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ID: ALA4630908

Title: Data for DCP probe GSK046

Authors: SGC Frankfurt

Abstract: SGC Frankfurt donated chemical probe project: GSK046 was donated by GlaxoSmithKline. Website: https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/GSK046. Control: No control. References: 1. Preston, Alex, Stephen Atkinson, Paul Bamborough, Chun-Wa Chung, Peter D. Craggs, Laurie Gordon, Paola Grandi, James R. J. Gray, Emma J. Jones, Matthew Lindon, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Francesco Rianjongdee, Inmaculada Rioja, Jonathan Seal, Simon Taylor, Ian Wall, Robert J. Watson, James Woolven, and Emmanuel H. Demont. 2020. ‘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’. Journal of Medicinal Chemistry 63(17):9070–92. doi: 10.1021/acs.jmedchem.0c00605. PMID: 32691591. 2. Harrison, Lee A., Stephen J. Atkinson, Anna Bassil, Chun-Wa Chung, Paola Grandi, James R. J. Gray, Etienne Levernier, Antonia Lewis, David Lugo, Cassie Messenger, Anne-Marie Michon, Darren J. Mitchell, Alex Preston, Rab K. Prinjha, Inmaculada Rioja, Jonathan T. Seal, Simon Taylor, Ian D. Wall, Robert J. Watson, James M. Woolven, and Emmanuel H. Demont. 2021. ‘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’. Journal of Medicinal Chemistry. PMID: 34232650. 3. Gilan, Omer, Inmaculada Rioja, Kathy Knezevic, Matthew J. Bell, Miriam M. Yeung, Nicola R. Harker, Enid Y. N. Lam, Chun-Wa Chung, Paul Bamborough, Massimo Petretich, Marjeta Urh, Stephen J. Atkinson, Anna K. Bassil, Emma J. Roberts, Dane Vassiliadis, Marian L. Burr, Alex G. S. Preston, Christopher Wellaway, Thilo Werner, James R. Gray, Anne-Marie Michon, Thomas Gobbetti, Vinod Kumar, Peter E. Soden, Andrea Haynes, Johanna Vappiani, David F. Tough, Simon Taylor, Sarah-Jane Dawson, Marcus Bantscheff, Matthew Lindon, Gerard Drewes, Emmanuel H. Demont, Danette L. Daniels, Paola Grandi, Rab K. Prinjha, and Mark A. Dawson. 2020. ‘Selective Targeting of BD1 and BD2 of the BET Proteins in Cancer and Immunoinflammation’. Science (New York, N.Y.) 368(6489):387–94. PMID: 32193360.

DOI: 10.6019/CHEMBL4630908