| Remdesivir: a review of its discovery and development leading to emergency use authorization for treatment of COVID-19 RT Eastman, JS Roth, KR Brimacombe, A Simeonov, M Shen, S Patnaik, ... ACS central Science 6 (5), 672-683, 2020 | 1002 | 2020 |
| Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis D Anastasiou, Y Yu, WJ Israelsen, JK Jiang, MB Boxer, BS Hong, ... Nature chemical biology 8 (10), 839-847, 2012 | 809 | 2012 |
| A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate ME Pacold, KR Brimacombe, SH Chan, JM Rohde, CA Lewis, ... Nature chemical biology 12 (6), 452-458, 2016 | 504 | 2016 |
| Small molecule inhibitor of NRF2 selectively intervenes therapeutic resistance in KEAP1-deficient NSCLC tumors A Singh, S Venkannagari, KH Oh, YQ Zhang, JM Rohde, L Liu, ... ACS chemical biology 11 (11), 3214-3225, 2016 | 485 | 2016 |
| Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo FJ Najm, M Madhavan, A Zaremba, E Shick, RT Karl, DC Factor, TE Miller, ... Nature 522 (7555), 216-220, 2015 | 443 | 2015 |
| Effective transvascular delivery of nanoparticles across the blood-brain tumor barrier into malignant glioma cells H Sarin, AS Kanevsky, H Wu, KR Brimacombe, SH Fung, AA Sousa, ... Journal of translational medicine 6, 1-15, 2008 | 310 | 2008 |
| Synthesis and structure–activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein MD Hall, KR Brimacombe, MS Varonka, KM Pluchino, JK Monda, J Li, ... Journal of medicinal chemistry 54 (16), 5878-5889, 2011 | 129 | 2011 |
| Discovery and optimization of potent, cell-active pyrazole-based inhibitors of lactate dehydrogenase (LDH) G Rai, KR Brimacombe, BT Mott, DJ Urban, X Hu, SM Yang, TD Lee, ... Journal of medicinal chemistry 60 (22), 9184-9204, 2017 | 124 | 2017 |
| Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays DJ Urban, NJ Martinez, MI Davis, KR Brimacombe, DM Cheff, TD Lee, ... Scientific reports 7 (1), 12758, 2017 | 86 | 2017 |
| An OpenData portal to share COVID-19 drug repurposing data in real time KR Brimacombe, T Zhao, RT Eastman, X Hu, K Wang, M Backus, ... BioRxiv, 2020 | 81 | 2020 |
| Assay guidance manual [Internet] S Markossian, A Grossman, M Arkin, D Auld, C Austin, J Baell, ... Eli Lilly & Company and the National Center for Advancing Translational Sciences, 2004 | 81 | 2004 |
| ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model J Jiang, MJ Walsh, KR Brimacombe, D Anastasiou, Y Yu, WJ Israelsen, ... Probe Reports from the NIH Molecular Libraries Program [Internet], 2013 | 78 | 2013 |
| 2-Oxo-N-aryl-1, 2, 3, 4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase MJ Walsh, KR Brimacombe, H Veith, JM Bougie, T Daniel, W Leister, ... Bioorganic & medicinal chemistry letters 21 (21), 6322-6327, 2011 | 75 | 2011 |
| Inhibition of glutathione peroxidase mediates the collateral sensitivity of multidrug-resistant cells to tiopronin MD Hall, TS Marshall, ADT Kwit, LMM Jenkins, AE Dulcey, JP Madigan, ... Journal of Biological Chemistry 289 (31), 21473-21489, 2014 | 65 | 2014 |
| Discovery of NCT-501, a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1) SM Yang, A Yasgar, B Miller, M Lal-Nag, K Brimacombe, X Hu, H Sun, ... Journal of medicinal chemistry 58 (15), 5967-5978, 2015 | 64 | 2015 |
| High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2 NP Coussens, SC Kales, MJ Henderson, OW Lee, KY Horiuchi, Y Wang, ... Journal of Biological Chemistry 293 (35), 13750-13765, 2018 | 61 | 2018 |
| A high-content imaging-based screening pipeline for the systematic identification of anti-progeroid compounds N Kubben, KR Brimacombe, M Donegan, Z Li, T Misteli Methods 96, 46-58, 2016 | 58 | 2016 |
| A dual-fluorescence high-throughput cell line system for probing multidrug resistance KR Brimacombe, MD Hall, DS Auld, J Inglese, CP Austin, MM Gottesman, ... Assay and drug development technologies 7 (3), 233-249, 2009 | 57 | 2009 |
| Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET P Kannan, KR Brimacombe, WC Kreisl, JS Liow, SS Zoghbi, S Telu, ... Proceedings of the National Academy of Sciences 108 (6), 2593-2598, 2011 | 56 | 2011 |
| N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier P Kannan, KR Brimacombe, SS Zoghbi, JS Liow, C Morse, AK Taku, ... Drug Metabolism and Disposition 38 (6), 917-922, 2010 | 52 | 2010 |
Matthew D HallNational Center for Advancing Translational Sciences (NCATS)Verified email at mail.nih.gov