| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10588332 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) with 15-fold selectivity versus mGlu2. The mGlu3 NAM was discovered via a 'molecular switch' from a closely related, potent mGlu5 positive allosteric modulator (PAM), VU0092273. This NAM (VU0463597, ML289) displays an IC50 value of 0.66 μM and is inactive against mGlu5.
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Authors
Douglas J. Sheffler, Cody J. Wenthur, Joshua A. Bruner, Sheridan J.S. Carrington, Paige N. Vinson, Kiran K. Gogi, Anna L. Blobaum, Ryan D. Morrison, Mitchell Vamos, Nicholas D.P. Cosford, Shaun R. Stauffer, J. Scott Daniels, Colleen M. Niswender,