1. Wellaway CR, Amans D, Bamborough P, Barnett H, Bit RA, Brown JA, Carlson NR, Chung CW, Cooper AWJ, Craggs PD, Davis RP, Dean TW, Evans JP, Gordon L, Harada IL, Hirst DJ, Humphreys PG, Jones KL, Lewis AJ, Lindon MJ, Lugo D, Mahmood M, McCleary S, Medeiros P, Mitchell DJ, O'Sullivan M, Le Gall A, Patel VK, Patten C, Poole DL, Shah RR, Smith JE, Stafford KAJ, Thomas PJ, Vimal M, Wall ID, Watson RJ, Wellaway N, Yao G, Prinjha RK.. (2020) Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening., 63 (2): [PMID:31904959] [10.1021/acs.jmedchem.9b01670] |
2. Filippakopoulos, Panagis P and 24 more authors. 2010-12-23 Selective inhibition of BET bromodomains. [PMID:20871596] |
3. Chung, Chun-Wa CW and 29 more authors. 2011-06-09 Discovery and characterization of small molecule inhibitors of the BET family bromodomains. [PMID:21568322] |
4. Hewings, David S and 11 more authors. 2011-10-13 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. [PMID:21851057] |
5. Dawson, Mark A and 26 more authors. 2011-10-02 Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. [PMID:21964340] |
6. Devaiah, Ballachanda N BN and 8 more authors. 2012-05-01 BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. [PMID:22509028] |
7. Zhang, Guangtao G and 13 more authors. 2012-08-17 Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. [PMID:22645123] |
8. Fish, Paul V and 18 more authors. 2012-11-26 Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. [PMID:23095041] |
9. Hewings, David S and 16 more authors. 2013-04-25 Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. [PMID:23517011] |
10. Mirguet, Olivier O and 23 more authors. 2013-10-10 Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. [PMID:24015967] |
11. Vidler, Lewis R LR and 9 more authors. 2013-10-24 Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening. [PMID:24090311] |
12. Zhang, Guangtao and 9 more authors. 2013-11-27 Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. [PMID:24144283] |
13. Fedorov, Oleg and 14 more authors. 2014-01-23 [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. [PMID:24313754] |
14. McLure, Kevin G KG and 14 more authors. 2013 RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. [PMID:24391744] |
15. Ciceri, Pietro and 14 more authors. 2014-04 Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. [PMID:24584101] |
16. Shortt, Jake J and 20 more authors. 2014-05-22 The drug vehicle and solvent N-methylpyrrolidone is an immunomodulator and antimyeloma compound. [PMID:24813887] |
17. Gosmini, Romain R and 23 more authors. 2014-10-09 The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. [PMID:25249180] |
18. McKeown, Michael R and 14 more authors. 2014-11-13 Biased multicomponent reactions to develop novel bromodomain inhibitors. [PMID:25314271] |
19. Noguchi-Yachide, Tomomi T, Sakai, Taki T, Hashimoto, Yuichi Y and Yamaguchi, Takao T. 2015-03-01 Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors. [PMID:25678016] |
20. Picaud, Sarah and 9 more authors. 2015-03-26 9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain. [PMID:25703523] |
21. Theodoulou, Natalie H NH and 20 more authors. 2016-02-25 Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. [PMID:25856009] |
22. Ran, Xu X and 9 more authors. 2015-06-25 Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. [PMID:26080064] |
23. Demont, Emmanuel H EH and 22 more authors. 2015-07-23 Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors. [PMID:26155854] |
24. Baud, Matthias G J; Lin-Shiao, Enrique; Zengerle, Michael; Tallant, Cynthia and Ciulli, Alessio. 2016-02-25 New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition. [PMID:26367539] |
25. Romero, F Anthony FA and 5 more authors. 2016-02-25 Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. [PMID:26572217] |
26. Hay, Duncan and 11 more authors. 2013-01-01 The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains. [PMID:26682033] |
27. Hügle, Martin M and 8 more authors. 2016-02-25 4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1). [PMID:26731611] |
28. Taylor, Alexander M AM and 22 more authors. 2016-02-11 Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains. [PMID:26985289] |
29. Li, Jie J and 8 more authors. 2016-10-04 Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. [PMID:27266999] |
30. Crawford, Terry D TD and 44 more authors. 2016-12-08 Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. [PMID:27682507] |
31. Picaud, Sarah and 22 more authors. 2016-10 Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. [PMID:27757418] |
32. Liu, Zhiqing and 6 more authors. 2017-06-08 Drug Discovery Targeting Bromodomain-Containing Protein 4. [PMID:28195723] |
33. Hasvold, Lisa A LA and 27 more authors. 2017-05-15 Methylpyrrole inhibitors of BET bromodomains. [PMID:28268136] |
34. Zhou, Bing and 14 more authors. 2018-01-25 Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. [PMID:28339196] |
35. Sun, Zhongya Z and 10 more authors. 2017-05-01 Discovery of novel BRD4 inhibitors by high-throughput screening, crystallography, and cell-based assays. [PMID:28347667] |
