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 | 113 | 2017 |
A drug of such damned nature. 1 challenges and opportunities in translational platinum drug research: miniperspective DM Cheff, MD Hall Journal of Medicinal Chemistry 60 (11), 4517-4532, 2017 | 103 | 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 | 84 | 2017 |
Resistance to epigenetic-targeted therapy engenders tumor cell vulnerabilities associated with enhancer remodeling AB Iniguez, G Alexe, EJ Wang, G Roti, S Patel, L Chen, S Kitara, ... Cancer Cell 34 (6), 922-938. e7, 2018 | 82 | 2018 |
Discovery of orally bioavailable, quinoline-based aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with potent cellular activity SM Yang, NJ Martinez, A Yasgar, C Danchik, C Johansson, Y Wang, ... Journal of medicinal chemistry 61 (11), 4883-4903, 2018 | 78 | 2018 |
The ferroptosis inducing compounds RSL3 and ML162 are not direct inhibitors of GPX4 but of TXNRD1 DM Cheff, C Huang, KC Scholzen, R Gencheva, MH Ronzetti, Q Cheng, ... Redox Biology 62, 102703, 2023 | 58 | 2023 |
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 | 54 | 2018 |
Canvass: A crowd-sourced, natural-product screening library for exploring biological space SE Kearney, G Zahoránszky-Kőhalmi, KR Brimacombe, MJ Henderson, ... ACS central science 4 (12), 1727-1741, 2018 | 38 | 2018 |
Pyrazole-based lactate dehydrogenase inhibitors with optimized cell activity and pharmacokinetic properties G Rai, DJ Urban, BT Mott, X Hu, SM Yang, GA Benavides, MS Johnson, ... Journal of medicinal chemistry 63 (19), 10984-11011, 2020 | 36 | 2020 |
Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors JM Rohde, KR Brimacombe, L Liu, ME Pacold, A Yasgar, DM Cheff, ... Bioorganic & medicinal chemistry 26 (8), 1727-1739, 2018 | 30 | 2018 |
Selective cellular probes for mammalian thioredoxin reductase TrxR1: rational design of RX1, a modular 1, 2-thiaselenane redox probe L Zeisel, JG Felber, KC Scholzen, L Poczka, D Cheff, MS Maier, Q Cheng, ... Chem 8 (5), 1493-1517, 2022 | 26 | 2022 |
Predictive models for estimating cytotoxicity on the basis of chemical structures H Sun, Y Wang, DM Cheff, MD Hall, M Shen Bioorganic & medicinal chemistry 28 (10), 115422, 2020 | 24 | 2020 |
Development of therapies for rare genetic disorders of GPX4: roadmap and opportunities DM Cheff, AR Muotri, BR Stockwell, EE Schmidt, Q Ran, RV Kartha, ... Orphanet Journal of Rare Diseases 16, 1-15, 2021 | 16 | 2021 |
Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer JM Rohde, S Karavadhi, R Pragani, L Liu, Y Fang, W Zhang, A McIver, ... Journal of medicinal chemistry 64 (8), 4913-4946, 2021 | 16 | 2021 |
Cytotoxic profiling of annotated and diverse chemical libraries using quantitative high-throughput screening OW Lee, S Austin, M Gamma, DM Cheff, TD Lee, KM Wilson, J Johnson, ... SLAS DISCOVERY: Advancing Life Sciences R&D 25 (1), 9-20, 2020 | 14 | 2020 |
Development of an assay pipeline for the discovery of novel small molecule inhibitors of human glutathione peroxidases GPX1 and GPX4 DM Cheff, Q Cheng, H Guo, J Travers, C Klumpp-Thomas, M Shen, ... Redox Biology 63, 102719, 2023 | 11 | 2023 |
Selective Cellular Probes for Mammalian Thioredoxin Reductase TrxR1: Rational Design of RX1, a Modular 1, 2-Thiaselenane Redox Probe. Chem 2022, 8(5), 1493–1517 L Zeisel, JG Felber, KC Scholzen, L Poczka, D Cheff, MS Maier, Q Cheng, ... J. CHEMPR 10, 2022 | 6 | 2022 |
Keeping it clean: the cell culture quality control experience at the National Center for Advancing Translational Sciences JS Roth, TD Lee, DM Cheff, ML Gosztyla, RR Asawa, C Danchik, ... SLAS DISCOVERY: Advancing the Science of Drug Discovery 25 (5), 491-497, 2020 | 5 | 2020 |
Small molecule inhibitors of the human histone lysine methyltransferase NSD2/WHSC1/MMSET identified from a quantitative High-Throughput screen with nucleosome substrate NP Coussens, SC Kales, MJ Henderson, OW Lee, KY Horiuchi, Y Wang, ... bioRxiv, 208439, 2017 | 4 | 2017 |
Correction to A Drug of Such Damned Nature. Challenges and Opportunities in Translational Platinum Drug Research DM Cheff, MD Hall Journal of Medicinal Chemistry 61 (19), 8944-8944, 2018 | 3 | 2018 |