50 results on '"Vangrevelinghe, Eric"'
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2. Discovery of NP3-253, a Potent Brain Penetrant Inhibitor of the NLRP3 Inflammasome.
3. Identification of TAK-756, A Potent TAK1 Inhibitor for the Treatment of Osteoarthritis through Intra-Articular Administration.
4. Identification and characterization of a phenyl-thiazolyl-benzoic acid derivative as a novel RAR/RXR agonist
5. Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors
6. Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood
7. Supplementary Table S2 from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent
8. Data from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent
9. Supplementary Figures, Methods, and References from Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent
10. Supplementary Data from Potent and Selective Inhibition of Polycythemia by the Quinoxaline JAK2 Inhibitor NVP-BSK805
11. Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia
12. Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
13. Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist
14. Conformational Studies of Poly(Methylidene Malonate 2.1.2)
15. Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay
16. Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β
17. Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain
18. Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model
19. Orally bioavailable Syk inhibitors with activity in a rat PK/PD model
20. An Activating Janus Kinase-3 Mutation Is Associated with Cytotoxic T Lymphocyte Antigen-4-Dependent Immune Dysregulation Syndrome
21. Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension
22. Syk inhibitors with high potency in presence of blood
23. NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitroand in vivo
24. An Integrated Approach for Fragment‐Based Lead Discovery: Virtual, NMR, and High‐Throughput Screening Combined with Structure‐Guided Design. Application to the Aspartyl Protease Renin.
25. 2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes
26. Discovery and Profiling of a Selective and Efficacious Syk Inhibitor
27. Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors
28. 2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors
29. Type II JAK2 Inhibitor NVP-CHZ868 Is Active in Vivo Against JAK2-Dependent B-Cell Acute Lymphoblastic Leukemias (B-ALLs)
30. JAK2 L884P Mutation Confers Resistance To The Type II JAK2 Inhibitor NVP-BBT594 When Co-Occurring With JAK2 R683G But Not JAK2 V617F
31. A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P3–P1 Pharmacophore
32. Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent
33. Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition
34. Genetic Resistance to JAK2 Enzymatic Inhibitors Is Overcome by HSP90 Inhibition
35. Identification of a Potent Janus Kinase 3 Inhibitor with High Selectivity within the Janus Kinase Family
36. Potent and Selective Inhibition of Polycythemia by the Quinoxaline JAK2 Inhibitor NVP-BSK805
37. Novel, Potent and Selective JAK2 Inhibitors.
38. A Small-Molecule Dengue Virus Entry Inhibitor
39. Computational Approaches for Fragment Optimization
40. New Developments and Applications of Docking and High-Throughput Docking for Drug Design and in silico Screening
41. Synthesis and Wagner—Meerwein Rearrangement of 9-(α-Hydroxyalkyl)xanthenes to 10-Substituted Dibenz[b,f]oxepins: Scope, Limitations and ab initio Calculations.
42. Synthesis and Wagner-Meerwein Rearrangement of 9-(α-Hydroxyalkyl)xanthenes to 10-Substituted Dibenz[b,f]oxepins: Scope, Limitations and ab initio Calculations
43. Discovery of a Potent and Selective Protein Kinase CK2 Inhibitor by High-Throughput Docking
44. Structure-Based Design and Synthesis of 2-Benzylidene-benzofuran-3-ones as Flavopiridol Mimics
45. 3D-QSAR CoMFA Study on Imidazolinergic I2 Ligands: A Significant Model through a Combined Exploration of Structural Diversity and Methodology
46. Discovery and Profiling ofa Selective and EfficaciousSyk Inhibitor.
47. Molecular modelling of poly(methylidene malonate 2.1.2) using a continuum solvation approach
48. A NovelClass of Oral Direct Renin Inhibitors: HighlyPotent 3,5-Disubstituted Piperidines Bearing a Tricyclic P3–P1Pharmacophore.
49. Type II JAK2 Inhibitor NVP-CHZ868 Is Active in VivoAgainst JAK2-Dependent B-Cell Acute Lymphoblastic Leukemias (B-ALLs)
50. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
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