Search Results - "Chang, Sichen" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

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

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

by 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.
Published in Bioorganic & medicinal chemistry letters (15.01.2017)

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Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

by Felts, Andrew S, Rodriguez, Alice L, Smith, Katrina A, Engers, Julie L, Morrison, Ryan D, Byers, Frank W, Blobaum, Anna L, Locuson, Charles W, Chang, Sichen, Venable, Daryl F, Niswender, Colleen M, Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W, Emmitte, Kyle A
Published in Journal of medicinal chemistry (25.11.2015)

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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

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

by 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.
Published in Bioorganic & medicinal chemistry letters (01.07.2017)

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Design and Synthesis of N‑Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

Design and Synthesis of N‑Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

by Engers, Julie L, Bollinger, Katrina A, Weiner, Rebecca L, Rodriguez, Alice L, Long, Madeline F, Breiner, Megan M, Chang, Sichen, Bollinger, Sean R, Bubser, Michael, Jones, Carrie K, Morrison, Ryan D, Bridges, Thomas M, Blobaum, Anna L, Niswender, Colleen M, Conn, P. Jeffrey, Emmitte, Kyle A, Lindsley, Craig W
Published in ACS medicinal chemistry letters (14.09.2017)

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

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

by 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., Woodf, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (01.07.2016)

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Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

by Wood, Michael R., Noetzel, Meredith J., Melancon, Bruce J., Poslusney, Michael S., Nance, Kellie D., Hurtado, Miguel A., Luscombe, Vincent B., Weiner, Rebecca L., Rodriguez, Alice L., Lamsal, Atin, Chang, Sichen, Bubser, Michael, Blobaum, Anna L., Engers, Darren W., Niswender, Colleen M., Jones, Carrie K., Brandon, Nicholas J., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Published in ACS medicinal chemistry letters (09.02.2017)

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Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists

by Capstick, Rory A., Whomble, David, Orsi, Douglas L., Felts, Andrew S., Rodriguez, Alice L., Vinson, Paige N., Chang, Sichen, Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Jones, Carrie K., Lindsley, Craig W., Han, Changho
Published in Bioorganic & medicinal chemistry letters (15.11.2022)

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Development of Potent and Selective Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 2 for the Potential Treatment of Alzheimer’s Disease

Development of Potent and Selective Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 2 for the Potential Treatment of Alzheimer’s Disease

by Coleman, Jeremy S, Capstick, Rory A, Rathnayake, Upendra A, Parr, Lauren, Chang, Sichen, Thompson, Analisa D, Qi, Aidong, Niswender, Colleen M, Boutaud, Olivier, Plumley, Hyekyung, Jones, Carrie K, Engers, Darren, Lindsley, Craig W
Published in Alzheimer's & dementia (01.12.2023)

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Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M5 Muscarinic Acetylcholine Receptor

Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M5 Muscarinic Acetylcholine Receptor

by Li, Jinming, Orsi, Douglas L., Engers, Julie L., Long, Madeline F., Capstick, Rory A., Maurer, Mallory A., Presley, Christopher C., Vinson, Paige N., Rodriguez, Alice L., Han, Allie, Cho, Hyekyung P., Chang, Sichen, Jackson, Megan, Bubser, Michael, Blobaum, Anna L., Boutaud, Olivier, Nader, Michael A., Niswender, Colleen M., Conn, P. Jeffrey, Jones, Carrie K., Lindsley, Craig W., Han, Changho
Published in Journal of medicinal chemistry (22.08.2024)

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Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M 5 Muscarinic Acetylcholine Receptor

Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M 5 Muscarinic Acetylcholine Receptor

by Li, Jinming, Orsi, Douglas L, Engers, Julie L, Long, Madeline F, Capstick, Rory A, Maurer, Mallory A, Presley, Christopher C, Vinson, Paige N, Rodriguez, Alice L, Han, Allie, Cho, Hyekyung P, Chang, Sichen, Jackson, Megan, Bubser, Michael, Blobaum, Anna L, Boutaud, Olivier, Nader, Michael A, Niswender, Colleen M, Conn, P Jeffrey, Jones, Carrie K, Lindsley, Craig W, Han, Changho
Published in Journal of medicinal chemistry (22.08.2024)

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Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS

Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS

by Dodd, Cayden J., Chronister, Keagan S., Rathnayake, Upendra, Parr, Lauren C., Li, Kangjun, Chang, Sichen, Mi, Dehui, Days, Emily L., Bauer, Joshua A., Cho, Hyekyung P., Boutaud, Olivier, Denton, Jerod S., Lindsley, Craig W., Han, Changho
Published in Bioorganic & medicinal chemistry letters (01.05.2023)

