Follow
Eric Vangrevelinghe
Eric Vangrevelinghe
Investigator III @ Novartis Institutes of Biomedical Research
Verified email at novartis.com
Title
Cited by
Cited by
Year
Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking
E Vangrevelinghe, K Zimmermann, J Schoepfer, R Portmann, D Fabbro, ...
Journal of medicinal chemistry 46 (13), 2656-2662, 2003
2892003
A small-molecule dengue virus entry inhibitor
QY Wang, SJ Patel, E Vangrevelinghe, HY Xu, R Rao, D Jaber, W Schul, ...
Antimicrobial agents and chemotherapy 53 (5), 1823-1831, 2009
2392009
Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition
O Weigert, AA Lane, L Bird, N Kopp, B Chapuy, D van Bodegom, ...
Journal of experimental medicine 209 (2), 259-273, 2012
1702012
Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805
F Baffert, CH Régnier, A De Pover, C Pissot-Soldermann, GA Tavares, ...
Molecular cancer therapeutics 9 (7), 1945-1955, 2010
1442010
Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent
R Andraos, Z Qian, D Bonenfant, J Rubert, E Vangrevelinghe, C Scheufler, ...
Cancer discovery 2 (6), 512-523, 2012
1432012
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics
J Schoepfer, H Fretz, B Chaudhuri, L Muller, E Seeber, L Meijer, O Lozach, ...
Journal of medicinal chemistry 45 (9), 1741-1747, 2002
1342002
Activity of the type II JAK2 inhibitor CHZ868 in B cell acute lymphoblastic leukemia
SC Wu, LS Li, N Kopp, J Montero, B Chapuy, A Yoda, AL Christie, H Liu, ...
Cancer cell 28 (1), 29-41, 2015
1142015
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family
G Thoma, F Nuninger, R Falchetto, E Hermes, GA Tavares, ...
Journal of medicinal chemistry 54 (1), 284-288, 2011
1112011
3D-QSAR CoMFA study on imidazolinergic I2 ligands: a significant model through a combined exploration of structural diversity and methodology
N Baurin, E Vangrevelinghe, L Morin-Allory, JY Mérour, P Renard, ...
Journal of medicinal chemistry 43 (6), 1109-1122, 2000
662000
Discovery and SAR of potent, orally available 2, 8-diaryl-quinoxalines as a new class of JAK2 inhibitors
C Pissot-Soldermann, M Gerspacher, P Furet, C Gaul, P Holzer, ...
Bioorganic & Medicinal Chemistry Letters 20 (8), 2609-2613, 2010
442010
2, 6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes
MJ van Eis, JP Evenou, P Floersheim, C Gaul, SW Cowan-Jacob, ...
Bioorganic & medicinal chemistry letters 21 (24), 7367-7372, 2011
432011
Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension
D Shaw, G Hollingworth, N Soldermann, E Sprague, W Schuler, ...
Bioorganic & medicinal chemistry letters 24 (20), 4812-4817, 2014
412014
New scoring functions for virtual screening from molecular dynamics simulations with a quantum-refined force-field (QRFF-MD). Application to cyclin-dependent kinase 2
P Ferrara, A Curioni, E Vangrevelinghe, T Meyer, T Mordasini, ...
Journal of chemical information and modeling 46 (1), 254-263, 2006
412006
An activating janus kinase-3 mutation is associated with cytotoxic T lymphocyte antigen-4-dependent immune dysregulation syndrome
H Sic, M Speletas, V Cornacchione, M Seidl, M Beibel, B Linghu, F Yang, ...
Frontiers in Immunology 8, 1824, 2017
312017
Discovery and profiling of a selective and efficacious Syk inhibitor
G Thoma, AB Smith, MJ van Eis, E Vangrevelinghe, J Blanz, R Aichholz, ...
Journal of Medicinal Chemistry 58 (4), 1950-1963, 2015
292015
Optimizing a weakly binding fragment into a potent RORγt inverse agonist with efficacy in an in vivo inflammation model
DA Carcache, A Vulpetti, J Kallen, H Mattes, D Orain, R Stringer, ...
Journal of medicinal chemistry 61 (15), 6724-6735, 2018
262018
A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P3P1 Pharmacophore
N Ostermann, S Ruedisser, C Ehrhardt, W Breitenstein, A Marzinzik, ...
Journal of medicinal chemistry 56 (6), 2196-2206, 2013
242013
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors
M Gerspacher, P Furet, C Pissot-Soldermann, C Gaul, P Holzer, ...
Bioorganic & Medicinal Chemistry Letters 20 (5), 1724-1727, 2010
222010
Computational approaches for fragment optimization
E Vangrevelinghe, S Rudisser
Current Computer-Aided Drug Design 3 (1), 69-83, 2007
222007
Syk inhibitors with high potency in presence of blood
G Thoma, J Blanz, P Bühlmayer, P Drückes, M Kittelmann, AB Smith, ...
Bioorganic & Medicinal Chemistry Letters 24 (10), 2278-2282, 2014
212014
The system can't perform the operation now. Try again later.
Articles 1–20