2no3

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[[Image:2no3.gif|left|200px]]
[[Image:2no3.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2no3 |SIZE=350|CAPTION= <scene name='initialview01'>2no3</scene>, resolution 3.20&Aring;
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The line below this paragraph, containing "STRUCTURE_2no3", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=859:2-({2-[(3-HYDROXYPHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)BENZAMIDE'>859</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= MAPK8, JNK1, PRKM8 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2no3| PDB=2no3 | SCENE= }}
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|RELATEDENTRY=[[2g01|2g01]], [[2gmx|2gmx]], [[2h96|2h96]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2no3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2no3 OCA], [http://www.ebi.ac.uk/pdbsum/2no3 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2no3 RCSB]</span>
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}}
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'''Novel 4-anilinopyrimidines as potent JNK1 Inhibitors'''
'''Novel 4-anilinopyrimidines as potent JNK1 Inhibitors'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Abad-Zapatero, C.]]
[[Category: Abad-Zapatero, C.]]
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[[Category: anilinopyrimidines jnk1 inhibitor]]
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[[Category: Anilinopyrimidines jnk1 inhibitor]]
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[[Category: c-jun n-terminal kinase]]
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[[Category: C-jun n-terminal kinase]]
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[[Category: jnk1]]
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[[Category: Jnk1]]
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[[Category: jnk1 inhibitor]]
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[[Category: Jnk1 inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 09:41:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:05:49 2008''
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Revision as of 06:41, 4 May 2008

Template:STRUCTURE 2no3

Novel 4-anilinopyrimidines as potent JNK1 Inhibitors


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.

About this Structure

2NO3 is a Single protein structure of sequence from Homo sapiens. 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 Page seeded by OCA on Sun May 4 09:41:32 2008

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