2r0u

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[[Image:2r0u.gif|left|200px]]
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{{STRUCTURE_2r0u| PDB=2r0u | SCENE= }}
{{STRUCTURE_2r0u| PDB=2r0u | SCENE= }}
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'''Crystal Structure of Chek1 in Complex with Inhibitor 54'''
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===Crystal Structure of Chek1 in Complex with Inhibitor 54===
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==Overview==
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From HTS lead 1, a novel benzoisoquinolinone class of ATP-competitive Chk1 inhibitors was devised and synthesized via a photochemical route. Using X-ray crystallography as a guide, potency was rapidly enhanced through the installation of a tethered basic amine designed to interact with an acidic residue (Glu91) in the enzyme pocket. Further SAR was explored at the solvent front and near to the H1 pocket and resulted in the discovery of low MW, sub-nanomolar inhibitors of Chk1.
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(as it appears on PubMed at http://www.pubmed.gov), where 17900896 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17900896}}
==About this Structure==
==About this Structure==
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[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Ubl conjugation]]
[[Category: Ubl conjugation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 16:02:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 04:04:10 2008''

Revision as of 01:04, 28 July 2008

Image:2r0u.png

Template:STRUCTURE 2r0u

Crystal Structure of Chek1 in Complex with Inhibitor 54

Template:ABSTRACT PUBMED 17900896

About this Structure

2R0U is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase., Garbaccio RM, Huang S, Tasber ES, Fraley ME, Yan Y, Munshi S, Ikuta M, Kuo L, Kreatsoulas C, Stirdivant S, Drakas B, Rickert K, Walsh ES, Hamilton KA, Buser CA, Hardwick J, Mao X, Beck SC, Abrams MT, Tao W, Lobell R, Sepp-Lorenzino L, Hartman GD, Bioorg Med Chem Lett. 2007 Nov 15;17(22):6280-5. Epub 2007 Sep 7. PMID:17900896

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