SAR156497, an Exquisitely Selective Inhibitor of Aurora Kinases
Carry, Jean-Christophe, Clerc, François, Minoux, Hervé, Schio, Laurent, Mauger, Jacques, Nair, Anil, Parmantier, Eric, Le Moigne, Ronan, Delorme, Cécile, Nicolas, Jean-Paul, Krick, Alain, Abécassis, Pierre-Yves, Crocq-Stuerga, Véronique, Pouzieux, Stéphanie, Delarbre, Laure, Maignan, Sébastien, Bertrand, Thomas, Bjergarde, Kirsten, Ma, Nina, Lachaud, Sylvette, Guizani, Houlfa, Lebel, Rémi, Doerflinger, Gilles, Monget, Sylvie, Perron, Sébastien, Gasse, Francis, Angouillant-Boniface, Odile, Filoche-Rommé, Bruno, Murer, Michel, Gontier, Sylvie, Prévost, Céline, Monteiro, Marie-Line, Combeau, Cécile
Published in Journal of medicinal chemistry (08.01.2015)
Published in Journal of medicinal chemistry (08.01.2015)
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Journal Article
Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease
Lesuisse, Dominique, Malanda, André, Peyronel, Jean-François, Evanno, Yannick, Lardenois, Patrick, De-Peretti, Danielle, Abécassis, Pierre-Yves, Barnéoud, Pascal, Brunel, Pascale, Burgevin, Marie-Claude, Cegarra, Céline, Auger, Florian, Dommergue, Amélie, Lafon, Corinne, Even, Luc, Tsi, Joanna, Luc, Thy Phuong Hieu, Almario, Antonio, Olivier, Anne, Castel, Marie-Noëlle, Taupin, Véronique, Rooney, Thomas, Vigé, Xavier
Published in Bioorganic & medicinal chemistry letters (01.04.2019)
Published in Bioorganic & medicinal chemistry letters (01.04.2019)
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Journal Article
Data on synthesis, ADME and pharmacological properties and early safety pharmacology evaluation of a series of novel NURR1/NOT agonist potentially useful for the treatment of Parkinson's disease
Malanda, André, Abécassis, Pierre-Yves, Barnéoud, Pascal, Brunel, Pascale, Taupin, Véronique, Vigé, Xavier, Lesuisse, Dominique
Published in Data in brief (01.12.2019)
Published in Data in brief (01.12.2019)
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Journal Article
The Circadian Clock Components CRY1 and CRY2 Are Necessary to Sustain Sex Dimorphism in Mouse Liver Metabolism
Bur, Isabelle M., Cohen-Solal, Anne M., Carmignac, Danielle, Abecassis, Pierre-Yves, Chauvet, Norbert, Martin, Agnès O., van der Horst, Gijsbertus T.J., Robinson, Iain C.A.F., Maurel, Patrick, Mollard, Patrice, Bonnefont, Xavier
Published in The Journal of biological chemistry (03.04.2009)
Published in The Journal of biological chemistry (03.04.2009)
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Journal Article
SAR439859, a Novel Selective Estrogen Receptor Degrader (SERD), Demonstrates Effective and Broad Antitumor Activity in Wild-Type and Mutant ER-Positive Breast Cancer Models
Shomali, Maysoun, Cheng, Jane, Sun, Fangxian, Koundinya, Malvika, Guo, Zhuyan, Hebert, Andrew T, McManus, Jessica, Levit, Mikhail N, Hoffmann, Dietmar, Courjaud, Albane, Arrebola, Rosalia, Cao, Hui, Pollard, Jack, Lee, Joon Sang, Besret, Laurent, Caron, Anne, Bangari, Dinesh S, Abecassis, Pierre-Yves, Schio, Laurent, El-Ahmad, Youssef, Halley, Frank, Tabart, Michel, Certal, Victor, Thompson, Fabienne, McCort, Gary, Filoche-Rommé, Bruno, Cheng, Hong, Garcia-Echeverria, Carlos, Debussche, Laurent, Bouaboula, Monsif
Published in Molecular cancer therapeutics (01.02.2021)
Published in Molecular cancer therapeutics (01.02.2021)
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Journal Article
Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3 S )-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7 H -benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer
