ArticleJournal of medicinal chemistry2023
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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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.
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Who cites it
21 citing papers in PubMed, 37 citations in OpenAlex.
- Phase 2b Trial of the PDE10A Inhibitor MK-8189 in People With an Acute Episode of Schizophrenia.Journal of clinical psychopharmacologyTrial
- Is AI Capable of Real-World Drug Discovery?Journal of chemical information and modeling · 2026Article
- MOZAIC: compound growth via in silico reactions and global optimization using Conformational Space Annealing.Bioinformatics (Oxford, England) · 2026Article
- Developments and challenges in hit progression within fragment-based drug discovery.Nature communications · 2026Review
- Article
- Phosphodiesterase Inhibition Increases Striatal GDNF and Protects Against Preclinical Parkinsonism.Journal of neurochemistry · 2025Article
- Unveiling optimal molecular features for hERG insights with automatic machine learning.Journal of pharmaceutical analysis · 2025Article
- Inhibition of Phosphodiesterase 10A by MP-10 Rescues Behavioral Deficits and Normalizes Microglial Morphology and Synaptic Pruning in A Mouse Model of FOXP1 Syndrome.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Chemoselective synthesis of 1,3,4-thiadiazoles from acyl hydrazines and nitroalkanes using elemental sulfur.Nature communications · 2025Article
- PDE10A Inhibition Reduces NLRP3 Activation and Pyroptosis in Sepsis and Nerve Injury.International journal of molecular sciences · 2025Article
- In the Brain of Phosphodiesterases: Potential Therapeutic Targets for Schizophrenia.Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology · 2025Review
- Emerging Pharmacological Approaches for Psychosis and Agitation in Alzheimer's Disease.CNS drugs · 2025Review
- PDE1B and PDE10A as novel targets for schizophrenia: from molecular design and synthesis to therapeutic promise.Frontiers in pharmacology · 2025Review
- Unlocking the potential of lumateperone and novel anti-psychotics for schizophrenia.BioImpacts : BI · 2025Review
- Overview of Novel Antipsychotic Drugs: State of the Art, New Mechanisms, and Clinical Aspects of Promising Compounds.Biomedicines · 2025Review
- Future Therapeutic Strategies for Alzheimer's Disease: Focus on Behavioral and Psychological Symptoms.International journal of molecular sciences · 2024Review
- Article
- Imidazopyrimidine: from a relatively exotic scaffold to an evolving structural motif in drug discovery.RSC medicinal chemistry · 2024Review
- Fragment-based drug discovery for disorders of the central nervous system: designing better drugs piece by piece.Frontiers in chemistry · 2024Review
- A Homogeneous Bioluminescent System to Monitor Cyclic Guanosine Monophosphate.ACS pharmacology & translational science · 2023Article
Corrections and comments
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Authors and funding
19 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
PDE10A is an important regulator of striatal signaling that, when inhibited, can normalize dysfunctional activity. Given the involvement of dysfunctional striatal activity with schizophrenia, PDE10A inhibition represents a potentially novel means for its treatment. With the goal of developing PDE10A inhibitors, early optimization of a fragment hit through rational design led to a series of potent pyrimidine PDE10A inhibitors that required further improvements in physicochemical properties, off-target activities, and pharmacokinetics. Herein we describe the discovery of an isomeric pyrimidine series that addresses the liabilities seen with earlier compounds and resulted in the invention of compound
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What OpenQuestion holds
Registered trials
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.