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Discovery of Pyrimidoindolones as Novel Family VIII Bromodomain Binders.

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Title: Discovery of Pyrimidoindolones as Novel Family VIII Bromodomain Binders.
Authors: Boerth JA; Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States., Schimpl M; Protein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Lucas SCC; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Zhang J; Bioscience, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States., Code EL; Assays and Profiling, Discovery Sciences, R&D, AstraZeneca, Waltham, Massachusetts 02451, United States., Embrey KJ; New Modalities & Parenteral Development, PT&D, Operations, AstraZeneca, Macclesfield SK10 2NA, U.K., Rawlins PB; Protein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Wang H; Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States., Storer RI; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Di Fruscia P; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Nelson JE; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Milbradt AG; Mechanistic and Structural Biology, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Börjesson U; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Gothenburg SE-43183, Sweden., Gohlke A; Protein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K., Korboukh V; Assays and Profiling, Discovery Sciences, R&D, AstraZeneca, Waltham, Massachusetts 02451, United States., Gopalsamy A; Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.
Source: ACS medicinal chemistry letters [ACS Med Chem Lett] 2025 May 08; Vol. 16 (6), pp. 1073-1079. Date of Electronic Publication: 2025 May 08 (Print Publication: 2025).
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE
Database: MEDLINE Ultimate
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  Data: Discovery of Pyrimidoindolones as Novel Family VIII Bromodomain Binders.
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  Data: <searchLink fieldCode="AU" term="%22Boerth+JA%22">Boerth JA</searchLink>; Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Schimpl+M%22">Schimpl M</searchLink>; Protein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Lucas+SCC%22">Lucas SCC</searchLink>; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Zhang+J%22">Zhang J</searchLink>; Bioscience, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Code+EL%22">Code EL</searchLink>; Assays and Profiling, Discovery Sciences, R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Embrey+KJ%22">Embrey KJ</searchLink>; New Modalities & Parenteral Development, PT&D, Operations, AstraZeneca, Macclesfield SK10 2NA, U.K.<br /><searchLink fieldCode="AU" term="%22Rawlins+PB%22">Rawlins PB</searchLink>; Protein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Wang+H%22">Wang H</searchLink>; Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Storer+RI%22">Storer RI</searchLink>; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Di+Fruscia+P%22">Di Fruscia P</searchLink>; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Nelson+JE%22">Nelson JE</searchLink>; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Milbradt+AG%22">Milbradt AG</searchLink>; Mechanistic and Structural Biology, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Börjesson+U%22">Börjesson U</searchLink>; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Gothenburg SE-43183, Sweden.<br /><searchLink fieldCode="AU" term="%22Gohlke+A%22">Gohlke A</searchLink>; Protein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.<br /><searchLink fieldCode="AU" term="%22Korboukh+V%22">Korboukh V</searchLink>; Assays and Profiling, Discovery Sciences, R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Gopalsamy+A%22">Gopalsamy A</searchLink>; Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.
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  Data: <searchLink fieldCode="JN" term="%22101521073%22">ACS medicinal chemistry letters</searchLink> [ACS Med Chem Lett] 2025 May 08; Vol. 16 (6), pp. 1073-1079. <i>Date of Electronic Publication: </i>2025 May 08 (<i>Print Publication: </i>2025).
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