ArticleBioorganic & medicinal chemistry letters2017
Optimization of M
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In one paragraph
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 13 papers.
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13citing papers in PubMed
–field-weighted citation impact
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
13 citing papers in PubMed.
- 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
- Discovery of VU6008677: A Structurally Distinct Tricyclic MACS medicinal chemistry letters · 2024Article
- Characterization of a Novel M4 PAM PET Radioligand [11C]PF06885190 in Nonhuman Primates (NHP).Molecules (Basel, Switzerland) · 2023Article
- Discovery of structurally distinct tricyclic MBioorganic & medicinal chemistry letters · 2021Article
- Targeting Muscarinic Acetylcholine Receptors for the Treatment of Psychiatric and Neurological Disorders.Trends in pharmacological sciences · 2019Review
- SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic MBioorganic & medicinal chemistry letters · 2019Article
- Novel MBioorganic & medicinal chemistry letters · 2019Article
- 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
- Discovery of a novel 2,4-dimethylquinoline-6-carboxamide MBioorganic & medicinal chemistry letters · 2017Article
- Discovery of a novel, CNS penetrant 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
21 authors.
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.
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.
Kellie D NanceVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Eileen M EngelbergVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Changho HanVanderbilt 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.
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.
Frank W ByersVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, 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 WoodAstraZeneca, Neuroscience, Innovative Medicines & Early Development, Waltham, MA 02451, 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.
Dedong WuAstraZeneca, Pharmaceutical Science, 35 Gatehouse Drive, Waltham, MA 02451, USA.
Nicholas J BrandonAstraZeneca, Neuroscience, Innovative Medicines & Early Development, Waltham, MA 02451, USA.
Mark E DugganAstraZeneca, Neuroscience, Innovative Medicines & Early Development, Waltham, MA 02451, 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
$7.1MNICHD NIH HHS U54 HD083211NIMH NIH HHS R01 MH073676NIMH NIH HHS U01 MH087965NIMH NIH HHS U54 MH084659
Abstract
This letter describes the further chemical optimization of the 5-amino-thieno[2,3-c]pyridazine series (VU0467154/VU0467485) of M
Indexed as
Drug DiscoveryTranslational Research, BiomedicalAllosteric RegulationAnimalsCrystallography, X-RayHydrogen BondingPyridazinesRatsStructure-Activity RelationshipThiophenesPyridazinesThiophenesVU0476406M(4)Muscarinic acetylcholine receptorNon-human primate (NHP)Positive allosteric modulator (PAM)Structure-Activity Relationship (SAR)
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.