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Akademický článek

Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

Autor: Tichenor MS; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Wiener JJM; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Rao NL; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Bacani GM; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Wei J; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Pooley Deckhut C; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Barbay JK; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Kreutter KD; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Chang L; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Clancy KW; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Murrey HE; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Wang W; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Ahn K; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Huber M; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Rex E; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Coe KJ; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Wu J; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Rui H; Janssen Research & Development, 4560 Jinke Road, Pudong New Area, Shanghai 201319, P. R. China., Sepassi K; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Gaudiano M; Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Bekkers M; Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Cornelissen I; Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Packman K; Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Seierstad M; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Xiouras C; Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Bembenek SD; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Alexander R; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Milligan C; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Balasubramanian S; Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Lebsack AD; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Venable JD; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Philippar U; Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium., Edwards JP; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Hirst G; Janssen Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121-1126, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 Nov 10; Vol. 65 (21), pp. 14326-14336. Date of Electronic Publication: 2022 Oct 31.

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Akademický článek

Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.

Autor: Tichenor MS; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Wiener JJM; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Rao NL; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Pooley Deckhut C; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Barbay JK; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Kreutter KD; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Bacani GM; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Wei J; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Chang L; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Murrey HE; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Wang W; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Ahn K; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Huber M; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Rex E; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Coe KJ; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Wu J; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Seierstad M; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Bembenek SD; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Leonard KA; Janssen Research & Development, 1400 McKean Road, Spring House, Pennsylvania 19477-0776, United States., Lebsack AD; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Venable JD; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States., Edwards JP; Janssen Research & Development, 3210 Merryfield Row, San Diego, California 92121-1126, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2021 Apr 05; Vol. 12 (5), pp. 782-790. Date of Electronic Publication: 2021 Apr 05 (Print Publication: 2021).

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Akademický článek

Accelerating Lead Identification by High Throughput Virtual Screening: Prospective Case Studies from the Pharmaceutical Industry.

Autor: Damm-Ganamet KL, Arora N, Becart S, Edwards JP, Lebsack AD, McAllister HM, Nelen MI; Discovery Sciences , Janssen Research and Development , Welsh and McKean Roads , Spring House , Pennsylvania 19477 , United States., Rao NL, Westover L; Discovery Sciences , Janssen Research and Development , Welsh and McKean Roads , Spring House , Pennsylvania 19477 , United States., Wiener JJM, Mirzadegan T

Publikováno v: Journal of chemical information and modeling [J Chem Inf Model] 2019 May 28; Vol. 59 (5), pp. 2046-2062. Date of Electronic Publication: 2019 Mar 13.

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Akademický článek

Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein-Protein Interaction.

Autor: Blevitt JM; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , La Jolla, California 92121, United States., Hack MD; Lead Discovery, Discovery Sciences, Janssen R&D LLC , La Jolla, California 92121, United States., Herman KL; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , La Jolla, California 92121, United States., Jackson PF; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , La Jolla, California 92121, United States., Krawczuk PJ; Immunology, Janssen R&D LLC , Spring House, Pennsylvania 19477, United States., Lebsack AD; Immunology, Janssen R&D LLC , La Jolla, California 92121, United States., Liu AX; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , Spring House, Pennsylvania 19477, United States., Mirzadegan T; Lead Discovery, Discovery Sciences, Janssen R&D LLC , La Jolla, California 92121, United States., Nelen MI; Lead Discovery, Discovery Sciences, Janssen R&D LLC , Spring House, Pennsylvania 19477, United States., Patrick AN; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , Spring House, Pennsylvania 19477, United States., Steinbacher S; Proteros Biostructures , 82152 Martinsried, Germany., Milla ME; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , La Jolla, California 92121, United States., Lumb KJ; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC , Spring House, Pennsylvania 19477, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2017 Apr 27; Vol. 60 (8), pp. 3511-3517. Date of Electronic Publication: 2017 Mar 16.

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Akademický článek

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.

Autor: Rech JC; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: jrech2@its.jnj.com., Bhattacharya A; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Branstetter BJ; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Love CJ; Janssen Pharmaceutical Research & Development L.L.C., Turnhoutseweg 30, Beerse, Belgium., Leenaerts JE; Janssen Pharmaceutical Research & Development L.L.C., Turnhoutseweg 30, Beerse, Belgium., Cooymans LP; Janssen Pharmaceutical Research & Development L.L.C., Turnhoutseweg 30, Beerse, Belgium., Eckert WA 3rd; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Ao H; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Wang Q; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Chaplan SR; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Wickenden AD; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Lebsack AD; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States., Breitenbucher JG; Janssen Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Oct 01; Vol. 26 (19), pp. 4781-4784. Date of Electronic Publication: 2016 Aug 20.

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