36. Zhao, Yujun Y and 15 more authors. 2017-05-11 Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. [PMID:28463487] |
37. Ayoub, Alex M AM and 16 more authors. 2017-06-22 BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. [PMID:28535045] |
38. Chan, Kwok-Ho; Zengerle, Michael; Testa, Andrea and Ciulli, Alessio. 2018-01-25 Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. [PMID:28595007] |
39. Shao, Mingfeng M and 10 more authors. 2017-09-01 Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. [PMID:28765013] |
40. Ali, Imran I, Lee, Jooyun J, Go, Areum A, Choi, Gildon G and Lee, Kwangho K. 2017-10-15 Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment. [PMID:28939121] |
41. Moustakim, Moses; Clark, Peter G K; Hay, Duncan A; Dixon, Darren J and Brennan, Paul E. 2016-12-07 Chemical probes and inhibitors of bromodomains outside the BET family. [PMID:29170712] |
42. Ouyang, Liang L and 9 more authors. 2017-12-28 Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. [PMID:29172540] |
43. Xiang, Qiuping Q and 14 more authors. 2018-03-08 Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. [PMID:29541371] |
44. Zhang, Maofeng M and 18 more authors. 2018-04-12 Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC). [PMID:29566488] |
45. Liu, Zhiqing and 5 more authors. 2018-05-10 Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation. [PMID:29649741] |
46. Law, Robert P RP and 9 more authors. 2018-05-24 Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. [PMID:29656650] |
47. Feng, Yuxin Y and 7 more authors. 2018-05-25 Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors. [PMID:29730189] |
48. Xue, Xiaoqian X and 16 more authors. 2018-05-25 Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer. [PMID:29758518] |
49. Jennings, Laura E LE and 22 more authors. 2018-07-15 BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. [PMID:29776834] |
50. Zhao, Yujun Y and 19 more authors. 2018-07-26 Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor. [PMID:30015487] |
51. Qin, Chong and 23 more authors. 2018-08-09 Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. [PMID:30019901] |
52. Liu, Shuai and 13 more authors. 2018-09-13 Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. [PMID:30125504] |
53. Wiedemann, Bianca B, Weisner, Jörn J and Rauh, Daniel D. 2018-08-01 Chemical modulation of transcription factors. [PMID:30151079] |
54. Divakaran, Anand A and 12 more authors. 2018-10-25 Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. [PMID:30253095] |
55. Xing, Jing J and 13 more authors. 2019-02-01 Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors. [PMID:30529546] |
56. Duan, Yingchao Y and 5 more authors. 2018-11-01 Targeting Brd4 for cancer therapy: inhibitors and degraders. [PMID:30542529] |
57. Watts, Ellen E and 8 more authors. 2019-03-14 Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity. [PMID:30789735] |
58. Yang, Shyh-Ming SM and 7 more authors. 2019-05-15 Lead optimization and efficacy evaluation of quinazoline-based BET family inhibitors for potential treatment of cancer and inflammatory diseases. [PMID:30905542] |
59. Rong, Juan and 10 more authors. 2019-10-01 Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors. [PMID:31421967] |
60. Carlson, Angela S and 6 more authors. 2019-09-12 Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors. [PMID:31531200] |
61. Jiang, Fei and 9 more authors. 2020-01-01 Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. [PMID:31767403] |
62. Jiang, Fei and 16 more authors. 2019-12-26 Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis. [PMID:31789032] |
63. Yang, Yifei and 5 more authors. 2019-12-12 Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-a]pyrazin-8(7H)-one as Novel BRD4 Inhibitors. [PMID:31857846] |
64. Pan, Zhaoping and 9 more authors. 2020-04-09 Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells. [PMID:32153186] |
65. Li, Yangfeng and 11 more authors. 2020-07-09 Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. [PMID:32453591] |
66. Ghazy, Ehab and 12 more authors. 2020-08-15 Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. [PMID:32497960] |
67. Ferguson, Fleur M and 11 more authors. 2020-07-23 Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one Scaffold. [PMID:32530623] |
68. Xu, Yu and 6 more authors. 2020-12-15 Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. [PMID:32883643] |
69. He, Zhang-Xu and 5 more authors. 2021-01-01 Current development of CBP/p300 inhibitors in the last decade. [PMID:33045661] |
70. Yang, Yifei and 6 more authors. 2021-01-01 Design, synthesis and biological evaluation of imidazolopyridone derivatives as novel BRD4 inhibitors. [PMID:33191086] |
71. Yang, Yifei; Fang, Lincheng; Chen, Pan; Zhang, Huibin and Zhou, Jinpei. 2020-11-12 Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer. [PMID:33214826] |
72. Hügle, Martin and 10 more authors. 2020-12-24 4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines. [PMID:33275431] |
73. Sato, Masanori; Kondo, Takekazu; Kohno, Yasushi and Seto, Shigeki. 2021-03-15 Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model. [PMID:33549905] |