2x8d | pdb_00002x8d

DISCOVERY OF A NOVEL CLASS OF TRIAZOLONES AS CHECKPOINT KINASE INHIBITORS - HIT TO LEAD EXPLORATION

spinqualitylabelsall models 2x8d, resolution 1.90Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2x8d is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: SO4, X8D Related: 2wmt, 2cgx, 2c3j, 2bro, 2brb, 2wmw, 2wmu, 2wmr, 2brh, 2cgv, 1nvr, 2c3k, 2wmq, 2cgw, 1zlt, 2brn, 2ayp, 2wmx, 1zys, 2cgu, 2br1, 1ia8, 2brg, 1nvs, 2brm, 1nvq, 2wmv, 2wms, 2c3l, 2x8e, 2x8i Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described. Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors--hit to lead exploration.,Oza V, Ashwell S, Brassil P, Breed J, Deng C, Ezhuthachan J, Haye H, Horn C, Janetka J, Lyne P, Newcombe N, Otterbien L, Pass M, Read J, Roswell S, Su M, Toader D, Yu D, Yu Y, Valentine A, Webborn P, White A, Zabludoff S, Zheng X Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. Epub 2010 Jul 29. PMID:20673630 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Serine/threonine protein kinase

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