2gu8

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{{STRUCTURE_2gu8| PDB=2gu8 | SCENE= }}
{{STRUCTURE_2gu8| PDB=2gu8 | SCENE= }}
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'''Discovery of 2-Pyrimidyl-5-Amidothiophenes as Novel and Potent Inhibitors for AKT: Synthesis and SAR Studies'''
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===Discovery of 2-Pyrimidyl-5-Amidothiophenes as Novel and Potent Inhibitors for AKT: Synthesis and SAR Studies===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16765046 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16765046}}
==About this Structure==
==About this Structure==
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[[Category: Pka]]
[[Category: Pka]]
[[Category: Ternary complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:32:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 12:44:40 2008''

Revision as of 09:44, 29 July 2008

Template:STRUCTURE 2gu8

Discovery of 2-Pyrimidyl-5-Amidothiophenes as Novel and Potent Inhibitors for AKT: Synthesis and SAR Studies

Template:ABSTRACT PUBMED 16765046

About this Structure

Full crystallographic information is available from OCA.

Reference

Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies., Lin X, Murray JM, Rico AC, Wang MX, Chu DT, Zhou Y, Del Rosario M, Kaufman S, Ma S, Fang E, Crawford K, Jefferson AB, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4163-8. Epub 2006 Jun 9. PMID:16765046

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