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  1. Article ; Online: Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.

    Hansen, Bettina Borreschmidt / Jepsen, Tue Heesgaard / Larsen, Mogens / Sindet, Rikke / Vifian, Thomas / Burhardt, Mia Nørreskov / Larsen, Jens / Seitzberg, Jimmi Gerner / Carnerup, Martin A / Jerre, Anders / Mølck, Christina / Lovato, Paola / Rai, Sanjay / Nasipireddy, Venkatarathnam Reddy / Ritzén, Andreas

    Journal of medicinal chemistry

    2020  Volume 63, Issue 13, Page(s) 7008–7032

    Abstract: Herein, we report the discovery of a series of JAK1-selective kinase inhibitors with high potency and excellent JAK family subtype selectivity. A fragment screening ... ...

    Abstract Herein, we report the discovery of a series of JAK1-selective kinase inhibitors with high potency and excellent JAK family subtype selectivity. A fragment screening hit
    MeSH term(s) Drug Design ; Hydrophobic and Hydrophilic Interactions ; Janus Kinase 1/antagonists & inhibitors ; Janus Kinase 1/chemistry ; Janus Kinase 1/metabolism ; Molecular Docking Simulation ; Protein Conformation ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Pyrazoles/chemistry ; Pyridones/chemistry ; Pyridones/metabolism ; Pyridones/pharmacology ; Stereoisomerism ; Substrate Specificity
    Chemical Substances Protein Kinase Inhibitors ; Pyrazoles ; Pyridones ; Janus Kinase 1 (EC 2.7.10.2)
    Language English
    Publishing date 2020-06-08
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c00359
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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  2. Article ; Online: Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.

    Ritzén, Andreas / Sindet, Rikke / Hentzer, Morten / Svendsen, Nannette / Brodbeck, Robbin M / Bundgaard, Christoffer

    Bioorganic & medicinal chemistry letters

    2009  Volume 19, Issue 12, Page(s) 3275–3278

    Abstract: This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC(50)=30 nM) in vitro, and reaches high brain levels in both rats and mice after oral ... ...

    Abstract This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC(50)=30 nM) in vitro, and reaches high brain levels in both rats and mice after oral administration.
    MeSH term(s) Administration, Oral ; Alkynes/chemistry ; Alkynes/pharmacology ; Allosteric Regulation ; Animals ; Brain/metabolism ; Drug Discovery ; Heterocyclic Compounds/chemistry ; Heterocyclic Compounds/pharmacology ; Mice ; Rats ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate/agonists ; Structure-Activity Relationship
    Chemical Substances Alkynes ; Grm5 protein, mouse ; Grm5 protein, rat ; Heterocyclic Compounds ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate
    Language English
    Publishing date 2009-06-15
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2009.04.095
    Database MEDical Literature Analysis and Retrieval System OnLINE

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