5LXD
Crystal structure of DYRK2 in complex with EHT 1610 (compound 2)
Summary for 5LXD
| Entry DOI | 10.2210/pdb5lxd/pdb |
| Descriptor | Dual specificity tyrosine-phosphorylation-regulated kinase 2, methyl 9-[(2-fluoranyl-4-methoxy-phenyl)amino]-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate, 1,2-ETHANEDIOL, ... (4 entities in total) |
| Functional Keywords | transferase, kinase, inhibitor, unusual binding mode, structural genomics, structural genomics consortium, sgc |
| Biological source | Homo sapiens (Human) |
| Cellular location | Cytoplasm: Q92630 |
| Total number of polymer chains | 2 |
| Total formula weight | 95326.06 |
| Authors | Chaikuad, A.,von Delft, F.,Arrowsmith, C.H.,Edwards, A.,Bountra, C.,Besson, T.,Knapp, S.,Structural Genomics Consortium (SGC) (deposition date: 2016-09-20, release date: 2016-10-26, Last modification date: 2017-01-11) |
| Primary citation | Chaikuad, A.,Diharce, J.,Schroder, M.,Foucourt, A.,Leblond, B.,Casagrande, A.S.,Desire, L.,Bonnet, P.,Knapp, S.,Besson, T. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J. Med. Chem., 59:10315-10321, 2016 Cited by PubMed: 27766861DOI: 10.1021/acs.jmedchem.6b01083 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.58 Å) |
Structure validation
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