| Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity S Howard, V Berdini, JA Boulstridge, MG Carr, DM Cross, J Curry, ... Journal of medicinal chemistry 52 (2), 379-388, 2009 | 382 | 2009 |
| RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1-and RAS-driven cancers RJ Nichols, F Haderk, C Stahlhut, CJ Schulze, G Hemmati, D Wildes, ... Nature cell biology 20 (9), 1064-1073, 2018 | 321 | 2018 |
| Identification of novel p38α MAP kinase inhibitors using fragment-based lead generation AL Gill, M Frederickson, A Cleasby, SJ Woodhead, MG Carr, ... Journal of medicinal chemistry 48 (2), 414-426, 2005 | 234 | 2005 |
| 3, 4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors A Gill, M Carr, M O'Brien, P Wyatt, V Berdini US Patent App. 11/571,713, 2008 | 91 | 2008 |
| Allosteric inhibition of SHP2 stimulates antitumor immunity by transforming the immunosuppressive environment E Quintana, CJ Schulze, DR Myers, TJ Choy, K Mordec, D Wildes, ... Cancer research 80 (13), 2889-2902, 2020 | 75 | 2020 |
| Using matched molecular series as a predictive tool to optimize biological activity NM O’Boyle, J Boström, RA Sayle, A Gill Journal of Medicinal Chemistry 57 (6), 2704-2713, 2014 | 67 | 2014 |
| Automated iterative Csp3–C bond formation DJ Blair, S Chitti, M Trobe, DM Kostyra, HMS Haley, RL Hansen, ... Nature 604 (7904), 92-97, 2022 | 64 | 2022 |
| Pharmaceutical compounds V Berdini, JE Curry, NJ Gallagher, AL Gill, JF Lyons US Patent 8,399,442, 2013 | 63 | 2013 |
| Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring D Ménard, I Niculescu-Duvaz, HP Dijkstra, D Niculescu-Duvaz, ... Journal of medicinal chemistry 52 (13), 3881-3891, 2009 | 61 | 2009 |
| New lead generation strategies for protein kinase inhibitors-fragment based screening approaches A Gill Mini reviews in medicinal chemistry 4 (3), 301-311, 2004 | 53 | 2004 |
| The discovery of novel protein kinase inhibitors by using fragment‐based high‐throughput X‐ray crystallography A Gill, A Cleasby, H Jhoti Chembiochem 6 (3), 506-512, 2005 | 52 | 2005 |
| Structure Guided Lead Generation for M. tuberculosis Thymidylate Kinase (Mtb TMK): Discovery of 3-Cyanopyridone and 1,6-Naphthyridin-2-one as Potent Inhibitors M Naik, A Raichurkar, BS Bandodkar, BV Varun, S Bhat, R Kalkhambkar, ... Journal of medicinal chemistry 58 (2), 753-766, 2015 | 51 | 2015 |
| Stapled Vasoactive Intestinal Peptide (VIP) Derivatives Improve VPAC2 Agonism and Glucose-Dependent Insulin Secretion F Giordanetto, JD Revell, L Knerr, M Hostettler, A Paunovic, C Priest, ... ACS medicinal chemistry letters 4 (12), 1163-1168, 2013 | 50 | 2013 |
| Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF) D Niculescu-Duvaz, C Gaulon, HP Dijkstra, I Niculescu-Duvaz, A Zambon, ... Journal of medicinal chemistry 52 (8), 2255-2264, 2009 | 50 | 2009 |
| Kinetic efficiency: the missing metric for enhancing compound quality? GA Holdgate, AL Gill Drug discovery today 16 (21-22), 910-913, 2011 | 49 | 2011 |
| Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth BJ Lee, JA Boyer, GL Burnett, AP Thottumkara, N Tibrewal, SL Wilson, ... Nature chemical biology 17 (10), 1065-1074, 2021 | 44 | 2021 |
| Heart regeneration: opportunities and challenges for drug discovery with novel chemical and therapeutic methods or agents AT Plowright, O Engkvist, A Gill, L Knerr, QD Wang Angewandte Chemie International Edition 53 (16), 4056-4075, 2014 | 43 | 2014 |
| Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases V Berdini, MG Carr, AL Gill, S Howard, EF Navarro, G Trewartha, ... US Patent 8,110,573, 2012 | 40 | 2012 |
| 3, 4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators V Berdini, MA O'brien, MG Carr, TR Early, AL Gill, G Trewartha, ... US Patent 7,385,059, 2008 | 40 | 2008 |
| What is the most important approach in current drug discovery: doing the right things or doing things right? T Elebring, A Gill, AT Plowright Drug discovery today 17 (21-22), 1166-1169, 2012 | 32 | 2012 |