El-Ahmad, Youssef, Tabart, Michel, Halley, Frank, Certal, Victor, Thompson, Fabienne, Filoche-Rommé, Bruno, Gruss-Leleu, Florence, Muller, Claire, Brollo, Maurice, Fabien, Laurence, Loyau, Véronique, Bertin, Luc, Richepin, Patrick, Pilorge, Fabienne, Desmazeau, Pascal, Girardet, Chrystelle, Beccari, Sylvie, Louboutin, Audrey, Lebourg, Gilles, Le-Roux, Jacques, Terrier, Corinne, Vallée, François, Steier, Valérie, Mathieu, Magali, Rak, Alexey, Abecassis, Pierre-Yves, Vicat, Pascale, Benard, Tsiala, Bouaboula, Monsif, Sun, Fangxian, Shomali, Maysoun, Hebert, Andrew, Levit, Mikhail, Cheng, Hong, Courjaud, Albane, Ginesty, Celine, Perrault, Christelle, Garcia-Echeverria, Carlos, McCort, Gary, Schio, Laurent
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Journal Article
Discovery of (2S)‑8-[(3R)‑3-Methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro‑2H‑pyrimido[1,2‑a]pyrimidin-6-one: A Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors
Pasquier, Benoit, El-Ahmad, Youssef, Filoche-Rommé, Bruno, Dureuil, Christine, Fassy, Florence, Abecassis, Pierre-Yves, Mathieu, Magali, Bertrand, Thomas, Benard, Tsiala, Barrière, Cédric, El Batti, Samira, Letallec, Jean-Philippe, Sonnefraud, Véronique, Brollo, Maurice, Delbarre, Laurence, Loyau, Véronique, Pilorge, Fabienne, Bertin, Luc, Richepin, Patrick, Arigon, Jérôme, Labrosse, Jean-Robert, Clément, Jacques, Durand, Florence, Combet, Romain, Perraut, Pierre, Leroy, Vincent, Gay, Frédéric, Lefrançois, Dominique, Bretin, François, Marquette, Jean-Pierre, Michot, Nadine, Caron, Anne, Castell, Christelle, Schio, Laurent, McCort, Gary, Goulaouic, Hélène, Garcia-Echeverria, Carlos, Ronan, Baptiste
Published in Journal of medicinal chemistry (08.01.2015)
Published in Journal of medicinal chemistry (08.01.2015)
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Journal Article
Discovery of (2 S )-8-[(3 R )-3-Methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2 H -pyrimido[1,2- a ]pyrimidin-6-one: A Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors
Pasquier, Benoit, El-Ahmad, Youssef, Filoche-Rommé, Bruno, Dureuil, Christine, Fassy, Florence, Abecassis, Pierre-Yves, Mathieu, Magali, Bertrand, Thomas, Benard, Tsiala, Barrière, Cédric, El Batti, Samira, Letallec, Jean-Philippe, Sonnefraud, Véronique, Brollo, Maurice, Delbarre, Laurence, Loyau, Véronique, Pilorge, Fabienne, Bertin, Luc, Richepin, Patrick, Arigon, Jérôme, Labrosse, Jean-Robert, Clément, Jacques, Durand, Florence, Combet, Romain, Perraut, Pierre, Leroy, Vincent, Gay, Frédéric, Lefrançois, Dominique, Bretin, François, Marquette, Jean-Pierre, Michot, Nadine, Caron, Anne, Castell, Christelle, Schio, Laurent, McCort, Gary, Goulaouic, Hélène, Garcia-Echeverria, Carlos, Ronan, Baptiste
Published in Journal of medicinal chemistry (08.01.2015)
Published in Journal of medicinal chemistry (08.01.2015)
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Journal Article
Discovery and Optimization of Pyrimidone Indoline Amide PI3Kβ Inhibitors for the Treatment of Phosphatase and Tensin Homologue (PTEN)-Deficient Cancers
Certal, Victor, Carry, Jean-Christophe, Halley, Frank, Virone-Oddos, Angela, Thompson, Fabienne, Filoche-Rommé, Bruno, El-Ahmad, Youssef, Karlsson, Andreas, Charrier, Véronique, Delorme, Cécile, Rak, Alexey, Abecassis, Pierre-Yves, Amara, Céline, Vincent, Loïc, Bonnevaux, Hélène, Nicolas, Jean-Paul, Mathieu, Magali, Bertrand, Thomas, Marquette, Jean-Pierre, Michot, Nadine, Benard, Tsiala, Perrin, Marc-Antoine, Lemaitre, Olivier, Guerif, Stephane, Perron, Sébastien, Monget, Sylvie, Gruss-Leleu, Florence, Doerflinger, Gilles, Guizani, Houlfa, Brollo, Maurice, Delbarre, Laurence, Bertin, Luc, Richepin, Patrick, Loyau, Véronique, Garcia-Echeverria, Carlos, Lengauer, Christoph, Schio, Laurent
Published in Journal of medicinal chemistry (13.02.2014)
Published in Journal of medicinal chemistry (13.02.2014)
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Journal Article
Discovery and Optimization of New Benzimidazole- and Benzoxazole-Pyrimidone Selective PI3Kβ Inhibitors for the Treatment of Phosphatase and TENsin homologue (PTEN)-Deficient Cancers
Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Delorme, Cécile, Karlsson, Andreas, Rak, Alexey, Thompson, Fabienne, Filoche-Rommé, Bruno, El-Ahmad, Youssef, Carry, Jean-Christophe, Abecassis, Pierre-Yves, Lejeune, Pascale, Vincent, Loic, Bonnevaux, Hélène, Nicolas, Jean-Paul, Bertrand, Thomas, Marquette, Jean-Pierre, Michot, Nadine, Benard, Tsiala, Below, Peter, Vade, Isabelle, Chatreaux, Fabienne, Lebourg, Gilles, Pilorge, Fabienne, Angouillant-Boniface, Odile, Louboutin, Audrey, Lengauer, Christoph, Schio, Laurent
Published in Journal of medicinal chemistry (24.05.2012)
Published in Journal of medicinal chemistry (24.05.2012)
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Journal Article
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors
Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Thompson, Fabienne, Filoche-Rommé, Bruno, El-Ahmad, Youssef, Carry, Jean-Christophe, Delorme, Cécile, Karlsson, Andreas, Abecassis, Pierre-Yves, Vincent, Loic, Bonnevaux, Hélène, Nicolas, Jean-Paul, Morales, Renaud, Michot, Nadine, Vade, Isabelle, Louboutin, Audrey, Perron, Sébastien, Doerflinger, Gilles, Tric, Bernadette, Monget, Sylvie, Lengauer, Christoph, Schio, Laurent
Published in Bioorganic & medicinal chemistry letters (15.10.2012)
Published in Bioorganic & medicinal chemistry letters (15.10.2012)
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Journal Article
Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors
Certal, Victor, Halley, Frank, Virone-Oddos, Angela, Filoche-Rommé, Bruno, Carry, Jean-Christophe, Gruss-Leleu, Florence, Bertin, Luc, Guizani, Houlfa, Pilorge, Fabienne, Richepin, Patrick, Karlsson, Andreas, Charrier, Véronique, Abecassis, Pierre-Yves, Vincent, Loic, Nicolas, Jean-Paul, Lengauer, Christoph, Garcia-Echeverria, Carlos, Schio, Laurent
Published in Bioorganic & medicinal chemistry letters (15.03.2014)
Published in Bioorganic & medicinal chemistry letters (15.03.2014)
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Journal Article
Design of potent and selective GSK3β inhibitors with acceptable safety profile and pharmacokinetics
Lesuisse, Dominique, Tiraboschi, Gilles, Krick, Alain, Abecassis, Pierre-Yves, Dutruc-Rosset, Gilles, Babin, Didier, Halley, Frank, Châtreau, Fabienne, Lachaud, Sylvette, Chevalier, Alain, Quarteronet, Dominique, Burgevin, Marie-Claude, Amara, Céline, Bertrand, Philippe, Rooney, Thomas
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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Journal Article
In vivo testing of drug-linker stability
Abecassis, Pierre-Yves, Amara, Céline
Published in Methods in molecular biology (Clifton, N.J.) (01.01.2013)
Published in Methods in molecular biology (Clifton, N.J.) (01.01.2013)
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Journal Article
Discovery of 6‑(2,4-Dichlorophenyl)-5-[4-[(3S)‑1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro‑7H‑benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer
El-Ahmad, Youssef, Tabart, Michel, Halley, Frank, Certal, Victor, Thompson, Fabienne, Filoche-Rommé, Bruno, Gruss-Leleu, Florence, Muller, Claire, Brollo, Maurice, Fabien, Laurence, Loyau, Véronique, Bertin, Luc, Richepin, Patrick, Pilorge, Fabienne, Desmazeau, Pascal, Girardet, Chrystelle, Beccari, Sylvie, Louboutin, Audrey, Lebourg, Gilles, Le-Roux, Jacques, Terrier, Corinne, Vallée, François, Steier, Valérie, Mathieu, Magali, Rak, Alexey, Abecassis, Pierre-Yves, Vicat, Pascale, Benard, Tsiala, Bouaboula, Monsif, Sun, Fangxian, Shomali, Maysoun, Hebert, Andrew, Levit, Mikhail, Cheng, Hong, Courjaud, Albane, Ginesty, Celine, Perrault, Christelle, Garcia-Echeverria, Carlos, McCort, Gary, Schio, Laurent
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Journal Article
