2no3
From Proteopedia
(New page: 200px<br /> <applet load="2no3" size="450" color="white" frame="true" align="right" spinBox="true" caption="2no3, resolution 3.20Å" /> '''Novel 4-anilinopyri...) |
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| - | [[Image:2no3.gif|left|200px]]<br /> | + | [[Image:2no3.gif|left|200px]]<br /><applet load="2no3" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2no3" size=" | + | |
caption="2no3, resolution 3.20Å" /> | caption="2no3, resolution 3.20Å" /> | ||
'''Novel 4-anilinopyrimidines as potent JNK1 Inhibitors'''<br /> | '''Novel 4-anilinopyrimidines as potent JNK1 Inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A new series of 4-anilinopyrimidines has been synthesized and evaluated as | + | A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are also described. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2NO3 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and 859 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http:// | + | 2NO3 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=859:'>859</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Mitogen-activated_protein_kinase Mitogen-activated protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.24 2.7.11.24] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2NO3 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: jnk1 inhibitors]] | [[Category: jnk1 inhibitors]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:09:06 2008'' |
Revision as of 16:09, 21 February 2008
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Novel 4-anilinopyrimidines as potent JNK1 Inhibitors
Contents |
Overview
A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are also described.
Disease
Known disease associated with this structure: Diabetes mellitus, noninsulin-dependent OMIM:[604641]
About this Structure
2NO3 is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Mitogen-activated protein kinase, with EC number 2.7.11.24 Full crystallographic information is available from OCA.
Reference
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies., Liu M, Wang S, Clampit JE, Gum RJ, Haasch DL, Rondinone CM, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G, Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72. Epub 2006 Nov 2. PMID:17107797
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