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

Structural highlights

3pmx is a 1 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.87Å
Ligands:, , , , ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Publication Abstract from PubMed

Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.

Structure based evolution of a novel series of positive modulators of the AMPA receptor.,Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. Epub 2010 Nov 25. PMID:21190850[1]

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

See Also

References

  1. Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L. Structure based evolution of a novel series of positive modulators of the AMPA receptor. Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. Epub 2010 Nov 25. PMID:21190850 doi:10.1016/j.bmcl.2010.11.098

3pmx, resolution 1.87Å

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