Application of fragment-based lead generation to the discovery of novel, cyclic amidine β-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency PD Edwards, JS Albert, M Sylvester, D Aharony, D Andisik, O Callaghan, ... Journal of medicinal chemistry 50 (24), 5912-5925, 2007 | 254 | 2007 |
Structural insight into allosteric modulation of protease-activated receptor 2 RKY Cheng, C Fiez-Vandal, O Schlenker, K Edman, B Aggeler, DG Brown, ... Nature 545 (7652), 112-115, 2017 | 238 | 2017 |
Discovery of a novel warhead against β-secretase through fragment-based lead generation S Geschwindner, LL Olsson, JS Albert, J Deinum, PD Edwards, T de Beer, ... Journal of medicinal chemistry 50 (24), 5903-5911, 2007 | 174 | 2007 |
An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes JS Albert, N Blomberg, AL Breeze, AJH Brown, JN Burrows, PD Edwards, ... Current Topics in Medicinal Chemistry 7 (16), 1600-1629, 2007 | 148 | 2007 |
Crystal structure of microsomal prostaglandin E2 synthase provides insight into diversity in the MAPEG superfamily T Sjögren, J Nord, M Ek, P Johansson, G Liu, S Geschwindner Proceedings of the National Academy of Sciences 110 (10), 3806-3811, 2013 | 129 | 2013 |
Single-molecule biosensors: Recent advances and applications N Akkilic, S Geschwindner, F Höök Biosensors and Bioelectronics 151, 111944, 2020 | 115 | 2020 |
Ligand binding thermodynamics in drug discovery: still a hot tip? S Geschwindner, J Ulander, P Johansson Journal of medicinal chemistry 58 (16), 6321-6335, 2015 | 113 | 2015 |
Ligand binding mechanism in steroid receptors: from conserved plasticity to differential evolutionary constraints K Edman, A Hosseini, MK Bjursell, A Aagaard, L Wissler, A Gunnarsson, ... Structure 23 (12), 2280-2290, 2015 | 108 | 2015 |
Preserved transmembrane protein mobility in polymer-supported lipid bilayers derived from cell membranes H Pace, L Simonsson Nyström, A Gunnarsson, E Eck, C Monson, ... Analytical chemistry 87 (18), 9194-9203, 2015 | 106 | 2015 |
Gremlin1 preferentially binds to bone morphogenetic protein-2 (BMP-2) and BMP-4 over BMP-7 RH Church, A Krishnakumar, A Urbanek, S Geschwindner, J Meneely, ... Biochemical Journal 466 (1), 55-68, 2015 | 96 | 2015 |
Discovery of a novel oral glucocorticoid receptor modulator (AZD9567) with improved side effect profile L Ripa, K Edman, M Dearman, G Edenro, R Hendrickx, V Ullah, ... Journal of Medicinal Chemistry 61 (5), 1785-1799, 2018 | 66 | 2018 |
Affinity-based, biophysical methods to detect and analyze ligand binding to recombinant proteins: matching high information content with high throughput GA Holdgate, M Anderson, F Edfeldt, S Geschwindner Journal of structural biology 172 (1), 142-157, 2010 | 65 | 2010 |
Molecular architecture of potassium chloride co-transporter KCC2 M Agez, P Schultz, I Medina, DJ Baker, MP Burnham, RA Cardarelli, ... Scientific reports 7 (1), 16452, 2017 | 59 | 2017 |
Application of optical biosensors in small-molecule screening activities S Geschwindner, JF Carlsson, W Knecht Sensors 12 (4), 4311-4323, 2012 | 59 | 2012 |
Crystal structure and NMR studies of the apo SH2 domains of ZAP-70: two bikes rather than a tandem RHA Folmer, S Geschwindner, Y Xue Biochemistry 41 (48), 14176-14184, 2002 | 56 | 2002 |
Role of calcium ions in the structure and function of thedi-isopropylfluorophosphatase from Loligo vulgaris J HARTLEIB, S GESCHWINDNER, EI SCHARFF, H RÜTERJANS Biochemical Journal 353 (3), 579-589, 2001 | 55 | 2001 |
Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion K Bamberg, U Johansson, K Edman, L William-Olsson, S Myhre, ... PLoS One 13 (2), e0193380, 2018 | 51 | 2018 |
Biophysical methods in drug discovery from small molecule to pharmaceutical G Holdgate, S Geschwindner, A Breeze, G Davies, N Colclough, ... Protein-Ligand Interactions: Methods and Applications, 327-355, 2013 | 51 | 2013 |
Synthesis and structure-activity relationship of 4-(1, 3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors J Malmström, J Viklund, C Slivo, A Costa, M Maudet, C Sandelin, G Hiller, ... Bioorganic & medicinal chemistry letters 22 (18), 5919-5923, 2012 | 46 | 2012 |
Agonists and antagonists of protease-activated receptor 2 discovered within a DNA-encoded chemical library using mutational stabilization of the target DG Brown, GA Brown, P Centrella, K Certel, RM Cooke, JW Cuozzo, ... SLAS DISCOVERY: Advancing the Science of Drug Discovery 23 (5), 429-436, 2018 | 43 | 2018 |