BMS-345541 Is a Highly Selective Inhibitor of IκB Kinase That Binds at an Allosteric Site of the Enzyme and Blocks NF-κB-dependent Transcription in Mice

James R. Burke, Mark A. Pattoli, Kurt R. Gregor, +9

Journal of Biological Chemistry

Discovery of a 1<i>H</i>-Benzoimidazol-2-yl)-1<i>H</i>-pyridin-2-one (BMS-536924) Inhibitor of Insulin-like Growth Factor I Receptor Kinase with in Vivo Antitumor Activity

Mark D. Wittman, Joan M. Carboni, Ricardo M. Attar, +30

Journal of Medicinal Chemistry

PharmacotherapyInsulin ReceptorInsulin SignalingPharmaceutical ChemistryTumor Biology +19

Novel N-Linked Aminopiperidine Inhibitors of Bacterial Topoisomerase Type II: Broad-Spectrum Antibacterial Agents with Reduced hERG Activity

Folkert Reck, Richard A. Alm, Patrick Brassil, +16

Journal of Medicinal Chemistry

Reduced Herg ActivityAntimicrobial ChemotherapyPharmaceutical ChemistryDrug ResistanceMedicinal Chemistry +19

Novel N-Linked Aminopiperidine Inhibitors of Bacterial Topoisomerase Type II with Reduced p<i>K</i>_a: Antibacterial Agents with an Improved Safety Profile

Folkert Reck, Richard A. Alm, Patrick Brassil, +12

Journal of Medicinal Chemistry

Evaluation of Multiple in Vitro Systems for Assessment of CYP3A4 Induction in Drug Discovery: Human Hepatocytes, Pregnane X Receptor Reporter Gene, and Fa2N-4 and HepaRG Cells

Dermot F. McGinnity, George Zhang, Jane R. Kenny, +7

Drug Metabolism and Disposition

Development of Gut-Selective Pan-Janus Kinase Inhibitor TD-1473 for Ulcerative Colitis: A Translational Medicine Programme

William J. Sandborn, Deanna D. Nguyen, David T. Beattie, +15

Journal of Crohn s and Colitis

Discovery of Checkpoint Kinase Inhibitor (<i>S</i>)-5-(3-Fluorophenyl)-<i>N</i>-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by Structure-Based Design and Optimization of Thiophenecarboxamide Ureas

Vibha Oza, Susan Ashwell, Lynsie Almeida, +22

Journal of Medicinal Chemistry

Drug TargetMolecular BiologyChemical BiologyPharmaceutical ChemistryMolecular Pharmacology +18

Novel DNA Gyrase Inhibiting Spiropyrimidinetriones with a Benzisoxazole Scaffold: SAR and in Vivo Characterization

Gregory S. Basarab, Patrick Brassil, P. Doig, +8

Journal of Medicinal Chemistry

Pharmaceutical ScienceDrug TargetStaphylococcus AureusMolecular BiologyChemical Biology +17

Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization

James J. Dowling, Claudio Chuaqui, Timothy Pontz, +18

ACS Medicinal Chemistry Letters

Combinatorial ChemistryDrug TargetStructure-guided HybridizationMolecular BiologyCell Proliferation +16

Discovery of (+)-<i>N</i>-(3-Aminopropyl)-<i>N</i>-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-<i>d</i>]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a Kinesin Spindle Protein Inhibitor and Potential Anticancer Agent

Maria‐Elena Theoclitou, Brian Aquila, M. Block, +22

Journal of Medicinal Chemistry