3nus
From Proteopedia
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3nus FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3nus OCA], [http://pdbe.org/3nus PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3nus RCSB], [http://www.ebi.ac.uk/pdbsum/3nus PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3nus ProSAT]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3nus FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3nus OCA], [http://pdbe.org/3nus PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3nus RCSB], [http://www.ebi.ac.uk/pdbsum/3nus PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3nus ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Fragment screening of phosphoinositide-dependent kinase-1 (PDK1) in a biochemical kinase assay afforded hits that were characterized and prioritized based on ligand efficiency and binding interactions with PDK1 as determined by NMR. Subsequent crystallography and follow-up screening led to the discovery of aminoindazole 19, a potent leadlike PDK1 inhibitor with high ligand efficiency. Well-defined structure-activity relationships and protein crystallography provide a basis for further elaboration and optimization of 19 as a PDK1 inhibitor. | ||
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| + | Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.,Medina JR, Blackledge CW, Heerding DA, Campobasso N, Ward P, Briand J, Wright L, Axten JM ACS Med Chem Lett. 2010 Jul 22;1(8):439-42. doi: 10.1021/ml100136n. eCollection, 2010 Nov 11. PMID:24900229<ref>PMID:24900229</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 3nus" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
*[[3-phosphoinositide-dependent protein kinase 1|3-phosphoinositide-dependent protein kinase 1]] | *[[3-phosphoinositide-dependent protein kinase 1|3-phosphoinositide-dependent protein kinase 1]] | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Revision as of 08:18, 10 October 2018
phosphoinositide-dependent kinase-1 (PDK1) with fragment8
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