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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 02/2020, Volume 30, Issue 4, p. 126811
This Letter details our efforts to develop new M-4 PAM scaffolds with improved pharmacological properties. This endeavor involved replacing the... 
CHEMISTRY, MEDICINAL | M-4 | Positive allosteric modulator (PAM) | PRECLINICAL CANDIDATE | Structure activity relationship (SAR) | CHEMISTRY, ORGANIC | RECEPTOR | POTENTIATORS | Muscarinic acetylcholine receptor
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 02/2020, Volume 30, Issue 3, p. 126812
This Letter details our efforts to discover structurally unique M-4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of... 
CHEMISTRY, MEDICINAL | M-4 | Positive allosteric modulator (PAM) | Structure activity relationship (SAR) | CHEMISTRY, ORGANIC | RECEPTOR | OPTIMIZATION | POTENTIATORS | DERIVATIVES | Muscarinic acetylcholine receptor
Journal Article
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, pp. 1714 - 1718
This letter describes progress towards an M-4 PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the thieno[2,3-c[... 
CHEMISTRY, MEDICINAL | SERIES | SAR | CHEMISTRY, ORGANIC | RECEPTOR | DISCOVERY | CHALLENGES | Muscarinic acetylcholine receptor | Structure-activity relationship (SAR) | M-4 | Positive allosteric modulator (PAM) | OPTIMIZATION | Pharmacokinetics
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2020, Volume 30, Issue 4, p. 126811
[Display omitted] •Discovery of novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide-based M4 PAMs.•Broad survey of diverse heterocyclic cores.•Balanced... 
Structure activity relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2020, Volume 30, Issue 3, p. 126812
[Display omitted] •Discovery of two novel tricyclic-based M4 PAMs.•Utility of scaffold hopping to improve potency/properties/DMPK.•Balanced human and rat M4... 
Structure activity relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2019, Volume 29, Issue 21, p. 126678
[Display omitted] •Novel 2.4-dimehtylcinnoline-based M4 PAMs.•Utility of scaffold hopping to improve properties/DMPK.•Balanced human and rat M4 PAM potency.... 
Structure activity relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, pp. 1714 - 1718
[Display omitted] •First disclosure of VU6005806/AZN-00016130, an M4 PAM profiled as a putative candidate.•Novel SAR findings based on novel variations to the... 
Structure-activity relationship (SAR) | Pharmacokinetics | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2017, Volume 27, Issue 22, pp. 4999 - 5001
[Display omitted] This Letter details our efforts to replace the 3-amino moiety, an essential pharmacophore for M4 PAM activity in most M4 PAMs to date, within... 
Structure-Activity Relationship (SAR) | Positive allosteric modulator (PAM) | M4 | Muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2011, Volume 21, Issue 9, pp. 2697 - 2701
This Letter describes a chemical lead optimization campaign directed at VU0108370, a weak M 1 PAM hit with a novel chemical scaffold from a functional HTS... 
BQCA | Muscarinic | Alzheimer’s disease | Positive allosteric modulator (PAM) | ML169 | Acetylcholine | MLPCN | Alzheimer's disease | CHEMISTRY, MEDICINAL | MUSCARINIC RECEPTORS | GPCRS | CHEMISTRY, ORGANIC
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 01/2010, Volume 20, Issue 2, pp. 558 - 562
This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M -preferring positive allosteric modulator (PAM), discovered... 
Allosteric | Positive allosteric modualtor | Muscarinic receptor | PAM
Journal Article
Journal Article
CURRENT TOPICS IN MEDICINAL CHEMISTRY, ISSN 1568-0266, 2014, Volume 14, Issue 15, pp. 1738 - 1754
There is mounting evidence from preclinical and early proof-of-concept studies suggesting that selective modulation of the M-1 muscarinic receptor is... 
ACTIVATION | CHEMISTRY, MEDICINAL | ALZHEIMERS-DISEASE | CNS | XANOMELINE | positive | MUSCARINIC ACETYLCHOLINE-RECEPTORS | DISCOVERY | Allosteric | quinolone | muscarinic | BQCA | modulator | LIGANDS | ANTAGONISTS | BINDING | Alzheimer's | AGONIST
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 01/2016, Volume 26, Issue 2, pp. 650 - 655
Selective activation of the M-1 receptor via a positive allosteric modulator (PAM) is a new approach for the treatment of the cognitive impairments associated... 
ACTIVATION | CHEMISTRY, MEDICINAL | SERIES | ALZHEIMERS-DISEASE | CHEMISTRY, ORGANIC | SCHIZOPHRENIA | XANOMELINE | Azaindole amide | AGONISTS | DISCOVERY | M-1 selective activator | MUSCARINIC ACETYLCHOLINE-RECEPTOR | M-1 positive allosteric modulator (PAM) | Intra-molecular hydrogen bond (IMHB) | IN-VIVO | CENTRAL-NERVOUS-SYSTEM
Journal Article
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