Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships
Gregory, Karen J, Noetzel, Meredith J, Rook, Jerri M, Vinson, Paige N, Stauffer, Shaun R, Rodriguez, Alice L, Emmitte, Kyle A, Zhou, Ya, Chun, Aspen C, Felts, Andrew S, Chauder, Brian A, Lindsley, Craig W, Niswender, Colleen M, Conn, P Jeffrey
Published in Molecular pharmacology (01.11.2012)
Published in Molecular pharmacology (01.11.2012)
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Preparation of H,(4) PyrrolidineQuin-BAM (PBAM)
Davis, Tyler A, Dobish, Mark C, Schwieter, Kenneth E, Chun, Aspen C, Johnston, Jeffrey N
Published in Organic syntheses (2012)
Published in Organic syntheses (2012)
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Discovery of N-(benzo[1,2,3]triazol-1-yl)-N-(benzyl)acetamido)phenyl) carboxamides as severe acute respiratory syndrome coronavirus (SARS-CoV) 3CLpro inhibitors: Identification of ML300 and noncovalent nanomolar inhibitors with an induced-fit binding
Turlington, Mark, Chun, Aspen, Tomar, Sakshi, Eggler, Aimee, Grum-Tokars, Valerie, Jacobs, Jon, Daniels, J. Scott, Dawson, Eric, Saldanha, Adrian, Chase, Peter, Baez-Santos, Yahira M., Lindsley, Craig W., Hodder, Peter, Mesecar, Andrew D., Stauffer, Shaun R.
Published in Bioorganic & medicinal chemistry letters (15.11.2013)
Published in Bioorganic & medicinal chemistry letters (15.11.2013)
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The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu(4) PAM development candidate
Panarese, Joseph D., Engers, Darren W., Wu, Yong-Jin, Guernon, Jason M., Chun, Aspen, Gregro, Alison R., Bender, Aaron M., Capstick, Rory A., Wieting, Joshua M., Bronson, Joanne J., Macor, John E., Westphal, Ryan, Soars, Matthew, Engers, Julie E., Felts, Andrew S., Rodriguez, Alice L., Emmitte, Kyle A., Jones, Carrie K., Blobaum, Anna L., Conn, P. Jeffrey, Niswender, Colleen M., Hopkins, Corey R., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.01.2019)
Published in Bioorganic & medicinal chemistry letters (15.01.2019)
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Discovery of VU2957 (Valiglurax): An mGlu(4) Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease
Panarese, Joseph D., Engers, Darren W., Wu, Yong-Jin, Bronson, Joanne J., Macor, John E., Chun, Aspen, Rodriguez, Alice L., Felts, Andrew S., Engers, Julie L., Loch, Matthew T., Emmitte, Kyle A., Castelhano, Arlindo L., Kates, Michael J., Nader, Michael A., Jones, Carrie K., Blobaurn, Anna L., Conn, P. Jeffrey, Niswender, Colleen M., Hopkins, Corey R., Lindsley, Craig W.
Published in ACS medicinal chemistry letters (01.03.2019)
Published in ACS medicinal chemistry letters (01.03.2019)
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The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate
Panarese, Joseph D., Engers, Darren W., Wu, Yong-Jin, Guernon, Jason M., Chun, Aspen, Gregro, Alison R., Bender, Aaron M., Capstick, Rory A., Wieting, Joshua M., Bronson, Joanne J., Macor, John E., Westphal, Ryan, Soars, Matthew, Engers, Julie E., Felts, Andrew S., Rodriguez, Alice L., Emmitte, Kyle A., Jones, Carrie K., Blobaum, Anna L., Jeffrey Conn, P., Niswender, Colleen M., Hopkins, Corey R., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.01.2019)
Published in Bioorganic & medicinal chemistry letters (15.01.2019)
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Journal Article
Discovery of VU2957 (Valiglurax): An mGlu 4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease
Panarese, Joseph D, Engers, Darren W, Wu, Yong-Jin, Bronson, Joanne J, Macor, John E, Chun, Aspen, Rodriguez, Alice L, Felts, Andrew S, Engers, Julie L, Loch, Matthew T, Emmitte, Kyle A, Castelhano, Arlindo L, Kates, Michael J, Nader, Michael A, Jones, Carrie K, Blobaum, Anna L, Conn, P Jeffrey, Niswender, Colleen M, Hopkins, Corey R, Lindsley, Craig W
Published in ACS medicinal chemistry letters (14.03.2019)
Published in ACS medicinal chemistry letters (14.03.2019)
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Exploration of Allosteric Agonism Structure–Activity Relationships within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5‑((3-Fluorophenyl)ethynyl)‑N‑(3-methyloxetan-3-yl)picolinamide (ML254)
Turlington, Mark, Noetzel, Meredith J, Chun, Aspen, Zhou, Ya, Gogliotti, Rocco D, Nguyen, Elizabeth D, Gregory, Karen J, Vinson, Paige N, Rook, Jerri M, Gogi, Kiran K, Xiang, Zixiu, Bridges, Thomas M, Daniels, J. Scott, Jones, Carrie, Niswender, Colleen M, Meiler, Jens, Conn, P. Jeffrey, Lindsley, Craig W, Stauffer, Shaun R
Published in Journal of medicinal chemistry (24.10.2013)
Published in Journal of medicinal chemistry (24.10.2013)
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Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson’s Disease
Panarese, Joseph D, Engers, Darren W, Wu, Yong-Jin, Bronson, Joanne J, Macor, John E, Chun, Aspen, Rodriguez, Alice L, Felts, Andrew S, Engers, Julie L, Loch, Matthew T, Emmitte, Kyle A, Castelhano, Arlindo L, Kates, Michael J, Nader, Michael A, Jones, Carrie K, Blobaum, Anna L, Conn, P. Jeffrey, Niswender, Colleen M, Hopkins, Corey R, Lindsley, Craig W
Published in ACS medicinal chemistry letters (14.03.2019)
Published in ACS medicinal chemistry letters (14.03.2019)
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Journal Article
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu 4 PAM development candidate
Panarese, Joseph D, Engers, Darren W, Wu, Yong-Jin, Guernon, Jason M, Chun, Aspen, Gregro, Alison R, Bender, Aaron M, Capstick, Rory A, Wieting, Joshua M, Bronson, Joanne J, Macor, John E, Westphal, Ryan, Soars, Matthew, Engers, Julie E, Felts, Andrew S, Rodriguez, Alice L, Emmitte, Kyle A, Jones, Carrie K, Blobaum, Anna L, Conn, P Jeffrey, Niswender, Colleen M, Hopkins, Corey R, Lindsley, Craig W
Published in Bioorganic & medicinal chemistry letters (15.01.2019)
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Published in Bioorganic & medicinal chemistry letters (15.01.2019)
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