Discovery of CVN636 : A Highly Potent, Selective, and CNS Penetrant mGluR 7 Allosteric Agonist.

Autor: Dickson L; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Teall M; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Chevalier E; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Cheung T; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Liwicki GM; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Mack S; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Stephenson A; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., White K; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Fosbeary R; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Harrison DC; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Brice NL; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Doyle K; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Ciccocioppo R; School of Pharmacy, Pharmacology Unit, University of Camerino, Camerino 62032, Italy., Wu C; WuXi Apptec Limited, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China., Almond S; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Patel TR; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Mitchell P; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Barnes M; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Ayscough AP; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Dawson LA; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Carlton M; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.; Takeda Cambridge Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K., Bürli RW; Cerevance Limited, 418 Cambridge Science Park, Cambridge CB4 0PZ, U.K.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2023 Mar 02; Vol. 14 (4), pp. 442-449. Date of Electronic Publication: 2023 Mar 02 (Print Publication: 2023).

Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.

Autor: Clegg MA; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom.; WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Bamborough P; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Chung CW; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Craggs PD; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Gordon L; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Grandi P; Cellzome GmbH, R&D MST GlaxoSmithKline, Meyerhofstrasse 1 69117 Heidelberg, Germany., Leveridge M; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Lindon M; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Liwicki GM; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Michon AM; Cellzome GmbH, R&D MST GlaxoSmithKline, Meyerhofstrasse 1 69117 Heidelberg, Germany., Molnar J; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Rioja I; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Soden PE; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Theodoulou NH; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom.; WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Werner T; Cellzome GmbH, R&D MST GlaxoSmithKline, Meyerhofstrasse 1 69117 Heidelberg, Germany., Tomkinson NCO; WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Prinjha RK; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom., Humphreys PG; GlaxoSmithKline R&D, Stevenage SG1 2NY, Hertfordshire, United Kingdom.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2020 Jun 11; Vol. 63 (11), pp. 5816-5840. Date of Electronic Publication: 2020 May 29.