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Journal of Medicinal Chemistry|August 23, 2014
Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)Patrick R Gentry, Masaya Kokubo, Thomas M Bridges, et al.Bioorganic & Medicinal Chemistry Letters|January 4, 2011
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probePaul R Reid, Thomas M Bridges, Douglas J Sheffler, et al.Bioorganic & Medicinal Chemistry Letters|December 4, 2012
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonismDouglas J Sheffler, Christian Sevel, Uyen Le, et al.ACS Chemical Biology|August 20, 2014
Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenicsHyekyung P Cho, Pedro M Garcia-Barrantes, John T Brogan, et al.Journal of Medicinal Chemistry|April 17, 2014
Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependenceRaveendra-Panickar Dhanya, Douglas J Sheffler, Russell Dahl, et al.ACS Medicinal Chemistry Letters|September 28, 2018
VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse EventsJulie L Engers, Elizabeth S Childress, Madeline F Long, et al.Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology|March 28, 2018
M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognitionSean P Moran, Jonathan W Dickerson, Hyekyung P Cho, et al.Journal of Medicinal Chemistry|October 30, 2013
Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)Patrick R Gentry, Masaya Kokubo, Thomas M Bridges, et al.Journal of Medicinal Chemistry|October 24, 2018
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide CoresElizabeth S Childress, Joshua M Wieting, Andrew S Felts, et al.Bioorganic & Medicinal Chemistry Letters|May 15, 2018
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine coreJeanette L Bertron, Hyekyung P Cho, Pedro M Garcia-Barrantes, et al.Pageof 30