A potent and selective small-molecule degrader of STAT3 achieves complete tumor regression in vivo L Bai, H Zhou, R Xu, Y Zhao, K Chinnaswamy, D McEachern, J Chen, ... Cancer cell 36 (5), 498-511. e17, 2019 | 422 | 2019 |
Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer X Han, C Wang, C Qin, W Xiang, E Fernandez-Salas, CY Yang, M Wang, ... Journal of medicinal chemistry 62 (2), 941-964, 2019 | 326 | 2019 |
Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER) J Hu, B Hu, M Wang, F Xu, B Miao, CY Yang, M Wang, Z Liu, DF Hayes, ... Journal of medicinal chemistry 62 (3), 1420-1442, 2019 | 223 | 2019 |
Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands X Han, L Zhao, W Xiang, C Qin, B Miao, T Xu, M Wang, CY Yang, ... Journal of medicinal chemistry 62 (24), 11218-11231, 2019 | 169 | 2019 |
Structure-based discovery of SD-36 as a potent, selective, and efficacious PROTAC degrader of STAT3 protein H Zhou, L Bai, R Xu, Y Zhao, J Chen, D McEachern, K Chinnaswamy, ... Journal of medicinal chemistry 62 (24), 11280-11300, 2019 | 154 | 2019 |
CSAR data set release 2012: ligands, affinities, complexes, and docking decoys JB Dunbar Jr, RD Smith, KL Damm-Ganamet, A Ahmed, EX Esposito, ... Journal of chemical information and modeling 53 (8), 1842-1852, 2013 | 121 | 2013 |
Structure-based design of γ-carboline analogues as potent and specific BET bromodomain inhibitors X Ran, Y Zhao, L Liu, L Bai, CY Yang, B Zhou, JL Meagher, ... Journal of medicinal chemistry 58 (12), 4927-4939, 2015 | 111 | 2015 |
A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation H Zhou, J Lu, L Liu, D Bernard, CY Yang, E Fernandez-Salas, ... Nature communications 8 (1), 1150, 2017 | 83 | 2017 |
Design of the first‐in‐class, highly potent irreversible inhibitor targeting the menin‐MLL protein–protein interaction S Xu, A Aguilar, T Xu, K Zheng, L Huang, J Stuckey, K Chinnaswamy, ... Angewandte Chemie 130 (6), 1617-1621, 2018 | 59 | 2018 |
CSAR benchmark exercise 2013: evaluation of results from a combined computational protein design, docking, and scoring/ranking challenge RD Smith, KL Damm-Ganamet, JB Dunbar Jr, A Ahmed, K Chinnaswamy, ... Journal of chemical information and modeling 56 (6), 1022-1031, 2016 | 58 | 2016 |
High-affinity peptidomimetic inhibitors of the DCN1-UBC12 protein–protein interaction H Zhou, W Zhou, B Zhou, L Liu, TR Chern, K Chinnaswamy, J Lu, ... Journal of Medicinal Chemistry 61 (5), 1934-1950, 2018 | 54 | 2018 |
Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor K Ramkumar, S Samanta, A Kyani, S Yang, S Tamura, E Ziemke, ... Nature communications 7 (1), 1-13, 2016 | 53 | 2016 |
From proteomics to discovery of first-in-class ST2 inhibitors active in vivo AM Ramadan, E Daguindau, JC Rech, K Chinnaswamy, J Zhang, ... JCI insight 3 (14), 2018 | 33 | 2018 |
SD-91 as a potent and selective STAT3 degrader capable of achieving complete and long-lasting tumor regression H Zhou, L Bai, R Xu, D McEachern, K Chinnaswamy, R Li, B Wen, ... ACS Medicinal Chemistry Letters 12 (6), 996-1004, 2021 | 27 | 2021 |
EEDi-5285: An exceptionally potent, efficacious, and orally active small-molecule inhibitor of embryonic ectoderm development RK Rej, C Wang, J Lu, M Wang, E Petrunak, KP Zawacki, D McEachern, ... Journal of medicinal chemistry 63 (13), 7252-7267, 2020 | 27 | 2020 |
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin–MLL Interaction with Strong In Vivo Antitumor Activity S Xu, A Aguilar, L Huang, T Xu, K Zheng, D McEachern, S Przybranowski, ... Journal of medicinal chemistry 63 (9), 4997-5010, 2020 | 26 | 2020 |
Discovery and characterization of 2, 5-substituted benzoic acid dual inhibitors of the anti-apoptotic Mcl-1 and Bfl-1 proteins KJ Kump, L Miao, ASA Mady, NH Ansari, UK Shrestha, Y Yang, M Pal, ... Journal of medicinal chemistry 63 (5), 2489-2510, 2020 | 26 | 2020 |
Structure-based discovery of M-89 as a highly potent inhibitor of the menin-mixed lineage leukemia (Menin-MLL) protein–protein interaction A Aguilar, K Zheng, T Xu, S Xu, L Huang, E Fernandez-Salas, L Liu, ... Journal of medicinal chemistry 62 (13), 6015-6034, 2019 | 24 | 2019 |
Buried hydrogen bond interactions contribute to the high potency of complement factor D inhibitors CY Yang, JG Phillips, JA Stuckey, L Bai, H Sun, J Delproposto, WC Brown, ... ACS Medicinal Chemistry Letters 7 (12), 1092-1096, 2016 | 22 | 2016 |
Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity H Zhou, J Lu, K Chinnaswamy, JA Stuckey, L Liu, D McEachern, CY Yang, ... Nature Communications 12 (1), 2621, 2021 | 18 | 2021 |