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Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.

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Title: Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
Authors: McCoull W; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Abrams RD; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Anderson E; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Blades K; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Barton P; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Box M; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Burgess J; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Byth K; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Cao Q; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Chuaqui C; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Carbajo RJ; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Cheung T; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Code E; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Ferguson AD; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Fillery S; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Fuller NO; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Gangl E; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Gao N; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Grist M; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Hargreaves D; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Howard MR; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Hu J; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Kemmitt PD; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Nelson JE; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., O'Connell N; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Prince DB; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States., Raubo P; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Rawlins PB; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Robb GR; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Shi J; Pharmaron Beijing Co., Ltd. 6 Taihe Road BDA, Beijing 100176 P. R. China., Waring MJ; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Whittaker D; IMED Oncology, AstraZeneca , Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K., Wylot M; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K., Zhu X; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2017 May 25; Vol. 60 (10), pp. 4386-4402. Date of Electronic Publication: 2017 May 09.
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
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PubType: Academic Journal
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IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Prince+DB%22">Prince DB</searchLink>; IMED Oncology and Discovery Sciences, AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.<br /><searchLink fieldCode="AU" term="%22Raubo+P%22">Raubo P</searchLink>; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.<br /><searchLink fieldCode="AU" term="%22Rawlins+PB%22">Rawlins PB</searchLink>; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.<br /><searchLink fieldCode="AU" term="%22Robb+GR%22">Robb GR</searchLink>; IMED Oncology and Discovery Sciences, AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.<br /><searchLink fieldCode="AU" term="%22Shi+J%22">Shi J</searchLink>; Pharmaron Beijing Co., Ltd. 6 Taihe Road BDA, Beijing 100176 P. 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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2017 May 25; Vol. 60 (10), pp. 4386-4402. <i>Date of Electronic Publication: </i>2017 May 09.
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