Discovery and Optimization of Pyrimidone Indoline Amide P13K beta Inhibitors for the Treatment of Phosphatase and Tensin Homologue (PTEN)-Deficient Cancers
Certal, Victor, Carry, Jean-Christophe, Halley, Frank, Virone-Oddos, Angela, Thompson, Fabienne, Filoche-Romme, Bruno, El-Ahmad, Youssef, Karlsson, Andreas, Charrier, Veronique, Delorme, Cecile, Rak, Alexey, Abecassis, Pierre-Yves, Amara, Celine, Vincent, Loic, Bonnevaux, Helene, Nicolas, Jean-Paul, Mathieu, Magali, Bertrand, Thomas, Marquette, Jean-Pierre, Michot, Nadine, Benard, Tsiala, Perrin, Marc-Antoine, Lemaitre, Olivier, Guerif, Stephane, Perron, Sebastien, Monget, Sylvie, Gruss-Leleu, Florence, Doerflinger, Gilles, Guizani, Houlfa, Brollo, Maurice, Delbarre, Laurence, Benin, Luc, Richepin, Patrick, Loyau, Veronique, Garcia-Echeverria, Carlos, Lengauer, Christoph, Schio, Laurent
Published in Journal of medicinal chemistry (13.02.2014)
Published in Journal of medicinal chemistry (13.02.2014)
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Journal Article
Abstract 3070: Discovery of novel potent allele-selective KRAS-G12C covalent inhibitors stemming from DNA-encoded library
McCort, Gary, Arrebola, Rosalia, Calvet, Loreley, Ronan, Baptiste, Vergne, Fabrice, Duffieux, Francis, Rak, Alexey, Meaux, Isabelle, Papin, David, Fassy, Florence, Delorme, Cecile, Matthieu, Magali, Nicolas, Jean-Paul, Marcireau, Christophe, Steier, Valerie, Abecassis, Pierre-Yves, Czepczor, Valerie, Thomson, Heather A., Hupp, Christopher D., Guilinger, J.P., Zhang, Ying, Keefe, Anthony D., Cuozzo, John W., Liu, Julie, Debussche, Laurent
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
SARI 56497, an Exquisitely Selective Inhibitor of Aurora Kinases
Carry, Jean-Christophe, Clerc, Francois, Minoux, Herve, Schio, Laurent, Mauger, Jacques, Nair, Anil, Parmantier, Eric, Le Moigne, Ronan, Delorme, Cecile, Nicolas, Jean-Paul, Krick, Alain, Abecassis, Pierre-Yves, Crocq-Stuerga, Veronique, Pouzieux, Stephanie, Delarbre, Laure, Maignan, Sebastien, Bertrand, Thomas, Bjergarde, Kirsten, Ma, Nina, Lachaud, Sylvette, Guizani, Houlfa, Lebel, Remi, Doerflinger, Gilles, Monget, Sylvie, Perron, Sebastien, Gasse, Francis, Angouillant-Boniface, Odile, Filoche-Romme, Bruno, Murer, Michel, Gontier, Sylvie, Prevost, Celine, Monteiro, Marie-Line, Combeau, Cecile
Published in Journal of medicinal chemistry (08.01.2015)
Published in Journal of medicinal chemistry (08.01.2015)
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Journal Article
Abstract 5775: Identification of SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that has strong anti-tumor activity in wild-type and mutant ER+ breast cancer models
Shomali, Maysoun, El-Ahmad, Youssef, Halley, Frank, Cheng, Jane, Weinstein, Michael, Wang, Muchun, Sun, Fangxian, Malkova, Natalia, Levit, Mikhail, Koundinya, Malvika, Gou, Zhuyan, Hebert, Andrew, McManus, Jessica, Hoffman, Dietmar, Cao, Hui, Jung, Joonil, Pollard, Jack, Vincent, Sylvie, Ackerson, Timothy, Adrian, Francisco, Winter, Chris, Richon, Victoria, Chen, Hong, Hsu, Karl, Lager, Joanne, Courjaud, Albane, Arrebola, Rosalia, Besret, Laurent, Abecassis, Pierre-Yves, Schio, Laurent, McCort, Gary, Tabart, Michel, Certal, Victor, Thompson, Fabienne, Filoche-Rommé, Bruno, Debussche, Laurent, Cohen, Patrick, Garcia-Echeverria, Carlos, Bouaboula, Monsif
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Abstract LB-053: Towards new cryptophycins as promising payloads for ADC
Brun, Marie-Priscille, Bouchard, Hervé, Clerc, François, Zhang, Jidong, Abecassis, Pierre-Yves, Amara, Céline, Beys, Eric, Efremenko, Florence, Nicolazzi, Céline, Pascual, Marie-Hélène, Pasquier, Olivier, Krick, Alain, Berne, Pierre-François, Gauzy, Laurence, Karst, Nathalie, Huille, Sylvain, Henry, Christophe, Lefebvre, Anne-Marie, Sassoon, Ingrid
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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