The promise and peril of chemical probes CH Arrowsmith, JE Audia, C Austin, J Baell, J Bennett, J Blagg, C Bountra, ... Nature chemical biology 11 (8), 536-541, 2015 | 854 | 2015 |
Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer JS Duncan, MC Whittle, K Nakamura, AN Abell, AA Midland, ... Cell 149 (2), 307-321, 2012 | 846 | 2012 |
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells M Vedadi, D Barsyte-Lovejoy, F Liu, S Rival-Gervier, A Allali-Hassani, ... Nature chemical biology 7 (8), 566-574, 2011 | 562 | 2011 |
An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1 KD Konze, A Ma, F Li, D Barsyte-Lovejoy, T Parton, CJ MacNevin, F Liu, ... ACS chemical biology 8 (6), 1324-1334, 2013 | 489 | 2013 |
Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons HS Huang, JA Allen, AM Mabb, IF King, J Miriyala, B Taylor-Blake, ... Nature 481 (7380), 185-189, 2012 | 406 | 2012 |
Discovery of β-arrestin–biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy JA Allen, JM Yost, V Setola, X Chen, MF Sassano, M Chen, S Peterson, ... Proceedings of the National Academy of Sciences 108 (45), 18488-18493, 2011 | 387 | 2011 |
Advancing targeted protein degradation for cancer therapy B Dale, M Cheng, KS Park, HÜ Kaniskan, Y Xiong, J Jin Nature Reviews Cancer 21 (10), 638-654, 2021 | 355 | 2021 |
Inhibition of lapatinib-induced kinome reprogramming in ERBB2-positive breast cancer by targeting BET family bromodomains TJ Stuhlmiller, SM Miller, JS Zawistowski, K Nakamura, AS Beltran, ... Cell reports 11 (3), 390-404, 2015 | 340 | 2015 |
Inhibitors of protein methyltransferases and demethylases HU Kaniskan, ML Martini, J Jin Chemical reviews 118 (3), 989-1068, 2018 | 286 | 2018 |
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP F Liu, D Barsyte-Lovejoy, F Li, Y Xiong, V Korboukh, XP Huang, ... Journal of medicinal chemistry 56 (21), 8931-8942, 2013 | 278 | 2013 |
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65 XP Huang, J Karpiak, WK Kroeze, H Zhu, X Chen, SS Moy, KA Saddoris, ... Nature 527 (7579), 477-483, 2015 | 269 | 2015 |
Structure and inhibition of microbiome β-glucuronidases essential to the alleviation of cancer drug toxicity BD Wallace, AB Roberts, RM Pollet, JD Ingle, KA Biernat, SJ Pellock, ... Chemistry & biology 22 (9), 1238-1249, 2015 | 267 | 2015 |
Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys Y Nagai, N Miyakawa, H Takuwa, Y Hori, K Oyama, B Ji, M Takahashi, ... Nature neuroscience 23 (9), 1157-1167, 2020 | 263 | 2020 |
In silico design of novel probes for the atypical opioid receptor MRGPRX2 K Lansu, J Karpiak, J Liu, XP Huang, JD McCorvy, WK Kroeze, T Che, ... Nature chemical biology 13 (5), 529-536, 2017 | 263 | 2017 |
Light-induced control of protein destruction by opto-PROTAC J Liu, H Chen, L Ma, Z He, D Wang, Y Liu, Q Lin, T Zhang, N Gray, ... Science advances 6 (8), eaay5154, 2020 | 261 | 2020 |
A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases MS Eram, Y Shen, MM Szewczyk, H Wu, G Senisterra, F Li, KV Butler, ... ACS chemical biology 11 (3), 772-781, 2016 | 256 | 2016 |
Discovery of a 2, 4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a F Liu, X Chen, A Allali-Hassani, AM Quinn, GA Wasney, A Dong, ... Journal of medicinal chemistry 52 (24), 7950-7953, 2009 | 253 | 2009 |
First Chelated Chiral N-Heterocyclic Bis-Carbene Complexes DS Clyne, J Jin, E Genest, JC Gallucci, TV RajanBabu Organic Letters 2 (8), 1125-1128, 2000 | 244 | 2000 |
Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia B Xu, DM On, A Ma, T Parton, KD Konze, SG Pattenden, DF Allison, L Cai, ... Blood, The Journal of the American Society of Hematology 125 (2), 346-357, 2015 | 241 | 2015 |
Artificial intelligence and machine learning‐aided drug discovery in central nervous system diseases: State‐of‐the‐arts and future directions S Vatansever, A Schlessinger, D Wacker, HÜ Kaniskan, J Jin, MM Zhou, ... Medicinal research reviews 41 (3), 1427-1473, 2021 | 237 | 2021 |