Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia MR Wood, MJ Noetzel, BJ Melancon, MS Poslusney, KD Nance, ... ACS medicinal chemistry letters 8 (2), 233-238, 2017 | 55 | 2017 |
Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs JM Rook, M Abe, HP Cho, KD Nance, VB Luscombe, JJ Adams, ... ACS chemical neuroscience 8 (4), 866-883, 2017 | 52 | 2017 |
20 years an orphan: is GPR84 a plausible medium-chain fatty acid-sensing receptor? VB Luscombe, D Lucy, CJR Bataille, AJ Russell, DR Greaves DNA and Cell Biology 39 (11), 1926-1937, 2020 | 36 | 2020 |
Challenges in the development of an M4 PAM in vivo tool compound: the discovery of VU0467154 and unexpected DMPK profiles of close analogs MR Wood, MJ Noetzel, MS Poslusney, BJ Melancon, JC Tarr, A Lamsal, ... Bioorganic & medicinal chemistry letters 27 (2), 171-175, 2017 | 32 | 2017 |
Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines M Abe, M Seto, RG Gogliotti, MT Loch, KA Bollinger, S Chang, ... ACS Medicinal Chemistry Letters 8 (10), 1110-1115, 2017 | 31 | 2017 |
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate … AS Felts, AL Rodriguez, AL Blobaum, RD Morrison, BS Bates, ... Journal of Medicinal Chemistry 60 (12), 5072-5085, 2017 | 30 | 2017 |
Discovery of a novel 2, 4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping MF Long, JL Engers, S Chang, X Zhan, RL Weiner, VB Luscombe, ... Bioorganic & medicinal chemistry letters 27 (22), 4999-5001, 2017 | 28 | 2017 |
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides JC Tarr, MR Wood, MJ Noetzel, BJ Melancon, A Lamsal, VB Luscombe, ... Bioorganic & medicinal chemistry letters 27 (23), 5179-5184, 2017 | 27 | 2017 |
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 … CW Reed, SE Yohn, JP Washecheck, HF Roenfanz, MC Quitalig, ... Journal of medicinal chemistry 62 (3), 1690-1695, 2019 | 26 | 2019 |
Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl) quinoline-3-carbonitrile core BR Bewley, PK Spearing, RL Weiner, VB Luscombe, X Zhan, S Chang, ... Bioorganic & medicinal chemistry letters 27 (18), 4274-4279, 2017 | 25 | 2017 |
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1 … ES Childress, JM Wieting, AS Felts, MM Breiner, MF Long, VB Luscombe, ... Journal of Medicinal Chemistry 62 (1), 378-384, 2018 | 23 | 2018 |
VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides CW Reed, KM McGowan, PK Spearing, BJ Stansley, HF Roenfanz, ... ACS Medicinal Chemistry Letters 8 (12), 1326-1330, 2017 | 21 | 2017 |
VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events JL Engers, ES Childress, MF Long, RA Capstick, VB Luscombe, HP Cho, ... ACS medicinal chemistry letters 9 (9), 917-922, 2018 | 15 | 2018 |
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl) piperazin-1-yl)-6-(piperidin-1-yl) pyridazines as novel, CNS penetrant pan-muscarinic antagonists AM Bender, RL Weiner, VB Luscombe, S Ajmera, HP Cho, S Chang, ... Bioorganic & medicinal chemistry letters 27 (15), 3576-3581, 2017 | 13 | 2017 |
Discovery of a novel 3, 4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping KJ Temple, JL Engers, MF Long, AR Gregro, KJ Watson, S Chang, ... Bioorganic & Medicinal Chemistry Letters 29 (21), 126678, 2019 | 10 | 2019 |
Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators JL Engers, AM Bender, JJ Kalbfleisch, HP Cho, KS Lingenfelter, ... ACS chemical neuroscience 10 (3), 1035-1042, 2018 | 10 | 2018 |
Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide … AM Bender, HP Cho, KD Nance, KS Lingenfelter, VB Luscombe, ... ACS chemical neuroscience 9 (7), 1572-1581, 2018 | 10 | 2018 |
VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate DW Engers, BJ Melancon, AR Gregro, JL Bertron, SR Bollinger, AS Felts, ... Bioorganic & Medicinal Chemistry Letters 29 (14), 1714-1718, 2019 | 7 | 2019 |
Bioorg Med Chem Lett JC Tarr, MR Wood, MJ Noetzel, BJ Melancon, V Luscombe, AL Rodriguez, ... submitted.[Google Scholar], 0 | 5 | |
Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes KJ Temple, MF Long, JL Engers, KJ Watson, S Chang, VB Luscombe, ... Bioorganic & Medicinal Chemistry Letters 30 (4), 126811, 2020 | 4 | 2020 |