PMID
Data
Article Title
Organization
Continued optimization of the M

Vanderbilt University School of Medicine
Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Vanderbilt University
Challenges in the development of an M

Vanderbilt University Medical Center
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.

Vanderbilt University Medical Center
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.

Vanderbilt University Medical Center
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.

Vanderbilt University Medical Center
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.

Vanderbilt University Medical Center
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics

Vanderbilt University
Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

Vanderbilt University Medical Center
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).

Vanderbilt University Medical Center
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 dependence.

Sanford-Burnham Medical Research Institute
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).

Vanderbilt University
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

Vanderbilt University Medical Center
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.

Vanderbilt University Medical Center
Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.

Vanderbilt University Medical Center
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Vanderbilt University Medical Center
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

Vanderbilt University Medical Center
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

Vanderbilt Institute of Chemical Biology/Chemical Synthesis Core
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

Vanderbilt University Medical Center
Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M5 Muscarinic Acetylcholine Receptor.

Vanderbilt University
Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.

Vanderbilt University
Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.

Vanderbilt University
Discovery of a potent M

Vanderbilt University
Development of

Vanderbilt University
Discovery of structurally distinct tricyclic M

Vanderbilt University
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M

Vanderbilt University School of Medicine
Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.

Vanderbilt University
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M

Vanderbilt University
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu

Vanderbilt University School of Medicine
Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

Vanderbilt University Medical Center
VU6007477, a Novel M

Vanderbilt Univercity
Challenges in the development of an M

Vanderbilt University School of Medicine
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M

Vanderbilt University
The discovery of VU0486846: steep SAR from a series of M

Vanderbilt University Medical Center
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.

Vanderbilt University School of Medicine
Discovery of a novel, CNS penetrant M

Vanderbilt University
Challenges in the development of an M

Vanderbilt University School of Medicine
Optimization of M

Vanderbilt University Medical Center
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.

Vanderbilt University School of Medicine
Indoline compounds as aldosterone synthase inhibitors

Merck Sharp & Dohme