Engineered luciferase reporter from a deep sea shrimp utilizing a novel imidazopyrazinone substrate MP Hall, J Unch, BF Binkowski, MP Valley, BL Butler, MG Wood, P Otto, ... ACS chemical biology 7 (11), 1848-1857, 2012 | 1703 | 2012 |
NanoBRET A Novel BRET Platform for the Analysis of Protein–Protein Interactions T Machleidt, CC Woodroofe, MK Schwinn, J Méndez, MB Robers, ... ACS chemical biology 10 (8), 1797-1804, 2015 | 503 | 2015 |
Application of BRET to monitor ligand binding to GPCRs LA Stoddart, EKM Johnstone, AJ Wheal, J Goulding, MB Robers, ... Nature methods 12 (7), 661-663, 2015 | 285 | 2015 |
Target engagement and drug residence time can be observed in living cells with BRET MB Robers, ML Dart, CC Woodroofe, CA Zimprich, TA Kirkland, ... Nature communications 6 (1), 10091, 2015 | 269 | 2015 |
Quantitative live-cell kinetic degradation and mechanistic profiling of PROTAC mode of action KM Riching, S Mahan, CR Corona, M McDougall, JD Vasta, MB Robers, ... ACS chemical biology 13 (9), 2758-2770, 2018 | 267 | 2018 |
Quantitative, wide-spectrum kinase profiling in live cells for assessing the effect of cellular ATP on target engagement JD Vasta, CR Corona, J Wilkinson, CA Zimprich, JR Hartnett, MR Ingold, ... Cell chemical biology 25 (2), 206-214. e11, 2018 | 242 | 2018 |
Potent and selective bivalent inhibitors of BET bromodomains MJ Waring, H Chen, AA Rabow, G Walker, R Bobby, S Boiko, ... Nature chemical biology 12 (12), 1097-1104, 2016 | 148 | 2016 |
Selective JAK3 inhibitors with a covalent reversible binding mode targeting a new induced fit binding pocket M Forster, A Chaikuad, SM Bauer, J Holstein, MB Robers, CR Corona, ... Cell chemical biology 23 (11), 1335-1340, 2016 | 119 | 2016 |
Quantifying CDK inhibitor selectivity in live cells CI Wells, JD Vasta, CR Corona, J Wilkinson, CA Zimprich, MR Ingold, ... Nature communications 11 (1), 2743, 2020 | 98 | 2020 |
Discovery of a selective inhibitor of doublecortin like kinase 1 FM Ferguson, B Nabet, S Raghavan, Y Liu, AL Leggett, M Kuljanin, ... Nature chemical biology 16 (6), 635-643, 2020 | 98 | 2020 |
Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia FF Wagner, L Benajiba, AJ Campbell, M Weïwer, JR Sacher, JP Gale, ... Science translational medicine 10 (431), eaam8460, 2018 | 90 | 2018 |
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Oplophorus-derived luciferases, novel coelenterazine substrates, and methods of use B Binkowski, LP Encell, M Hall, MB Robers, MR Slater, KV Wood, ... US Patent 8,669,103, 2014 | 79 | 2014 |
Discovery of a new isoxazole-3-hydroxamate-based histone deacetylase 6 inhibitor SS-208 with antitumor activity in syngeneic melanoma mouse models S Shen, M Hadley, K Ustinova, J Pavlicek, T Knox, S Noonepalle, ... Journal of medicinal chemistry 62 (18), 8557-8577, 2019 | 77 | 2019 |
Binding kinetics survey of the drugged kinome V Georgi, F Schiele, BT Berger, A Steffen, PA Marin Zapata, H Briem, ... Journal of the American Chemical Society 140 (46), 15774-15782, 2018 | 75 | 2018 |
KRAS is vulnerable to reversible switch-II pocket engagement in cells JD Vasta, DM Peacock, Q Zheng, JA Walker, Z Zhang, CA Zimprich, ... Nature chemical biology 18 (6), 596-604, 2022 | 73 | 2022 |
Brain penetrable histone deacetylase 6 inhibitor SW-100 ameliorates memory and learning impairments in a mouse model of fragile X syndrome AP Kozikowski, S Shen, M Pardo, MT Tavares, D Szarics, V Benoy, ... ACS chemical neuroscience 10 (3), 1679-1695, 2018 | 63 | 2018 |
Real-time analysis of the binding of fluorescent VEGF165a to VEGFR2 in living cells: effect of receptor tyrosine kinase inhibitors and fate of internalized agonist-receptor … LE Kilpatrick, R Friedman-Ohana, DC Alcobia, K Riching, CJ Peach, ... Biochemical Pharmacology 136, 62-75, 2017 | 54 | 2017 |
Mutation in Abl kinase with altered drug-binding kinetics indicates a novel mechanism of imatinib resistance A Lyczek, BT Berger, AM Rangwala, YT Paung, J Tom, H Philipose, J Guo, ... Proceedings of the National Academy of Sciences 118 (46), e2111451118, 2021 | 53 | 2021 |
Homogeneous assay for target engagement utilizing bioluminescent thermal shift ML Dart, T Machleidt, E Jost, MK Schwinn, MB Robers, C Shi, TA Kirkland, ... ACS medicinal chemistry letters 9 (6), 546-551, 2018 | 53 | 2018 |