2qhn

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[[Image:2qhn.jpg|left|200px]]
[[Image:2qhn.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2qhn |SIZE=350|CAPTION= <scene name='initialview01'>2qhn</scene>, resolution 1.70&Aring;
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The line below this paragraph, containing "STRUCTURE_2qhn", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:582+Binding+Site+For+Residue+A+500'>AC1</scene>
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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=582:5-ETHYL-3-METHYL-1,5-DIHYDRO-4H-PYRAZOLO[4,3-C]QUINOLIN-4-ONE'>582</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/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2qhn| PDB=2qhn | SCENE= }}
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|RELATEDENTRY=[[2qhm|2QHM]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2qhn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qhn OCA], [http://www.ebi.ac.uk/pdbsum/2qhn PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2qhn RCSB]</span>
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}}
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'''Crystal Structure of Chek1 in Complex with Inhibitor 1a'''
'''Crystal Structure of Chek1 in Complex with Inhibitor 1a'''
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[[Category: Munshi, S.]]
[[Category: Munshi, S.]]
[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
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[[Category: cell cycle checkpoint]]
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[[Category: Cell cycle checkpoint]]
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[[Category: chek1]]
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[[Category: Chek1]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:58:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:49:26 2008''
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Revision as of 11:58, 4 May 2008

Image:2qhn.jpg

Template:STRUCTURE 2qhn

Crystal Structure of Chek1 in Complex with Inhibitor 1a


Overview

The development of 2,5-dihydro-4H-pyrazolo[4,3-c]quinolin-4-ones as inhibitors of Chk1 kinase is described. Introduction of a fused ring at the C7/C8 positions of the pyrazoloquinolinone provided an increase in potency while guidance from overlapping inhibitor bound Chk1 X-ray crystal structures contributed to the discovery of a potent and solubilizing propyl amine moiety in compound 52 (Chk1 IC(50)=3.1 nM).

About this Structure

2QHN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors., Brnardic EJ, Garbaccio RM, Fraley ME, Tasber ES, Steen JT, Arrington KL, Dudkin VY, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5989-94. Epub 2007 Aug 19. PMID:17804227 Page seeded by OCA on Sun May 4 14:58:57 2008

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OCA

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