5IU2
Discovery of imidazoquinolines as a novel class of potent, selective and in vivo efficacious COT kinase inhibitors
Replaces: 4Y83Replaces: 4Y85Summary for 5IU2
Entry DOI | 10.2210/pdb5iu2/pdb |
Descriptor | Mitogen-activated protein kinase kinase kinase 8, N-[2-(morpholin-4-yl)ethyl]-6-(8-phenyl-1H-imidazo[4,5-c][1,7]naphthyridin-1-yl)-1,3-benzothiazol-2-amine (3 entities in total) |
Functional Keywords | cot, tpl-2, map3k8, kinase, inhibitor, complex, transferase |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm : P41279 |
Total number of polymer chains | 2 |
Total formula weight | 76285.62 |
Authors | Gutmann, S.,Hinniger, A. (deposition date: 2016-03-17, release date: 2016-08-24, Last modification date: 2024-02-07) |
Primary citation | Glatthar, R.,Stojanovic, A.,Troxler, T.,Mattes, H.,Mobitz, H.,Beerli, R.,Blanz, J.,Gassmann, E.,Druckes, P.,Fendrich, G.,Gutmann, S.,Martiny-Baron, G.,Spence, F.,Hornfeld, J.,Peel, J.E.,Sparrer, H. Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J.Med.Chem., 59:7544-7560, 2016 Cited by PubMed: 27502541DOI: 10.1021/acs.jmedchem.6b00598 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.7 Å) |
Structure validation
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