Discovery of <i>N</i>-(2-Chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a Dual Src/Abl Kinase Inhibitor with Potent Antitumor Activity in Preclinical Assays

Louis J. Lombardo, Francis Y. Lee, Ping Chen, +24

Journal of Medicinal Chemistry

Drug TargetPreclinical AssaysPharmacotherapyCompound 13Pharmaceutical Chemistry +17

MEK inhibitors: The chemistry and biological activity of U0126, its analogs, and cyclization products

John V. Duncia, Joseph B. Santella, C. Anne Higley, +22

Bioorganic & Medicinal Chemistry Letters

Biological ActivityMek InhibitorsMedicinal ChemistryBiochemistryNatural Sciences +10

2-Aminothiazole as a Novel Kinase Inhibitor Template. Structure−Activity Relationship Studies toward the Discovery of <i>N</i> -(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (Dasatinib, BMS-354825) as a Potent <i>pan</i> -Src Kinase Inhibitor

Jagabandhu Das, Ping Chen, Derek Norris, +18

Journal of Medicinal Chemistry

Selective Itk Inhibitors Block T-Cell Activation and Murine Lung Inflammation

Tai-An Lin, Kim W. McIntyre, Jagabandhu Das, +23

Biochemistry

Inflammatory Lung DiseaseLung InflammationT-regulatory CellImmunologyImmunologic Mechanism +19

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56lck inhibitors

Jagabandhu Das, Robert V. Moquin, James C. Lin, +10

Bioorganic & Medicinal Chemistry Letters

Potent P56lck InhibitorsMedicinal ChemistryBiochemistryMedicineNatural Sciences +6

A Monoclonal Antibody TrkB Receptor Agonist as a Potential Therapeutic for Huntington’s Disease

Daniel G. Todd, Ian Gowers, Simon DOWLER, +13

PLoS ONE

Neurodegenerative DiseasesHuntington ’Hd PathogenesisExon 1Medicine +12

Synthesis of 1,3-Diynes Using Palladium-Copper Catalysis

John Wityak, John B. Chan

Synthetic Communications

Materials ScienceCross-coupling ReactionEngineeringOrganic ChemistryAbstract 1,3-Diynes +4

Isoxazolines as Potent Antagonists of the Integrin α_vβ₃

William J. Pitts, John Wityak, Joanne M. Smallheer, +9

Journal of Medicinal Chemistry

Pharmaceutical SciencePharmacotherapyPlatelet AggregationExperimental PharmacologyPharmaceutical Chemistry +14

Synthesis of Thrombin Inhibitor DuP 714

John Wityak, Richard A. Earl, Matthew M. Abelman, +6

The Journal of Organic Chemistry

Altmetric Attention ScorePharmacotherapyChemical BiologyThrombosisMedicinal Chemistry +16

A Profiling Platform for the Characterization of Transglutaminase 2 (TG2) Inhibitors

Sabine Schaertl, Michael E. Prime, John Wityak, +6

SLAS DISCOVERY