Discovery and SAR of a novel series of non-MPEP site mGlu(5) PAMs based on an aryl glycine sulfonamide scaffold

Por Rodriguez, Alice L., Zhou, Ya, Williams, Richard, Weaver, C. David, Vinson, Paige N., Dawson, Eric S., Steckler, Thomas, Lavreysen, Hilde, Mackieg, Claire, Bartolomé, José M., Macdonald, Gregor J., Daniels, J. Scott, Niswender, Colleen M., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado em 2012

Further optimization of the mGlu(5) PAM clinical candidate VU0409551/JNJ-46778212: progress and challenges towards a back-up compound

Por Zhou, Ya, Malosh, Chrysa, Conde-Ceide, Susana, Martínez-Viturro, Carlos Manuel, Alcázar, Jesus, Lavreysen, Hilde, Mackie, Claire, Bridges, Thomas M., Daniels, J. Scott, Niswender, Colleen M., Jones, Carrie K., Macdonald, Gregor J., Steckler, Thomas, Conn, P. Jeffrey, Stauffer, Shaun R., Bartolomé-Nebreda, José Manuel, Lindsley, Craig W.
Publicado no Bioorg Med Chem Lett (2015)

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

Por Turlington, Mark, Noetzel, Meredith J., Bridges, Thomas M., Vinson, Paige N., Steckler, Thomas, Lavreysen, Hilde, Mackie, Claire, Bartolomé-Nebreda, José M., Conde-Ceide, Susana, Tong, Han Min, Macdonald, Gregor J., Daniels, J. Scott, Jones, Carrie K., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado no Bioorg Med Chem Lett (2014)

Optimization of an ether series of mGlu(5) positive allosteric modulators: Molecular determinants of MPEP-site interaction crossover

Por Manka, Jason T., Vinson, Paige N., Gregory, Karen J., Zhou, Ya, Williams, Richard, Gogi, Kiran, Days, Emily, Jadhav, Satya, Herman, Elizabeth J., Lavreysen, Hilde, Mackie, Claire, Bartolomé, José M., Macdonald, Gregor J., Steckler, Thomas, Daniels, J. Scott, Weaver, C. David, Niswender, Colleen M., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado em 2012

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu(5))

Por Martín-Martín, María Luz, Bartolomé-Nebreda, José Manuel, Conde-Ceide, Susana, Alonso de Diego, Sergio A., López, Silvia, Martínez-Viturro, Carlos M., Tong, Han Min, Lavreysen, Hilde, Macdonald, Gregor J., Steckler, Thomas, Mackie, Claire, Bridges, Thomas M., Daniels, J. Scott, Niswender, Colleen M., Noetzel, Meredith J., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado no Bioorg Med Chem Lett (2015)

Discovery of VU0409551/JNJ-46778212: An mGlu(5) Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia

Por Conde-Ceide, Susana, Martínez-Viturro, Carlos M., Alcázar, Jesús, Garcia-Barrantes, Pedro M., Lavreysen, Hilde, Mackie, Claire, Vinson, Paige N., Rook, Jerri M., Bridges, Thomas M., Daniels, J. Scott, Megens, Anton, Langlois, Xavier, Drinkenburg, Wilhelmus H., Ahnaou, Abdellah, Niswender, Colleen M., Jones, Carrie K., Macdonald, Gregor J., Steckler, Thomas, Conn, P. Jeffrey, Stauffer, Shaun R., Bartolomé-Nebreda, José Manuel, Lindsley, Craig W.
Publicado no ACS Med Chem Lett (2015)

Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators

Por Malosh, Chrysa, Turlington, Mark, Bridges, Thomas M., Rook, Jerri M., Noetzel, Meredith J., Vinson, Paige N., Steckler, Thomas, Lavreysen, Hilde, Mackie, Claire, Bartolomé-Nebreda, José M., Conde-Ceide, Susana, Martínez-Viturro, Carlos M., Piedrafita, María, Sánchez-Casado, M. Rosa, Macdonald, Gregor J., Daniels, J. Scott, Jones, Carrie K., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado no Bioorg Med Chem Lett (2015)

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu(5) receptor positive allosteric modulators with efficacy in preclinical m...

Por Conde-Ceide, Susana, Alcázar, Jesús, Alonso de Diego, Sergio A., López, Silvia, Martín-Martín, María Luz, Martínez-Viturro, Carlos M., Pena, Miguel-Angel, Tong, Han Min, Lavreysen, Hilde, Mackie, Claire, Bridges, Thomas M., Daniels, J. Scott, Niswender, Colleen M., Jones, Carrie K., Macdonald, Gregor J., Steckler, Thomas, Conn, P. Jeffrey, Stauffer, Shaun R., Lindsley, Craig W., Bartolomé-Nebreda, José Manuel
Publicado no Bioorg Med Chem Lett (2015)

Dihydrothiazolopyridone Derivatives as a Novel Family of Positive Allosteric Modulators of the Metabotropic Glutamate 5 (mGlu(5)) Receptor

Por Bartolomé-Nebreda, José Manuel, Conde-Ceide, Susana, Delgado, Francisca, Iturrino, Laura, Pastor, Joaquín, Pena, Miguel Ángel, Trabanco, Andrés A., Tresadern, Gary, Wassvik, Carola M., Stauffer, Shaun R., Jadhav, Satyawan, Gogi, Kiran, Vinson, Paige N., Noetzel, Meredith J., Days, Emily, Weaver, C. David, Lindsley, Craig W., Niswender, Colleen M., Jones, Carrie K., Conn, P. Jeffrey, Rombouts, Frederik, Lavreysen, Hilde, Macdonald, Gregor J., Mackie, Claire, Steckler, Thomas
Publicado em 2013

Discovery of 1,5-Disubstituted Pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

Por Cid, Jose María, Duvey, Guillaume, Cluzeau, Philippe, Nhem, Vanthea, Macary, Karim, Raux, Alexandre, Poirier, Nicolas, Muller, Jessica, Boléa, Christelle, Finn, Terry, Poli, Sonia, Epping-Jordan, Mark, Chamelot, Emilie, Derouet, Francis, Girard, Francoise, Macdonald, Gregor J., Vega, Juan Antonio, de Lucas, Ana Isabel, Matesanz, Encarnación, Lavreysen, Hilde, Linares, María Lourdes, Oehlrich, Daniel, Oyarzábal, Julen, Tresadern, Gary, Trabanco, Andrés A., Andrés, Jose Ignacio, Le Poul, Emmanuel, Imogai, Hassan, Lutjens, Robert, Rocher, Jean-Philippe
Publicado em 2010

Biased mGlu(5) positive allosteric modulators provide in vivo efficacy without potentiating mGlu(5) modulation of NMDAR currents

Por Rook, Jerri M., Xiang, Zixiu, Lv, Xiaohui, Ghoshal, Ayan, Dickerson, Jonathan W., Bridges, Thomas M., Johnson, Kari A., Foster, Daniel J., Gregory, Karen J., Vinson, Paige N., Thompson, Analisa D., Byun, Nellie, Collier, Rebekah L., Bubser, Michael, Nedelcovych, Michael T., Gould, Robert W., Stauffer, Shaun R., Daniels, J. Scott, Niswender, Colleen M., Lavreysen, Hilde, Mackie, Claire, Conde-Ceide, Susana, Alcazar, Jesus, Bartolomé-Nebreda, José M., Macdonald, Gregor J., Steckler, Thomas, Jones, Carrie K., Lindsley, Craig W., Conn, P. Jeffrey
Publicado no Neuron (2015)