ArticleBioorganic & medicinal chemistry letters2017
Challenges in the development of an M
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Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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22citing papers in PubMed
–field-weighted citation impact
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
22 citing papers in PubMed.
- Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct MACS chemical neuroscience · 2026Article
- Discovery of Pre-Clinical CandidateACS chemical neuroscience · 2025Article
- A golden age of muscarinic acetylcholine receptor modulation in neurological diseases.Nature reviews. Drug discovery · 2024Review
- Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic MACS chemical neuroscience · 2024Article
- PET imaging of M4 muscarinic acetylcholine receptors in rhesus macaques using [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2024Article
- Design, synthesis and evaluation of novel 2-phenyl-3-(1H-pyrazol-4-yl)pyridine positive allosteric modulators for the MEuropean journal of medicinal chemistry · 2023Article
- Article
- The pyridazine heterocycle in molecular recognition and drug discovery.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2023Review
- Persistent challenges in the development of an mGluBioorganic & medicinal chemistry letters · 2023Article
- Drug Design Targeting the Muscarinic Receptors and the Implications in Central Nervous System Disorders.Biomedicines · 2022Review
- Acetylcholine Muscarinic MBiological psychiatry · 2020Article
- Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias.Frontiers in pharmacology · 2020Review
- Targeting Muscarinic Acetylcholine Receptors for the Treatment of Psychiatric and Neurological Disorders.Trends in pharmacological sciences · 2019Review
- Novel MBioorganic & medicinal chemistry letters · 2019Article
- Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.Journal of medicinal chemistry · 2019Review
- PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems.ACS chemical neuroscience · 2018Article
- Positive allosteric modulation of MNeuropharmacology · 2018Review
- Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the MThe Journal of pharmacology and experimental therapeutics · 2018Article
- Challenges in the development of an MBioorganic & medicinal chemistry letters · 2017Article
- Challenges in the development of an MBioorganic & medicinal chemistry letters · 2017Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
20 authors.
Michael R WoodVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA.
Meredith J NoetzelVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Michael S PoslusneyVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Bruce J MelanconVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
James C TarrVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Atin LamsalVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Sichen ChangVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Vincent B LuscombeVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Rebecca L WeinerVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Hyekyung P ChoVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Michael BubserVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Carrie K JonesVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Vanderbilt Kennedy Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Colleen M NiswenderVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Vanderbilt Kennedy Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Michael W WoodNeuroscience Innovative Medicines, Astra Zeneca, 141 Portland Street, Cambridge, MA 02139, USA.
Darren W EngersVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Nicholas J BrandonNeuroscience Innovative Medicines, Astra Zeneca, 141 Portland Street, Cambridge, MA 02139, USA.
Mark E DugganNeuroscience Innovative Medicines, Astra Zeneca, 141 Portland Street, Cambridge, MA 02139, USA.
P Jeffrey ConnVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Vanderbilt Kennedy Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Thomas M BridgesVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA. Electronic address: thomas.m.bridges@vanderbilt.edu.
Craig W LindsleyVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA. Electronic address: craig.lindsley@vanderbilt.edu.
Funding
The Vanderbilt Specialized Chemistry Center for Accelerated Probe DevelopmentU54MH084659 · NIMH · VANDERBILT UNIVERSITY · PI MEILER, JENS · 2008 to 2013
$24.1MVanderbilt NCDDDG for Discovery of Novel Treatments for SchizophreniaU01MH087965 · NIMH · VANDERBILT UNIVERSITY · PI CONN, P JEFFREY, LINDSLEY, CRAIG · 2010 to 2014
$9.3MMuscarinic receptor activators as novel antipsychotic agentsR01MH073676 · NIMH · VANDERBILT UNIVERSITY · PI Jerri Michelle Rook · 2006 to 2026
$9.3MResearch Project: Sensory and Multisensory Contributions to AutismU54HD083211 · NICHD · VANDERBILT UNIVERSITY MEDICAL CENTER · PI DYKENS, ELISABETH MAY · 2015 to 2019
$7.1MFunctions of Metabotropic Glutamate Receptor SubtypesR37NS031373 · NINDS · VANDERBILT UNIVERSITY · PI CONN, P JEFFREY · 2014 to 2020
$3.5MNICHD NIH HHS U54 HD083211NIMH NIH HHS R01 MH073676NIMH NIH HHS U01 MH087965NIMH NIH HHS U54 MH084659NINDS NIH HHS R37 NS031373
Abstract
This letter describes the chemical optimization of a novel series of M
Indexed as
AnimalsHumansLigandsNucleoside Transport ProteinsPyridazinesRats, Sprague-DawleyReceptor, Muscarinic M4Structure-Activity RelationshipThiophenes5-amino-3,4-dimethyl-N-(4-((trifluoromethyl)sulfonyl)benzyl)thieno(2,3-c)pyridazine-6-carboxamideadenosine transporterLigandsNucleoside Transport ProteinsPyridazinesReceptor, Muscarinic M4ThiophenesM(4)Muscarinic acetylcholine receptorPositive allosteric modulator (PAM)SchizophreniaStructure-activity relationship (SAR)
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