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A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Oct 01; Vol. 20 (19), pp. 5753-6. Date of Electronic Publication: 2010 Aug 13. - Publication Year :
- 2010
-
Abstract
- Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Allosteric Regulation
Animals
Binding Sites
Crystallography, X-Ray
Drug Design
Drug Evaluation, Preclinical
High-Throughput Screening Assays
Humans
Indazoles chemical synthesis
Indazoles pharmacology
Microsomes metabolism
Protein Structure, Tertiary
Rats
Receptors, AMPA metabolism
Thiophenes chemical synthesis
Thiophenes pharmacology
Indazoles chemistry
Receptors, AMPA chemistry
Thiophenes chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20805031
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.07.138