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Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro

Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro

by Reed, Carson W., Rodriguez, Alice L., Kalbfleisch, Jacob J., Seto, Mabel, Jenkins, Matthew T., Blobaum, Anna L., Chang, Sichen, Lindsley, Craig W., Niswender, Colleen M.
Published in Bioorganic & medicinal chemistry letters (15.10.2022)

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Discovery of a potent M5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists

by Orsi, Douglas L., Felts, Andrew S., Rodriguez, Alice L., Vinson, Paige N., Cho, Hyekyung P., Chang, Sichen, Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Jones, Carrie K., Lindsley, Craig W., Han, Changho
Published in Bioorganic & medicinal chemistry letters (15.12.2022)

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Discovery of a novel 3,4-dimethylcinnoline carboxamide M-4 positive allosteric modulator (PAM) chemotype via scaffold hopping

Discovery of a novel 3,4-dimethylcinnoline carboxamide M-4 positive allosteric modulator (PAM) chemotype via scaffold hopping

by Temple, Kayla J., Engers, Julie L., Long, Madeline F., Gregro, Alison R., Watson, Katherine J., Chang, Sichen, Jenkins, Matthew T., Luscombe, Vincent B., Rodriguez, Alice L., Niswender, Colleen M., Bridges, Thomas M., Conn, P. Jeffrey, Engers, Darren W., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (01.11.2019)

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Evaluation of 1,2,3‐Triazoles as Amide Bioisosteres In Cystic Fibrosis Transmembrane Conductance Regulator Modulators VX‐770 and VX‐809

Evaluation of 1,2,3‐Triazoles as Amide Bioisosteres In Cystic Fibrosis Transmembrane Conductance Regulator Modulators VX‐770 and VX‐809

by Doiron, Jake E., Le, Christina A., Ody, Britton K., Brace, Jonathon B., Post, Savannah J., Thacker, Nathan L., Hill, Harrison M., Breton, Gary W., Mulder, Matthew J., Chang, Sichen, Bridges, Thomas M., Tang, Liping, Wang, Wei, Rowe, Steven M., Aller, Stephen G., Turlington, Mark
Published in Chemistry : a European journal (07.03.2019)

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Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

by Engers, Julie L, Rodriguez, Alice L, Konkol, Leah C, Morrison, Ryan D, Thompson, Analisa D, Byers, Frank W, Blobaum, Anna L, Chang, Sichen, Venable, Daryl F, Loch, Matthew T, Niswender, Colleen M, Daniels, J. Scott, Jones, Carrie K, Conn, P. Jeffrey, Lindsley, Craig W, Emmitte, Kyle A
Published in Journal of medicinal chemistry (24.09.2015)

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Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder

by Garrison, Aaron T, Orsi, Douglas L, Capstick, Rory A, Whomble, David, Li, Jinming, Carter, Trever R, Felts, Andrew S, Vinson, Paige N, Rodriguez, Alice L, Han, Allie, Hajari, Krishma, Cho, Hyekyung P, Teal, Laura B, Ragland, Madeline G, Ghamari-Langroudi, Masoud, Bubser, Michael, Chang, Sichen, Schnetz-Boutaud, Nathalie C, Boutaud, Olivier, Blobaum, Anna L, Foster, Daniel J, Niswender, Colleen M, Conn, P. Jeffrey, Lindsley, Craig W, Jones, Carrie K, Han, Changho
Published in Journal of medicinal chemistry (28.04.2022)

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Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M4 muscarinic acetylcholine receptor

Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M4 muscarinic acetylcholine receptor

by Bender, Aaron M., Carter, Trever R., Spock, Matthew, Rodriguez, Alice L., Dickerson, Jonathan W., Rook, Jerri M., Chang, Sichen, Qi, Aidong, Presley, Christopher C., Engers, Darren W., Harp, Joel M., Bridges, Thomas M., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.01.2022)

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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

by Davis, Dexter C., Bungard, Joseph D., Chang, Sichen, Rodriguez, Alice L., Blobaum, Annie L., Boutaud, Olivier, Melancon, Bruce J., Niswender, Colleen M., Jeffrey Conn, P., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.01.2021)

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Lead optimization of the VU0486321 series of mGlu 1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

Lead optimization of the VU0486321 series of mGlu 1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

by Davis, Dexter C., Bungard, Joseph D., Chang, Sichen, Rodriguez, Alice L., Blobaum, Annie L., Boutaud, Olivier, Melancon, Bruce J., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.01.2021)

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