Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit
Rianjongdee, Francesco, Atkinson, Stephen J, Chung, Chun-wa, Grandi, Paola, Gray, James R. J, Kaushansky, Laura J, Medeiros, Patricia, Messenger, Cassie, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Satz, Alexander L, Taylor, Simon, Wall, Ian D, Watson, Robert J, Yao, Gang, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
Seal, Jonathan T, Atkinson, Stephen J, Aylott, Helen, Bamborough, Paul, Chung, Chun-wa, Copley, Royston C. B, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Lindon, Matthew, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins
Preston, Alex, Atkinson, Stephen, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Jones, Emma J, Lindon, Matthew, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan, Taylor, Simon, Wall, Ian, Watson, Robert J, Woolven, James, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors
Lucas, Simon C. C, Atkinson, Stephen J, Chung, Chun-wa, Davis, Rob, Gordon, Laurie, Grandi, Paola, Gray, James J. R, Grimes, Thomas, Phillipou, Alexander, Preston, Alex G, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Tomkinson, Nicholas C. O, Wall, Ian, Watson, Robert J, Woolven, James, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Identification of a Series of N‑Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins
Harrison, Lee A, Atkinson, Stephen J, Bassil, Anna, Chung, Chun-wa, Grandi, Paola, Gray, James R. J, Levernier, Etienne, Lewis, Antonia, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jonathan T, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors
Seal, Jonathan T, Atkinson, Stephen J, Bamborough, Paul, Bassil, Anna, Chung, Chun-wa, Foley, James, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Kruger, Ryan G, Matteo, Jeanne J, McCabe, Michael T, Messenger, Cassie, Mitchell, Darren, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Wyce, Anastasia, Zhang, Xi-Ping, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors
Aylott, Helen E, Atkinson, Stephen J, Bamborough, Paul, Bassil, Anna, Chung, Chun-wa, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Messenger, Cassie, Mitchell, Darren, Phillipou, Alexander, Preston, Alex, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan T, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Journal Article
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family
Preston, Alex, Atkinson, Stephen J, Bamborough, Paul, Chung, Chun-wa, Gordon, Laurie J, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Lewis, Antonia J, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jon, Taylor, Simon, Thesmar, Pierre, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in ACS medicinal chemistry letters (13.08.2020)
Published in ACS medicinal chemistry letters (13.08.2020)
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Journal Article
Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate
Demont, Emmanuel H, Andrews, Benjamin I, Bit, Rino A, Campbell, Colin A, Cooke, Jason W. B, Deeks, Nigel, Desai, Sapna, Dowell, Simon J, Gaskin, Pam, Gray, James R. J, Haynes, Andrea, Holmes, Duncan S, Kumar, Umesh, Morse, Mary A, Osborne, Greg J, Panchal, Terry, Patel, Bela, Perboni, Alcide, Taylor, Simon, Watson, Robert, Witherington, Jason, Willis, Robert
Published in ACS medicinal chemistry letters (09.06.2011)
Published in ACS medicinal chemistry letters (09.06.2011)
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Journal Article
The utility of pharmacokinetic-pharmacodynamic modeling in the discovery and optimization of selective S1P(1) agonists
Taylor, Simon, Gray, James R J, Willis, Robert, Deeks, Nigel, Haynes, Andrea, Campbell, Colin, Gaskin, Pam, Leavens, Karen, Demont, Emmanuel, Dowell, Simon, Cryan, Jenni, Morse, Mary, Patel, Aarti, Garden, Helen, Witherington, Jason
Published in Xenobiotica (01.07.2012)
Published in Xenobiotica (01.07.2012)
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Journal Article
Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose
Demont, Emmanuel H, Arpino, Sandra, Bit, Rino A, Campbell, Colin A, Deeks, Nigel, Desai, Sapna, Dowell, Simon J, Gaskin, Pam, Gray, James R. J, Harrison, Lee A, Haynes, Andrea, Heightman, Tom D, Holmes, Duncan S, Humphreys, Philip G, Kumar, Umesh, Morse, Mary A, Osborne, Greg J, Panchal, Terry, Philpott, Karen L, Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P(3))-Sparing S1P(1) Agonists Active at Low Oral Doses
