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Publication Date Publication Date
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Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 03/2010, Volume 20, Issue 6, pp. 1972 - 1975
This Letter describes a chemical lead optimization campaign directed at VU0119498, a pan G mAChR M , M , M positive allosteric modulator (PAM) with the goal of... 
Acetylcholine | Muscarinic | PAM | mAChR | Structure-Activity Relationship | Receptors, Muscarinic - drug effects | Allosteric Regulation | Cholinergic Agents - pharmacology | Cholinergic Agents - chemistry | Drug Design
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 of Medicinal Chemistry, ISSN 0022-2623, 10/2013, Volume 56, Issue 20, pp. 7976 - 7996
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
NEUROPHARMACOLOGY, ISSN 0028-3908, 01/2018, Volume 128, pp. 492 - 502
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2019, Volume 29, Issue 21, p. 126678
This Letter details our efforts to replace the 2,4-dimethylquinoline carboxamide core of our previous M PAM series, which suffered from high predicted hepatic... 
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
This letter describes progress towards an M PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the thieno[2,3-... 
Structure-activity relationship (SAR) | Pharmacokinetics | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
ACS MEDICINAL CHEMISTRY LETTERS, ISSN 1948-5875, 02/2017, Volume 8, Issue 2, pp. 233 - 238
Herein, we report the structure-activity relationships within a series of potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M-4)... 
POSITIVE ALLOSTERIC MODULATOR | CHEMISTRY, MEDICINAL | Positive allosteric modulator (PAM) | VU0467485 | DISEASE | muscarinic acetylcholine receptor 4 (M-4) | XANOMELINE | schizophrenia | MUSCARINIC RECEPTOR AGONIST
Journal Article
EMBO reports, ISSN 1469-221X, 09/2019, Volume 20, Issue 9
Journal Article
Neuropharmacology, ISSN 0028-3908, 01/2018, Volume 128, pp. 492 - 502
Although selective activation of the M muscarinic acetylcholine receptor (mAChR) subtype has been shown to improve cognitive function in animal models of... 
M4 muscarinic acetylcholine receptor | MK-801 | Positive allosteric modulator | Cognitive enhancement | Antipsychotic-like activity | VU0467154 | muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2017, Volume 27, Issue 22, pp. 4999 - 5001
This Letter details our efforts to replace the 3-amino moiety, an essential pharmacophore for M PAM activity in most M PAMs to date, within the thieno[2,3-... 
Structure-Activity Relationship (SAR) | Positive allosteric modulator (PAM) | 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 PAM hit with a novel chemical scaffold from a functional HTS screen... 
BQCA | Muscarinic | Alzheimer’s disease | Positive allosteric modulator (PAM) | ML169 | Acetylcholine | MLPCN | Alzheimer's disease | CHEMISTRY, MEDICINAL | MUSCARINIC RECEPTORS | GPCRS | CHEMISTRY, ORGANIC
Journal Article