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

Discovery of Macrocyclic Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors that Demonstrate Potent Cellular Efficacy and In Vivo Activity in a Mouse Solid Tumor Xenograft Model

发现具有强效细胞活性和在小鼠实体瘤异种移植模型中体内活性的巨环髓系细胞白血病1 (Mcl-1) 抑制剂

Tarr, James C; Jeon, Kyuok; Veerasamy, Nagarathanam; Aichinger, Martin; Salovich, James M; Zhao, Bin; Sensintaffar, John L; Arnhof, Heribert; Wunberg, Tobias; Sgubin, Danielle; Arnold, Allison; Vekariya, Rakesh H; Christov, Plamen P; Kim, Kwangho; Fuchs, Julian Emanuel; Karier, Pol; Betzemeier, Bodo; Van Meveren, Mayme; Miriyala, Nagaraju; Olejniczak, Edward T; Engelhardt, Harald; Lee, Taekyu; McConnell, Darryl; Fesik, Stephen W

Clinical recommendations for polygenic risk score-enhanced breast cancer screening: Can.Heal project

基于多基因风险评分的乳腺癌筛查临床建议:Can.Heal 项目

Bubser, Michael; Bridges, Thomas M; Dencker, Ditte; Gould, Robert W; Grannan, Michael; Noetzel, Meredith J; Lamsal, Atin; Niswender, Colleen M; Daniels, J Scott; Poslusney, Michael S; Melancon, Bruce J; Tarr, James C; Byers, Frank W; Wess, Jürgen; Duggan, Mark E; Dunlop, John; Wood, Michael W; Brandon, Nicholas J; Wood, Michael R; Lindsley, Craig W; Conn, P Jeffrey; Jones, Carrie K; Taha, A; Matt McCrary, J; van Rooij, J; Lahousse, L; Paoletti, F; Pascucci, E; Vaht, M; Pastorino, R; Pezzullo, A M; Boccia, S

Fragment-based screening of programmed death ligand 1 (PD-L1)

基于片段的程序性死亡配体1(PD-L1)筛选

Perry, Evan; Mills, Jonathan J; Zhao, Bin; Wang, Feng; Sun, Qi; Christov, Plamen P; Tarr, James C; Rietz, Tyson A; Olejniczak, Edward T; Lee, Taekyu; Fesik, Stephen

Corrigendum to "Challenges in the development of an M(4) PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]

对“M(4) PAM 临床前候选药物开发中的挑战:一系列氮杂环丁烷衍生的叔酰胺的发现、构效关系和生物学表征”的更正 [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]

Tarr, James C; Wood, Michael R; Noetzel, Meredith J; Melancon, Bruce J; Lamsal, Atin; Luscombe, Vincent B; Rodriguez, Alice L; Byers, Frank W; Chang, Sichen; Cho, Hyekyung P; Engers, Darren W; Jones, Carrie K; Niswender, Colleen M; Wood, Michael W; Brandon, Nicholas J; Duggan, Mark E; Jeffrey Conn, P; Bridges, Thomas M; Lindsley, Craig W

Challenges in the development of an M(4) PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

M(4) PAM 体内工具化合物开发面临的挑战:VU0467154 的发现及其近缘类似物出乎意料的 DMPK 特征

Wood, Michael R; Noetzel, Meredith J; Poslusney, Michael S; Melancon, Bruce J; Tarr, James C; Lamsal, Atin; Chang, Sichen; Luscombe, Vincent B; Weiner, Rebecca L; Cho, Hyekyung P; Bubser, Michael; Jones, Carrie K; Niswender, Colleen M; Wood, Michael W; Engers, Darren W; Brandon, Nicholas J; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Challenges in the development of an M(4) PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

M(4) PAM 临床前候选药物开发中的挑战:一系列 3-氨基氮杂环丁烷衍生的酰胺的发现、构效关系研究和体内表征

Tarr, James C; Wood, Michael R; Noetzel, Meredith J; Bertron, Jeanette L; Weiner, Rebecca L; Rodriguez, Alice L; Lamsal, Atin; Byers, Frank W; Chang, Sichen; Cho, Hyekyung P; Jones, Carrie K; Niswender, Colleen M; Wood, Michael W; Brandon, Nicholas J; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Challenges in the development of an M(4) PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides

M(4) PAM 临床前候选药物开发中的挑战:一系列氮杂环丁烷衍生的叔酰胺的发现、构效关系和生物学表征

Tarr, James C; Wood, Michael R; Noetzel, Meredith J; Melancon, Bruce J; Lamsal, Atin; Luscombe, Vincent B; Rodriguez, Alice L; Byers, Frank W; Chang, Sichen; Cho, Hyekyung P; Engers, Darren W; Jones, Carrie K; Niswender, Colleen M; Wood, Michael W; Brandon, Nicholas J; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

基于5,6-二甲基-4-(哌啶-1-基)噻吩并[2,3-d]嘧啶核心结构,发现并优化了一系列新型高中枢神经系统渗透性的M4 PAMs。

Wood, Michael R; Noetzel, Meredith J; Engers, Julie L; Bollinger, Katrina A; Melancon, Bruce J; Tarr, James C; Han, Changho; West, Mary; Gregro, Alison R; Lamsal, Atin; Chang, Sichen; Ajmera, Sonia; Smith, Emery; Chase, Peter; Hodder, Peter S; Bubser, Michael; Jones, Carrie K; Hopkins, Corey R; Emmitte, Kyle A; Niswender, Colleen M; Wood, Michael W; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

基于非烯醇化酮核心的新型强效、中枢神经系统穿透性M4 PAMs的发现和构效关系研究:处置方面的挑战

Wood, Michael R; Noetzel, Meredith J; Tarr, James C; Rodriguez, Alice L; Lamsal, Atin; Chang, Sichen; Foster, Jarrett J; Smith, Emery; Chase, Peter; Hodder, Peter S; Engers, Darren W; Niswender, Colleen M; Brandon, Nicholas J; Wood, Michael W; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100.

选择性 M4 毒蕈碱乙酰胆碱受体正变构调节剂 VU0152100 的抗精神病药物样作用

Byun Nellie E, Grannan Michael, Bubser Michael, Barry Robert L, Thompson Analisa, Rosanelli John, Gowrishankar Raajaram, Kelm Nathaniel D, Damon Stephen, Bridges Thomas M, Melancon Bruce J, Tarr James C, Brogan John T, Avison Malcolm J, Deutch Ariel Y, Wess Jürgen, Wood Michael R, Lindsley Craig W, Gore John C, Conn P Jeffrey, Jones Carrie K