Vincent B. Luscombe

发表

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, N. Brandon, 2017, ACS medicinal chemistry letters.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

20 Years an Orphan: Is GPR84 a Plausible Medium-Chain Fatty Acid-Sensing Receptor?

D. Greaves, C. Bataille, A. Russell, 2020, DNA and cell biology.

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).

Anna L. Blobaum, C. Lindsley, P. Conn, 2019, Journal of medicinal chemistry.

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 Cores.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2018, Journal of medicinal chemistry.

VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

Anna L. Blobaum, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.

Anna L. Blobaum, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

VU6010608, a Novel mGlu 7 NAM from a Series of N ‑ (2-(1 H ‑ 1,2,4-Triazol-1-yl)-5-(tri ﬂ uoromethoxy)phenyl)benzamides

Anna L. Blobaum, C. Lindsley, C. Niswender, 2017 .

Neuroprotective activity of new Δ3-N-acylethanolamines in a focal ischemia stroke model.

M. Glass, M. Vyssotski, A. Clarkson, 2021, Lipids.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Evaluation of Synthetic Cytochrome P450-Mimetic Metalloporphyrins To Facilitate “Biomimetic” Biotransformation of a Series of mGlu5 Allosteric Ligands

C. Lindsley, P. Conn, C. Niswender, 2019, ACS omega.

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2017, ACS chemical neuroscience.

Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding

J. Meiler, C. Lindsley, Mariusz Butkiewicz, 2019, ACS Chemical Neuroscience.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Alice E. Berizzi, C. Langmead, P. Sexton, 2018, ACS chemical neuroscience.

Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype.

Julie L. Engers, C. Lindsley, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes.

Julie L. Engers, C. Lindsley, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Alison R. Gregro, Andrew S. Felts, N. Schnetz-Boutaud, 2019, Bioorganic & medicinal chemistry letters.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

C. Lindsley, P. Conn, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & medicinal chemistry letters.

Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Alison R. Gregro, Julie L. Engers, C. Lindsley, 2019, Bioorganic & medicinal chemistry letters.

Discovery of a Novel Class of Heteroaryl-Pyrrolidinones as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1.

Anna L. Blobaum, O. Boutaud, C. Lindsley, 2021, Bioorganic & medicinal chemistry letters.

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

Andrew S. Felts, Brittney S. Bates, Anna L. Blobaum, 2017, Journal of medicinal chemistry.

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

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & Medicinal Chemistry Letters.

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

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & medicinal chemistry letters.

VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2018, ACS medicinal chemistry letters.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Alison R. Gregro, Julie L. Engers, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

N. Brandon, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.

Alison R. Gregro, Andrew S. Felts, N. Brandon, 2019, Bioorganic & medicinal chemistry letters.