日期 影响因子
日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:
–

Decoding BCL6 Inhibitors: Computational Insights into the Impact of Water Networks on Potency

解码 BCL6 抑制剂：水网络对效力影响的计算见解

期刊:Journal of Chemical Information and Modeling
影响因子:5.3
doi:10.1021/acs.jcim.5c01188
Hares, Daniella E; Scarpino, Andrea; Bodnarchuk, Michael S; Hoelder, Swen
BCL6
发表日期：2025
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Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

通过优化三环喹啉酮发现一种用于抑制BCL6的体内化学探针

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.3c00155
Harnden, Alice C; Davis, Owen A; Box, Gary M; Hayes, Angela; Johnson, Louise D; Henley, Alan T; de Haven Brandon, Alexis K; Valenti, Melanie; Cheung, Kwai-Ming J; Brennan, Alfie; Huckvale, Rosemary; Pierrat, Olivier A; Talbot, Rachel; Bright, Michael D; Akpinar, Hafize Aysin; Miller, Daniel S J; Tarantino, Dalia; Gowan, Sharon; de Klerk, Selby; McAndrew, Peter Craig; Le Bihan, Yann-Vaï; Meniconi, Mirco; Burke, Rosemary; Kirkin, Vladimir; van Montfort, Rob L M; Raynaud, Florence I; Rossanese, Olivia W; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2023
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Determination of Ligand-Binding Affinity (K(d)) Using Transverse Relaxation Rate (R(2)) in the Ligand-Observed (1)H NMR Experiment and Applications to Fragment-Based Drug Discovery

利用配体观测的（1）H NMR实验中的横向弛豫速率（R（2））测定配体结合亲和力（K（d））及其在基于片段的药物发现中的应用

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.3c00758
Liu, Manjuan; Mirza, Amin; McAndrew, P Craig; Thapaliya, Arjun; Pierrat, Olivier A; Stubbs, Mark; Hahner, Tamas; Chessum, Nicola E A; Innocenti, Paolo; Caldwell, John; Cheeseman, Matthew D; Bellenie, Benjamin R; van Montfort, Rob L M; Newton, Gary K; Burke, Rosemary; Collins, Ian; Hoelder, Swen
发表日期：2023
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Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

优化形状互补性有助于发现高效的三环BCL6抑制剂

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.1c02174
Davis, Owen A; Cheung, Kwai-Ming J; Brennan, Alfie; Lloyd, Matthew G; Rodrigues, Matthew J; Pierrat, Olivier A; Collie, Gavin W; Le Bihan, Yann-Vaï; Huckvale, Rosemary; Harnden, Alice C; Varela, Ana; Bright, Michael D; Eve, Paul; Hayes, Angela; Henley, Alan T; Carter, Michael D; McAndrew, P Craig; Talbot, Rachel; Burke, Rosemary; van Montfort, Rob L M; Raynaud, Florence I; Rossanese, Olivia W; Meniconi, Mirco; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2022
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Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

提高结合亲和力和药代动力学可实现体内BCL6的持续降解

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.1c02175
Huckvale, Rosemary; Harnden, Alice C; Cheung, Kwai-Ming J; Pierrat, Olivier A; Talbot, Rachel; Box, Gary M; Henley, Alan T; de Haven Brandon, Alexis K; Hallsworth, Albert E; Bright, Michael D; Akpinar, Hafize Aysin; Miller, Daniel S J; Tarantino, Dalia; Gowan, Sharon; Hayes, Angela; Gunnell, Emma A; Brennan, Alfie; Davis, Owen A; Johnson, Louise D; de Klerk, Selby; McAndrew, Craig; Le Bihan, Yann-Vaï; Meniconi, Mirco; Burke, Rosemary; Kirkin, Vladimir; van Montfort, Rob L M; Raynaud, Florence I; Rossanese, Olivia W; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2022
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Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

深入探索：通过向溶剂化口袋生长来优化 BCL6 抑制剂

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.1c00946
Lloyd, Matthew G; Huckvale, Rosemary; Cheung, Kwai-Ming J; Rodrigues, Matthew J; Collie, Gavin W; Pierrat, Olivier A; Gatti Iou, Mahad; Carter, Michael; Davis, Owen A; McAndrew, P Craig; Gunnell, Emma; Le Bihan, Yann-Vaï; Talbot, Rachel; Henley, Alan T; Johnson, Louise D; Hayes, Angela; Bright, Michael D; Raynaud, Florence I; Meniconi, Mirco; Burke, Rosemary; van Montfort, Rob L M; Rossanese, Olivia W; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2021
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Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N(2)-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N(8)-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722)

引入甲基可抑制吡啶并[3,4-d]嘧啶单极纺锤体1 (MPS1) 抑制剂的代谢，并促成了 1 期临床候选药物 N(2)-(2-乙氧基-4-(4-甲基-4H-1,2,4-三唑-3-基)苯基)-6-甲基-N(8)-新戊基吡啶并[3,4-d]嘧啶-2,8-二胺 (BOS172722) 的发现。

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.8b00690
Woodward, Hannah L; Innocenti, Paolo; Cheung, Kwai-Ming J; Hayes, Angela; Roberts, Jennie; Henley, Alan T; Faisal, Amir; Mak, Grace Wing-Yan; Box, Gary; Westwood, Isaac M; Cronin, Nora; Carter, Michael; Valenti, Melanie; De Haven Brandon, Alexis; O'Fee, Lisa; Saville, Harry; Schmitt, Jessica; Burke, Rosemary; Broccatelli, Fabio; van Montfort, Rob L M; Raynaud, Florence I; Eccles, Suzanne A; Linardopoulos, Spiros; Blagg, Julian; Hoelder, Swen
代谢
发表日期：2018
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Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)

基于结构的口服生物利用度高的1H-吡咯并[3,2-c]吡啶类有丝分裂激酶单极纺锤体1 (MPS1) 抑制剂设计

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/jm401395s
Naud, Sébastien; Westwood, Isaac M; Faisal, Amir; Sheldrake, Peter; Bavetsias, Vassilios; Atrash, Butrus; Cheung, Kwai-Ming J; Liu, Manjuan; Hayes, Angela; Schmitt, Jessica; Wood, Amy; Choi, Vanessa; Boxall, Kathy; Mak, Grace; Gurden, Mark; Valenti, Melanie; de Haven Brandon, Alexis; Henley, Alan; Baker, Ross; McAndrew, Craig; Matijssen, Berry; Burke, Rosemary; Hoelder, Swen; Eccles, Suzanne A; Raynaud, Florence I; Linardopoulos, Spiros; van Montfort, Rob L M; Blagg, Julian
信号转导
发表日期：2013
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Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites

溴结构域乙酰赖氨酸结合位点的成药性分析和结构分类

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/jm300346w
Vidler, Lewis R; Brown, Nathan; Knapp, Stefan; Hoelder, Swen
发表日期：2012
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Discovery of small molecule cancer drugs: successes, challenges and opportunities

小分子抗癌药物的发现：成功、挑战与机遇

期刊:Molecular Oncology
影响因子:4.5
doi:10.1016/j.molonc.2012.02.004
Hoelder, Swen; Clarke, Paul A; Workman, Paul
肿瘤
肿瘤免疫
发表日期：2012
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