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Discovery of Molecular Switches Within the ADX-47273 mGlu5 PAM Scaffold That Modulate Modes of Pharmacology to Afford Potent mGlu5 NAMs, PAMs and Partial Antagonists

Jeffrey P Lamb, Darren W Engers, Colleen M Niswender, Alice L Rodriguez, Daryl F Venable, P Jeffrey Conn, Craig W Lindsley

Bioorg Med Chem Lett. 2011 May 1;21(9):2711-4.

PMID: 21183344

Abstract:

This Letter describes a chemical lead optimization campaign directed at a weak mGlu(5) NAM discovered while developing SAR for the mGlu(5) PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu(5) NAMs, mGlu(5) PAMs as well as mGlu(5) partial antagonists.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP851881602 ADX-47273 ADX-47273 851881-60-2 Price
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