Michael G. Johnson

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An Inhibitory Metabolite Leads to Dose- and Time-Dependent Pharmacokinetics of (R)-N-{1-[3-(4-Ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in Human Subjects After Multiple Dosing

G. Tonn, S. Wong, Sylvia C. Wong, 2009, Drug Metabolism and Disposition.

Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking

A. Ashworth, J. Irwin, B. Shoichet, 2020, Science Advances.

Gene Expression Analysis of Host Innate Immune Responses during Lethal H5N1 Infection in Ferrets

Ali Danesh, Patricia V. Turner, Thomas Rowe, 2008, Journal of Virology.

Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer.

Michael G. Johnson, J. Medina, Xinrong Ma, 2006, Cancer research.

Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.

Feng Xu, T. Schall, Qingge Xu, 2007, Bioorganic & medicinal chemistry letters.

Sequential Metabolism of AMG 487, a Novel CXCR3 Antagonist, Results in Formation of Quinone Reactive Metabolites That Covalently Modify CYP3A4 Cys239 and Cause Time-Dependent Inhibition of the Enzyme

D. Rock, R. Subramanian, G. Tonn, 2012, Drug Metabolism and Disposition.

Discovery of potent and specific CXCR3 antagonists.

B. Lemon, S. Miao, T. Sullivan, 2012, Bioorganic & medicinal chemistry letters.

The Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in vivo Selectivity over BACE2.

D. Whittington, Michael G. Johnson, M. Bartberger, 2020, Journal of medicinal chemistry.

Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.

E. Rickel, W. Shen, Michael G. Johnson, 2012, Bioorganic & medicinal chemistry letters.

Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.

R. Hungate, M. Rong, W. Zhong, 2010, Bioorganic & medicinal chemistry letters.

Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.

R. Hungate, M. Rong, W. Zhong, 2010, Bioorganic & medicinal chemistry letters.

Discovery and in Vivo Evaluation of Dual PI3K-beta/delta inhibitors

D. Whittington, Yi Chen, K. Miner, 2012 .

Antagonists of CXCR3: a review of current progress

Michael G. Johnson, J. Medina, T. Collins, 2007 .

Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.

S. Wong, Michael G. Johnson, Bettina van Lengerich, 2014, Bioorganic & medicinal chemistry letters.

Antagonism of CXCR 3 Inhibits Lung Metastasis in a Murine Model of Metastatic Breast Cancer

Michael G. Johnson, J. Medina, Xinrong Ma, 2006 .

Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.

R. Hungate, M. Rong, W. Zhong, 2011, Bioorganic & medicinal chemistry letters.

Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quino

J. McCarter, D. Whittington, Iain D. G. Campuzano, 2016, Journal of medicinal chemistry.

Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.

B. Lemon, T. Sullivan, G. Tonn, 2008, Bioorganic & medicinal chemistry letters.

Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.

Xiaolin Hao, Ben Fisher, Andreas Reichelt, 2015, Journal of medicinal chemistry.

Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.

D. Whittington, Yi Chen, K. Miner, 2012, Journal of medicinal chemistry.

G-Protein-Coupled Receptor Microarrays for Multiplexed Compound Screening

J. Lahiri, Ye Fang, Brian L. Webb, 2006, Journal of biomolecular screening.

Bioactivation of a Novel 2-Methylindole-Containing Dual Chemoattractant Receptor-Homologous Molecule Expressed on T-Helper Type-2 Cells/d-Prostanoid Receptor Antagonist Leads to Mechanism-Based CYP3A Inactivation: Glutathione Adduct Characterization and Prediction of In Vivo Drug-Drug Interaction

R. Subramanian, G. Tonn, Michael G. Johnson, 2010, Drug Metabolism and Disposition.

Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking

A. Ashworth, J. Irwin, B. Shoichet, 2021, Science Advances.

Discovery of novel intracellular receptor modulating drugs

S. Bender, L. Hamann, Michael G. Johnson, 1996, The Journal of Steroid Biochemistry and Molecular Biology.