Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis
Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Joncour, Agnès, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Rondet, Emilie, Peixoto, Christophe, Grassot, Jean-Marie, Picolet, Olivier, Annoot, Denis, Triballeau, Nicolas, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Blanque, Roland, Cottereaux, Celine, Vandervoort, Nele, Christophe, Thierry, Mollat, Patrick, Lamers, Marieke, Auberval, Marielle, Hrvacic, Boska, Ralic, Jovica, Oste, Line, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Journal Article
Virtual Screening Workflow Development Guided by the “Receiver Operating Characteristic” Curve Approach. Application to High-Throughput Docking on Metabotropic Glutamate Receptor Subtype 4
Triballeau, Nicolas, Acher, Francine, Brabet, Isabelle, Pin, Jean-Philippe, Bertrand, Hugues-Olivier
Published in Journal of medicinal chemistry (07.04.2005)
Published in Journal of medicinal chemistry (07.04.2005)
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Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2‑a]pyridine Series of Autotaxin Inhibitors
Joncour, Agnès, Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Peixoto, Christophe, Annoot, Denis, Lepissier, Luce, Heiermann, Jörg, Hengeveld, Willem Jan, Pilzak, Gregor, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Galien, René, David, Christelle, Vandervoort, Nele, Christophe, Thierry, Conrath, Katja, Jans, Mia, Wohlkonig, Alexandre, Soror, Sameh, Steyaert, Jan, Touitou, Robert, Fleury, Damien, Vercheval, Lionel, Mollat, Patrick, Triballeau, Nicolas, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (14.09.2017)
Published in Journal of medicinal chemistry (14.09.2017)
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Discovery and Optimization of an Azetidine Chemical Series As a Free Fatty Acid Receptor 2 (FFA2) Antagonist: From Hit to Clinic
Pizzonero, Mathieu, Dupont, Sonia, Babel, Marielle, Beaumont, Stéphane, Bienvenu, Natacha, Blanqué, Roland, Cherel, Laëtitia, Christophe, Thierry, Crescenzi, Benedetta, De Lemos, Elsa, Delerive, Philippe, Deprez, Pierre, De Vos, Steve, Djata, Fatoumata, Fletcher, Stephen, Kopiejewski, Sabrina, L’Ebraly, Christelle, Lefrançois, Jean-Michel, Lavazais, Stéphanie, Manioc, Murielle, Nelles, Luc, Oste, Line, Polancec, Denis, Quénéhen, Vanessa, Soulas, Florilène, Triballeau, Nicolas, van der Aar, Ellen M, Vandeghinste, Nick, Wakselman, Emanuelle, Brys, Reginald, Saniere, Laurent
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases
Mammoliti, Oscar, Jansen, Koen, El Bkassiny, Sandy, Palisse, Adeline, Triballeau, Nicolas, Bucher, Denis, Allart, Brigitte, Jaunet, Alex, Tricarico, Giovanni, De Wachter, Maxim, Menet, Christel, Blanc, Javier, Letfus, Vatroslav, Rupčić, Renata, Šmehil, Mario, Poljak, Tanja, Coornaert, Beatrice, Sonck, Kathleen, Duys, Inge, Waeckel, Ludovic, Lecru, Lola, Marsais, Florence, Jagerschmidt, Catherine, Auberval, Marielle, Pujuguet, Philippe, Oste, Line, Borgonovi, Monica, Wakselman, Emanuelle, Christophe, Thierry, Houvenaghel, Nicolas, Jans, Mia, Heckmann, Bertrand, Sanière, Laurent, Brys, Reginald
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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Journal Article
Discovery of Diarylhydantoins as New Selective Androgen Receptor Modulators
Nique, François, Hebbe, Séverine, Peixoto, Christophe, Annoot, Denis, Lefrançois, Jean-Michel, Duval, Eric, Michoux, Laurence, Triballeau, Nicolas, Lemoullec, Jean-Michel, Mollat, Patrick, Thauvin, Maxime, Prangé, Thierry, Minet, Dominique, Clément-Lacroix, Philippe, Robin-Jagerschmidt, Catherine, Fleury, Damien, Guédin, Denis, Deprez, Pierre
Published in Journal of medicinal chemistry (11.10.2012)
Published in Journal of medicinal chemistry (11.10.2012)
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Journal Article
Identification of a 4‑(Hydroxymethyl)diarylhydantoin as a Selective Androgen Receptor Modulator
Nique, François, Hebbe, Séverine, Triballeau, Nicolas, Peixoto, Christophe, Lefrançois, Jean-Michel, Jary, Hélène, Alvey, Luke, Manioc, Murielle, Housseman, Christopher, Klaassen, Hugo, Van Beeck, Kris, Guédin, Denis, Namour, Florence, Minet, Dominque, Van der Aar, Ellen, Feyen, Jean, Fletcher, Stephen, Blanqué, Roland, Robin-Jagerschmidt, Catherine, Deprez, Pierre
Published in Journal of medicinal chemistry (11.10.2012)
Published in Journal of medicinal chemistry (11.10.2012)
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Journal Article
Reinvestigation of the Branimycin Stereochemistry at Position 17‑C
Čikoš, Ana, Triballeau, Nicolas, Hubbard, Paul A, Žiher, Dinko, Stouten, Pieter F. W, Doyon, Julien G. P.-O, Deschrijver, Tiny, Wouters, Johan, Lépine, Renaud H. M, Saniere, Laurent
Published in Organic letters (19.02.2016)
Published in Organic letters (19.02.2016)
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Closure of the Venus Flytrap Module of mGlu8 Receptor and the Activation Process: Insights from Mutations Converting Antagonists into Agonists
Bessis, Anne-Sophie, Rondard, Philippe, Gaven, Florence, Brabet, Isabelle, Triballeau, Nicolas, Prézeau, Laurent, Acher, Francine, Pin, Jean-Philippe
