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

Discovery of VU0467319: an M(1) Positive Allosteric Modulator Candidate That Advanced into Clinical Trials

VU0467319 的发现:一种进入临床试验的 M(1) 正向变构调节剂候选药物

Poslunsey, Michael S; Wood, Michael R; Han, Changho; Stauffer, Shaun R; Panarese, Joseph D; Melancon, Bruce J; Engers, Julie L; Dickerson, Jonathan W; Peng, Weimin; Noetzel, Meredith J; Cho, Hyekyung P; Rodriguez, Alice L; Hopkins, Corey R; Morrison, Ryan; Crouch, Rachel D; Bridges, Thomas M; Blobaum, Anna L; Boutaud, Olivier; Daniels, J Scott; Kates, Michael J; Castelhano, Arlindo; Rook, Jerri M; Niswender, Colleen M; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig 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

In Vitro to in Vivo Translation of Allosteric Modulator Concentration-Effect Relationships: Implications for Drug Discovery

变构调节剂浓度-效应关系从体外到体内的转化:对药物发现的启示

Gregory, Karen J; Bridges, Thomas M; Gogliotti, Rocco G; Stauffer, Shaun R; Noetzel, Meredith J; Jones, Carrie K; Lindsley, Craig W; Conn, P Jeffrey; Niswender, Colleen M

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

Optimization of M(4) positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

M(4)正向变构调节剂(PAM)的优化:VU0476406的发现,一种用于转化药理学的非人灵长类动物体内工具化合物

Melancon, Bruce J; Wood, Michael R; Noetzel, Meredith J; Nance, Kellie D; Engelberg, Eileen M; Han, Changho; Lamsal, Atin; Chang, Sichen; Cho, Hyekyung P; Byers, Frank W; Bubser, Michael; Jones, Carrie K; Niswender, Colleen M; Wood, Michael W; Engers, Darren W; Wu, Dedong; 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