2ovy: Difference between revisions

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[[Image:2ovy.gif|left|200px]]
{{Seed}}
[[Image:2ovy.png|left|200px]]


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{{STRUCTURE_2ovy|  PDB=2ovy  |  SCENE=  }}  
{{STRUCTURE_2ovy|  PDB=2ovy  |  SCENE=  }}  


'''Crystal structure of the catalytic domain of rat phosphodiesterase 10A'''
===Crystal structure of the catalytic domain of rat phosphodiesterase 10A===




==Overview==
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A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A.
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==About this Structure==
==About this Structure==
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[[Category: Phosphodiesterase 10a]]
[[Category: Phosphodiesterase 10a]]
[[Category: Zn-binding site]]
[[Category: Zn-binding site]]
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