Published in Proceedings of the National Academy of Sciences - PNAS (20.08.2002)
Published in Proceedings of the National Academy of Sciences - PNAS (20.08.2002)
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Journal Article
Amino-Pyrrolidine Tricarboxylic Acids Give New Insight into Group III Metabotropic Glutamate Receptor Activation Mechanism
Frauli, Mélanie, Hubert, Nadia, Schann, Stephan, Triballeau, Nicolas, Bertrand, Hugues-Olivier, Acher, Francine, Neuville, Pascal, Pin, Jean-Philippe, Prézeau, Laurent
Published in Molecular pharmacology (01.03.2007)
Published in Molecular pharmacology (01.03.2007)
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Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS‑5 Inhibitor for the Treatment of Osteoarthritis
Brebion, Franck, Gosmini, Romain, Deprez, Pierre, Varin, Marie, Peixoto, Christophe, Alvey, Luke, Jary, Hélène, Bienvenu, Natacha, Triballeau, Nicolas, Blanque, Roland, Cottereaux, Céline, Christophe, Thierry, Vandervoort, Nele, Mollat, Patrick, Touitou, Robert, Leonard, Philip, Ceuninck, Frédéric De, Botez, Iuliana, Monjardet, Alain, van der Aar, Ellen, Amantini, David
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Journal Article
A Virtual Screening Hit Reveals New Possibilities for Developing Group III Metabotropic Glutamate Receptor Agonists
Selvam, Chelliah, Oueslati, Nadia, Lemasson, Isabelle A, Brabet, Isabelle, Rigault, Delphine, Courtiol, Tiphanie, Cesarini, Sara, Triballeau, Nicolas, Bertrand, Hugues-Olivier, Goudet, Cyril, Pin, Jean-Philippe, Acher, Francine C
Published in Journal of medicinal chemistry (08.04.2010)
Published in Journal of medicinal chemistry (08.04.2010)
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Journal Article
Correction to Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2‑a]pyridine Series of Autotaxin Inhibitors
Joncour, Agnès, Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Peixoto, Christophe, Annoot, Denis, Lepissier, Luce, Heiermann, Jörg, Hengeveld, Willem Jan, Pilzak, Gregor, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Galien, René, David, Christelle, Vandervoort, Nele, Christophe, Thierry, Conrath, Katja, Jans, Mia, Wohlkonig, Alexandre, Soror, Sameh, Steyaert, Jan, Touitou, Robert, Fleury, Damien, Vercheval, Lionel, Mollat, Patrick, Triballeau, Nicolas, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (10.05.2018)
Published in Journal of medicinal chemistry (10.05.2018)
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Journal Article
Rose Bengal analogs and vesicular glutamate transporters (VGLUTs)
Pietrancosta, Nicolas, Kessler, Albane, Favre-Besse, Franck-Cyril, Triballeau, Nicolas, Quentin, Thomas, Giros, Bruno, Mestikawy, Salah El, Acher, Francine C.
Published in Bioorganic & medicinal chemistry (15.09.2010)
Published in Bioorganic & medicinal chemistry (15.09.2010)
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Journal Article
High-Potency Olfactory Receptor Agonists Discovered by Virtual High-Throughput Screening: Molecular Probes for Receptor Structure and Olfactory Function
Triballeau, Nicolas, Van Name, Eric, Laslier, Guillaume, Cai, Diana, Paillard, Guillaume, Sorensen, Peter W., Hoffmann, Rémy, Bertrand, Hugues-Olivier, Ngai, John, Acher, Francine C.
Published in Neuron (Cambridge, Mass.) (10.12.2008)
Published in Neuron (Cambridge, Mass.) (10.12.2008)
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Journal Article
AZETIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF METABOLIC AND INFLAMMATORY DISEASES
VANDEGHINSTE NICK ERNEST RENE, BRYS REGINALD CHRISTOPHE XAVIER, TRIBALLEAU NICOLAS, SANIERE LAURENT RAYMOND MAURICE, DE VOS STEVE IRMA JOEL, PIZZONERO MATHIEU RAFAEL, POURBAIX L'EBRALY CHRISTELLE DOMINIQUE
Year of Publication 02.04.2014
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Year of Publication 02.04.2014
Patent
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): Identification of a new group III metabotropic glutamate receptor selective agonist
Schann, Stephan, Menet, Christel, Arvault, Paul, Mercier, Géraldine, Frauli, Mélanie, Mayer, Stanislas, Hubert, Nadia, Triballeau, Nicolas, Bertrand, Hugues-Olivier, Acher, Francine, Neuville, Pascal
Published in Bioorganic & medicinal chemistry letters (15.09.2006)
Published in Bioorganic & medicinal chemistry letters (15.09.2006)
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Journal Article
Discovery of 2‑[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2‑a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis
Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Joncour, Agnès, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Rondet, Emilie, Peixoto, Christophe, Grassot, Jean-Marie, Picolet, Olivier, Annoot, Denis, Triballeau, Nicolas, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Blanque, Roland, Cottereaux, Celine, Vandervoort, Nele, Christophe, Thierry, Mollat, Patrick, Lamers, Marieke, Auberval, Marielle, Hrvacic, Boska, Ralic, Jovica, Oste, Line, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Journal Article