5IU2

Discovery of imidazoquinolines as a novel class of potent, selective and in vivo efficacious COT kinase inhibitors

Replaces:  4Y83Replaces:  4Y85

Summary 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; PubMed: 27502541; DOI: 10.1021/acs.jmedchem.6b00598

Experimental method

X-RAY DIFFRACTION (2.7 Å)