Discovery of a Potent and Selective Protein Kinase CK2 Inhibitor by High-Throughput Docking

Eric Vangrevelinghe, Kaspar Zimmermann, Joseph Schoepfer, +3

Journal of Medicinal Chemistry

Molecular DockingMedicinal ChemistryDrug TargetHigh-throughput DockingNovel Therapy +13

A Small-Molecule Dengue Virus Entry Inhibitor

Qingyin Wang, Sejal Patel, Eric Vangrevelinghe, +12

Antimicrobial Agents and Chemotherapy

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition

Oliver Weigert, Andrew A. Lane, Liat Bird, +28

The Journal of Experimental Medicine

Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

Rita Andraos, Zhiyan Qian, Débora Bonenfant, +21

Cancer Discovery

Crystal StructureMolecular BiologySignaling PathwayReceptor Tyrosine KinaseActivation-loop Phosphorylation +19

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia

Shuo-Chieh Wu, Loretta S. Li, Nadja Kopp, +38

Cancer Cell

Hematological MalignancyMixed-phenotype Acute LeukemiaMalignant Blood DisorderImmunologyHematology +4

Potent and Selective Inhibition of Polycythemia by the Quinoxaline JAK2 Inhibitor NVP-BSK805

Fabienne Baffert, Catherine H. Régnier, Alain De Pover, +19

Molecular Cancer Therapeutics

PharmacotherapyExcellent SelectivityPharmaceutical ChemistryMyeloid NeoplasiaHematological Malignancy +18

Identification of a Potent Janus Kinase 3 Inhibitor with High Selectivity within the Janus Kinase Family

Gebhard Thoma, François Nuninger, Rocco Falchetto, +4

Journal of Medicinal Chemistry

Molecular RegulationMolecular PharmacologySignaling PathwayReceptor Tyrosine KinaseAutophagy +20

Structure-Based Design and Synthesis of 2-Benzylidene-benzofuran-3-ones as Flavopiridol Mimics

Joseph Schoepfer, Heinz Fretz, Bhabatosh Chaudhuri, +6

Journal of Medicinal Chemistry

3D-QSAR CoMFA Study on Imidazolinergic I₂ Ligands:  A Significant Model through a Combined Exploration of Structural Diversity and Methodology

Nicolas Baurin, Eric Vangrevelinghe, Luc Morin‐Allory, +5

Journal of Medicinal Chemistry

Drug TargetComfa MethologyChemistryChemical BiologyMedicinal Chemistry +17

Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension

Duncan Shaw, Greg Hollingworth, Nicolas Soldermann, +8

Bioorganic & Medicinal Chemistry Letters

Novel Rock InhibitorsHypertensionPulmonary Arterial HypertensionPulmonary CirculationCardiovascular Disease +8