. Pugh, W. Ravis, 2001, Journal of veterinary pharmacology and therapeutics.

Pharmacokinetics of flunixin meglumine in llamas following a single intravenous dose.

Alex Simpkins, R. Nagilla, D. Pugh, 2001, Journal of veterinary pharmacology and therapeutics.

Enantiomeric disposition of ketorolac in goats following administration of a single intravenous and oral dose.

R. Nagilla, K. Copedge, S. Miller, 2009, Journal of veterinary pharmacology and therapeutics.

Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics.

J. Bertin, M. Mahajan, R. Nagilla, 2020, Journal of pharmaceutical sciences.

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.

Carol A. Capriotti, J. Bertin, M. Convery, 2018, ACS medicinal chemistry letters.