Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development

James J. Crawford, Adam R. Johnson, Dinah Misner, +22

Journal of Medicinal Chemistry

Tyrosine KinaseImmunologyBiological TherapyPharmacotherapyImmunotherapeutics +22

A Physiologically Based Pharmacokinetic Modeling Approach to Predict Disease–Drug Interactions: Suppression of CYP3A by IL-6

Krishna K. Machavaram, Lisa M. Almond, Amin Rostami‐Hodjegan, +6

Clinical Pharmacology & Therapeutics

Cytokine LevelsImmunologyPhysiologically-based Pharmacokinetic ModelingPharmacodynamic ModelingSystems Pharmacology +18

Comparison of the function and expression of CYP26A1 and CYP26B1, the two retinoic acid hydroxylases

Ariel R. Topletz, Jayne E. Thatcher, Alex Zelter, +4

Biochemical Pharmacology

Aldehyde DehydrogenaseCellular EnzymologyBiochemistryNatural SciencesRetinoic Acid Hydroxylases +5

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design

Matthew Volgraf, Benjamin D. Sellers, Yu Jiang, +29

Journal of Medicinal Chemistry

Synaptic TransmissionNeurotransmitterSynaptic SignalingSocial SciencesMolecular Pharmacology +26

Drug–Drug Interaction Potential of Marketed Oncology Drugs: In Vitro Assessment of Time-Dependent Cytochrome P450 Inhibition, Reactive Metabolite Formation and Drug–Drug Interaction Prediction

Jane R. Kenny, Sophie Mukadam, Chenghong Zhang, +4

Pharmaceutical Research

Drug InteractionsMarketed Oncology DrugsPreclinical Drug EvaluationPharmacological StudyMedicine +8

Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition

Brian S. Safina, Stewart Baker, Matt Baumgardner, +44

Journal of Medicinal Chemistry

Drug TargetImmunologyInflammatory ArthritisSystems PharmacologyMolecular Pharmacology +23

A Comparison of the Roles of Peroxisome Proliferator-Activated Receptor and Retinoic Acid Receptor on CYP26 Regulation

Suzanne Tay, Leslie J. Dickmann, Vaishali Dixit, +1

Molecular Pharmacology

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349

Zhonghua Pei, Elizabeth Blackwood, Lichuan Liu, +27

ACS Medicinal Chemistry Letters

Drug TargetChemoprevention StrategyAdvanced Lead 1PharmacotherapyChemical Biology +19

Changes in maternal liver Cyp2c and Cyp2d expression and activity during rat pregnancy

Leslie J. Dickmann, Suzanne Tay, Tauri Senn, +5

Biochemical Pharmacology

Maternal Liver Cyp2cPlacental DevelopmentLiver PhysiologyPhysiologyGynecology +9

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved <i>in Vivo</i> Profile

Elisia Villemure, Matthew Volgraf, Yu Jiang, +19

ACS Medicinal Chemistry Letters