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Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2019, Volume 62, Issue 1, pp. 378 - 384
A scaffold hopping exercise from a monocyclic mGlu(2) NAM with poor rodent PK led to two novel heterobicyclic series of mGlu(2) NAMs based on either a... 
MGLUR2 | DESIGN | CHEMISTRY, MEDICINAL | RAT | IMMUNOHISTOCHEMICAL LOCALIZATION
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 09/2018, Volume 9, Issue 9, pp. 917 - 922
Herein, we report the chemical optimization of a new series of M1 positive allosteric modulators (PAMs) based on a novel pyrrolo­[2,3-b]­pyridine core,... 
cholinergic toxicity | VU6007477 | Positive allosteric modulator (PAM) | muscarinic acetylcholine receptor 1 (M
Journal Article
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 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of... 
Structure activity relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
ACS MEDICINAL CHEMISTRY LETTERS, ISSN 1948-5875, 09/2018, Volume 9, Issue 9, pp. 917 - 922
Herein, we report the chemical optimization of a new series of M-1 positive allosteric modulators (PAMs) based on a novel pyrrolo[2,3-b]pyridine core,... 
CHEMISTRY, MEDICINAL | ALLOSTERIC MODULATORS | cholinergic toxicity | muscarinic acetylcholine receptor 1 (M-1) | VU6007477 | DISCOVERY | MEMORY | Positive allosteric modulator (PAM) | DISEASE | IMPAIRMENTS | OPTIMIZATION | RECEPTORS | EXPRESSION
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, 08/2019, Volume 29, Issue 16, pp. 2224 - 2228
This letter describes progress towards an M PAM preclinical candidate inspired by an unexpected aldehyde oxidase (AO) metabolite of a novel, CNS penetrant... 
Aldehyde oxidase (AO) | Structure-activity relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor | M
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2019, Volume 29, Issue 16, p. 2224
This letter describes progress towards an M.sub.4 PAM preclinical candidate inspired by an unexpected aldehyde oxidase (AO) metabolite of a novel, CNS... 
Oxidases | Medical colleges | Neurosciences | Pyridine | Metabolites | Lubrication and lubricants | Physiological aspects | Drug discovery | Aldehydes
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2019, Volume 62, Issue 3, pp. 1690 - 1695
Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu ) negative allosteric modulator (NAM)... 
Journal Article
ACS Chemical Neuroscience, ISSN 1948-7193, 03/2019, Volume 10, Issue 3, pp. 1035 - 1042
This Letter describes the chemical optimization of a new series of muscarinic acetylcholine receptor subtype 1 (MO positive allosteric modulators (PAMs) based... 
muscarinic acetylcholine receptor 1 | CNS | Positive allosteric modulator | SAR | PAM | CHEMISTRY, MEDICINAL | SERIES | BIOCHEMISTRY & MOLECULAR BIOLOGY | NEUROSCIENCES | M-1 | IMPAIRMENTS | OPTIMIZATION | AGONIST
Journal Article
ACS Chemical Neuroscience, ISSN 1948-7193, 07/2018, Volume 9, Issue 7, pp. 1572 - 1581
The pharmacology of the M5 muscarinic acetylcholine receptor (mAChR) is the least understood of the five mAChR subtypes due to a historic lack of selective... 
selectivity | SAR | positive allosteric modulator (PAM) | muscarinic acetylcholine receptor
Journal Article
Bioorganic & medicinal chemistry letters, 02/2020, Volume 30, Issue 3, p. 126812
This Letter details our efforts to discover structurally unique M PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of... 
Journal Article
ACS medicinal chemistry letters, ISSN 1948-5875, 12/2017, Volume 8, Issue 12, p. 1326
Herein, we report the structure-activity relationships within a series of mGlu NAMs based on an -(2-(1... 
Journal Article
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