Demont, Emmanuel H., Bailey, James M., Bit, Rino A., Brown, Jack A., Campbell, Colin A., Deeks, Nigel, Dowell, Simon J., Eldred, Colin, Gaskin, Pam, Gray, James R. J., Haynes, Andrea, Hirst, David J., Holmes, Duncan S., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Renaux, Jessica F., Seal, Gail A. L., Smethurst, Chris A., Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Journal Article
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses
Demont, Emmanuel H, Bailey, James M, Bit, Rino A, Brown, Jack A, Campbell, Colin A, Deeks, Nigel, Dowell, Simon J, Eldred, Colin, Gaskin, Pam, Gray, James R J, Haynes, Andrea, Hirst, David J, Holmes, Duncan S, Kumar, Umesh, Morse, Mary A, Osborne, Greg J, Renaux, Jessica F, Seal, Gail A L, Smethurst, Chris A, Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Journal Article
Discovery of a Brain-Penetrant S1P(3)-Sparing Direct Agonist of the S1P(1) and S1P(5) Receptors Efficacious at Low Oral Dose
Demont, Emmanuel H., Arpino, Sandra, Bit, Rino A., Campbell, Colin A., Deeks, Nigel, Desai, Sapna, Dowell, Simon J., Gaskin, Pam, Gray, James R. J., Harrison, Lee A., Haynes, Andrea, Heightman, Tom D., Holmes, Duncan S., Humphreys, Philip G., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Panchal, Terry, Philpott, Karen L., Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
Discovery of a Brain-Penetrant S1P 3 -Sparing Direct Agonist of the S1P 1 and S1P 5 Receptors Efficacious at Low Oral Dose
Demont, Emmanuel H., Arpino, Sandra, Bit, Rino A., Campbell, Colin A., Deeks, Nigel, Desai, Sapna, Dowell, Simon J., Gaskin, Pam, Gray, James R. J., Harrison, Lee A., Haynes, Andrea, Heightman, Tom D., Holmes, Duncan S., Humphreys, Philip G., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Panchal, Terry, Philpott, Karen L., Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P 3 )-Sparing S1P 1 Agonists Active at Low Oral Doses
Demont, Emmanuel H., Bailey, James M., Bit, Rino A., Brown, Jack A., Campbell, Colin A., Deeks, Nigel, Dowell, Simon J., Eldred, Colin, Gaskin, Pam, Gray, James R. J., Haynes, Andrea, Hirst, David J., Holmes, Duncan S., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Renaux, Jessica F., Seal, Gail A. L., Smethurst, Chris A., Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Journal Article
The utility of pharmacokinetic–pharmacodynamic modeling in the discovery and optimization of selective S1P 1 agonists
Taylor, Simon, Gray, James R. J., Willis, Robert, Deeks, Nigel, Haynes, Andrea, Campbell, Colin, Gaskin, Pam, Leavens, Karen, Demont, Emmanuel, Dowell, Simon, Cryan, Jenni, Morse, Mary, Patel, Aarti, Garden, Helen, Witherington, Jason
Published in Xenobiotica (01.07.2012)
Published in Xenobiotica (01.07.2012)
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Journal Article
The utility of pharmacokinetic-pharmacodynamic modeling in the discovery and optimization of selective S1P1 agonists
Taylor, Simon, Gray, James R. J., Willis, Robert, Deeks, Nigel, Haynes, Andrea, Campbell, Colin, Gaskin, Pam, Leavens, Karen, Demont, Emmanuel, Dowell, Simon, Cryan, Jenni, Morse, Mary, Patel, Aarti, Garden, Helen, Witherington, Jason
Published in Xenobiotica (01.07.2012)
Published in Xenobiotica (01.07.2012)
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Journal Article
Discovery of a Selective S1P 1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate
Demont, Emmanuel H., Andrews, Benjamin I., Bit, Rino A., Campbell, Colin A., Cooke, Jason W. B., Deeks, Nigel, Desai, Sapna, Dowell, Simon J., Gaskin, Pam, Gray, James R. J., Haynes, Andrea, Holmes, Duncan S., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Panchal, Terry, Patel, Bela, Perboni, Alcide, Taylor, Simon, Watson, Robert, Witherington, Jason, Willis, Robert
Published in ACS medicinal chemistry letters (09.06.2011)
Published in ACS medicinal chemistry letters (09.06.2011)
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Journal Article
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1‑Phosphate Receptor 3 (S1P3)‑Sparing S1P1 Agonists Active at Low Oral Doses
Demont, Emmanuel H, Bailey, James M, Bit, Rino A, Brown, Jack A, Campbell, Colin A, Deeks, Nigel, Dowell, Simon J, Eldred, Colin, Gaskin, Pam, Gray, James R. J, Haynes, Andrea, Hirst, David J, Holmes, Duncan S, Kumar, Umesh, Morse, Mary A, Osborne, Greg J, Renaux, Jessica F, Seal, Gail A. L, Smethurst, Chris A, Taylor, Simon, Watson, Robert, Willis, Robert, Witherington, Jason
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Journal Article