| Structural highlights
2x8e 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: | ,
| | Related: | 2wmt, 2cgx, 2c3j, 2bro, 2brb, 2wmw, 2wmu, 2wmr, 2brh, 2cgv, 2c3k, 1nvr, 2wmq, 1zlt, 2cgw, 2brn, 2wmx, 2ayp, 1zys, 2cgu, 1ia8, 2br1, 2brg, 1nvs, 1nvq, 2brm, 2wmv, 2wms, 2c3l, 2x8d, 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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ 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. Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors--hit to lead exploration. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. Epub 2010 Jul 29. PMID:20673630 doi:10.1016/j.bmcl.2010.07.015
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