Stefanus J. Steyn

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Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS)

S. Steyn, M. Varma, A. El‐Kattan, 2015, Pharmaceutical Research.

Imaging Leucine-Rich Repeat Kinase 2 In Vivo with 18F-Labeled Positron Emission Tomography Ligand.

Steven H. Liang, L. Josephson, J. Daunais, 2022, Journal of medicinal chemistry.

PF-03814735, an Orally Bioavailable Small Molecule Aurora Kinase Inhibitor for Cancer Therapy

L. Pustilnik, J. Christensen, B. D. Cohen, 2010, Molecular Cancer Therapeutics.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Gregory W. Kauffman, David S. Ramirez, L. Pustilnik, 2017, MedChemComm.

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.

Gregory W. Kauffman, L. Pustilnik, A. Stepan, 2015, ACS medicinal chemistry letters.

β -OXIDATION OF [9,10(n)- 3 H]PALMITATE BY HUMAN LEUKOCYTES: A SIMPLE IN SITU ASSAY TO ASSESS MITOCHONDRIAL TOXICITY IN THE PRESENCE OF TOXINS

C. J. Van der Schyf, L. Mienie, Stefanus J. Steyn, 2000 .

Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline.

C. Thorn, J. Edgerton, Rebecca E O'connor, 2018, ACS chemical neuroscience.

Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.

C. Thorn, T. Kenakin, J. Edgerton, 2017, Journal of medicinal chemistry.

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Gregory W. Kauffman, L. Pustilnik, A. Stepan, 2015, Bioorganic & medicinal chemistry letters.

Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.

M. Mansour, S. Sakya, K. Borzilleri, 2009, Journal of medicinal chemistry.

DMD054031 1975..1993

R. Obach, L. Di, B. Feng, 2013 .

Inositol Phosphate Accumulation in Vivo Provides a Measure of Muscarinic M1 Receptor Activation.

J. Edgerton, V. Reinhart, S. Grimwood, 2016, Biochemistry.

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

R. Kurumbail, B. L. Kormos, M. Hayward, 2015, Journal of medicinal chemistry.

Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor.

R. D. Connell, L. Pustilnik, Joel Morris, 2007, Cancer research.

Studies on the interactions of tobacco leaf and tobacco smoke constituents and monoamine oxidase

S. Steyn, K. Castagnoli, G. Magnin, 2009, Neurotoxicity Research.

Leucine-rich Repeat Kinase 2 (LRRK2) Pharmacological Inhibition Abates α-Synuclein Gene-induced Neurodegeneration*

Elie Needle, A. West, L. Volpicelli-Daley, 2015, The Journal of Biological Chemistry.

pH-Dependent solubility and permeability criteria for provisional biopharmaceutics classification (BCS and BDDCS) in early drug discovery.

Li Di, Hui Zhang, Iain Gardner, 2012, Molecular pharmaceutics.

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.

Gregory W. Kauffman, J. Edgerton, S. Steyn, 2016, Journal of medicinal chemistry.

Biochemical and pharmacological characterization of human c-Met neutralizing monoclonal antibody CE-355621

G. Karam, J. Lapointe, J. Xu, 2012, mAbs.

Modulation of NMDA receptor function by inhibition of d-amino acid oxidase in rodent brain

A. Ganong, M. Hajós, P. Seymour, 2011, Neuropharmacology.

Design and optimization of selective azaindole amide M1 positive allosteric modulators.

Gregory W. Kauffman, R. Obach, J. Edgerton, 2016, Bioorganic & medicinal chemistry letters.

Projecting ADME Behavior and Drug-Drug Interactions in Early Discovery and Development: Application of the Extended Clearance Classification System

T. Maurer, D. Scott, S. Steyn, 2016, Pharmaceutical Research.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

L. Michael, T. Goosen, M. Tu, 2013, Bioorganic & medicinal chemistry letters.

Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.

R Scott Obach, George Chang, Ayman El-Kattan, 2010, Journal of medicinal chemistry.

Assessment of in silico models for fraction of unbound drug in human liver microsomes

George Chang, Jing Lin, G. Chang, 2010, Expert opinion on drug metabolism & toxicology.

Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold.

R. Kurumbail, B. L. Kormos, P. Verhoest, 2014, Bioorganic & medicinal chemistry letters.

Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS)

M. Varma, A. El‐Kattan, C. Allerton, 2015, Pharmaceutical Research.

Cytochrome-P450 Mediated Drug-Drug Interactions of Substrate Drugs: Assessing Clinical Risk Based on Molecular Properties and Extended Clearance Classification System.

S. Steyn, M. Varma, Stefanus J. Steyn, 2020, Molecular pharmaceutics.

Permeability Comparison between Hepatocyte and Low Efflux MDCKII Cell Monolayer

L. Di, Patrick E. Trapa, Y. Lai, 2014, The AAPS Journal.

LRRK2 inhibitors induce reversible changes in nonhuman primate lungs without measurable pulmonary deficits

Matthew L. Maddess, A. Stepan, T. Sherer, 2020, Science Translational Medicine.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Z. Hendsch, B. Posner, D. Kung, 2012, Bioorganic & medicinal chemistry letters.

Measurement of mitochondrial respiration in permeabilized murine neuroblastoma (N-2alpha) cells, a simple and rapid in situ assay to investigate mitochondrial toxins.

C. J. Van der Schyf, S. Steyn, L. Mienie, 2005, Journal of biochemical and biophysical methods.

Use of the dTAG system in vivo to degrade CDK2 and CDK5 in adult mice and explore potential safety liabilities

Seda Arat, S. Thibault, Wenyue Hu, 2023, Toxicological sciences : an official journal of the Society of Toxicology.

Rescue of Dying Neurons by (R)‐Deprenyl in the MPTP‐Mouse Model of Parkinson's Disease Does Not Include Restoration of Neostriatal Dopamine

K. Castagnoli, N. Castagnoli, Stefanus J. Steyn, 2001, Annals of the New York Academy of Sciences.

Insights From an Integrated Physiologically Based Pharmacokinetic Model for Brain Penetration.

D. Scott, Patrick E. Trapa, J. Liras, 2016, Journal of pharmaceutical sciences.

Selective Inhibition of MAO-B through Chronic Low-Dose (R)-Deprenyl Treatment in C57BL/6 Mice Has No Effect on Basal Neostriatal Dopamine Levels

K. Castagnoli, N. Castagnoli, Stefanus J. Steyn, 2001, Experimental Neurology.

High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models.

David B Duignan, John S Janiszewski, Theodore E Liston, 2008, Current drug metabolism.

Strategic use of plasma and microsome binding to exploit in vitro clearance in early drug discovery.

D. Scott, S. Steyn, G. Chang, 2010, ACS medicinal chemistry letters.

LRRK2 kinase inhibitors induce a reversible effect in the lungs of non-human primates with no measurable pulmonary deficits

Matthew L. Maddess, A. Stepan, T. Sherer, 2018, bioRxiv.

The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.

L. Pustilnik, S. Bhattacharya, J. Chen, 2007, Bioorganic & medicinal chemistry letters.

Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.

Kevin Ogilvie, M. Brodney, S. Mente, 2024, Journal of medicinal chemistry.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Z. Hendsch, B. Posner, D. Kung, 2012, Bioorganic & medicinal chemistry letters.

Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.

Gregory W. Kauffman, L. Pustilnik, É. Hajós‐Korcsok, 2024, Journal of medicinal chemistry.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Gregory W. Kauffman, David S. Ramirez, L. Pustilnik, 2017, MedChemComm.