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Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.

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Title: Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Authors: Down K; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Amour A; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Anderson NA; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Barton N; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Campos S; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Cannons EP; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Clissold C; Charles River Discovery, Chesterford Research Park, Saffron Walden CB10 1XL, U.K., Convery MA; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Coward JJ; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Doyle K; Charles River Discovery, Chesterford Research Park, Saffron Walden CB10 1XL, U.K., Duempelfeld B; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, Heidelberg 69117, Germany., Edwards CD; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Goldsmith MD; Charles River Discovery, Chesterford Research Park, Saffron Walden CB10 1XL, U.K., Krause J; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, Heidelberg 69117, Germany., Mallett DN; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., McGonagle GA; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Patel VK; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Rowedder J; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Rowland P; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Sharpe A; Charles River Discovery, Chesterford Research Park, Saffron Walden CB10 1XL, U.K., Sriskantharajah S; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Thomas DA; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Thomson DW; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, Heidelberg 69117, Germany., Uddin S; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Hamblin JN; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K., Hessel EM; Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage SG1 2NY, U.K.
Source: Journal of medicinal chemistry [J Med Chem] 2021 Sep 23; Vol. 64 (18), pp. 13780-13792. Date of Electronic Publication: 2021 Sep 11.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.1c01102