2gu8: Difference between revisions
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New page: left|200px<br /><applet load="2gu8" size="350" color="white" frame="true" align="right" spinBox="true" caption="2gu8, resolution 2.20Å" /> '''Discovery of 2-Pyrim... |
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==Overview== | ==Overview== | ||
A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and | A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and evaluated for AKT inhibition. SAR studies resulted in potent inhibitors of AKT with IC(50) values as low as single digit nanomolar as represented by compound 2aa. Compound 2aa showed cellular activity including antiproliferation and downstream target modulation. Selectivity profile is described. A co-crystal of 2aa with PKA is determined and discussed. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Murray, J | [[Category: Murray, J M.]] | ||
[[Category: 796]] | [[Category: 796]] | ||
[[Category: akt]] | [[Category: akt]] | ||
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[[Category: ternary complex]] | [[Category: ternary complex]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:35:27 2008'' | ||
