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3o6g

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3o6g, resolution 1.80Å ()
Ligands: , , ,
Gene: Gria2, Glur2 (Rattus norvegicus)
Related: 3o28, 3o29, 3o2a, 3o6h, 3o6i, 3pmv, 3pmw, 3pmx


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator

Publication Abstract from PubMed

Starting from lead compound 1, we demonstrate how X-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity.

A novel series of positive modulators of the AMPA receptor: Structure-based lead optimization., Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L, Bioorg Med Chem Lett. 2010 Aug 15. PMID:20817521

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

3o6g is a 1 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

See Also

Reference

  • Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L. A novel series of positive modulators of the AMPA receptor: Structure-based lead optimization. Bioorg Med Chem Lett. 2010 Aug 15. PMID:20817521 doi:10.1016/j.bmcl.2010.08.063
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