ArticleBioorganic & medicinal chemistry letters2013
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Structure-Activity Relationships of Pan-GαACS chemical neuroscience · 2018Article
- The Hypnotic, Anxiolytic, and Antinociceptive Profile of a Novel µ-Opioid Agonist.Molecules (Basel, Switzerland) · 2017Article
- Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel MACS chemical neuroscience · 2016Article
- Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.Bioorganic & medicinal chemistry letters · 2015Article
- Development of allosteric modulators of GPCRs for treatment of CNS disorders.Neurobiology of disease · 2014Review
- Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.Drug discovery today · 2013Review
- Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits.ACS chemical neuroscience · 2013Review
- Discovery of ML326: The first sub-micromolar, selective M5 PAM.Bioorganic & medicinal chemistry letters · 2013Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
This Letter describes the further optimization of an MLPCN probe molecule (ML137) through the introduction of 5- and 6-membered spirocycles in place of the isatin ketone. Interestingly divergent structure-activity relationships, when compared to earlier M1 PAMs, are presented. These novel spirocycles possess improved efficacy relative to ML137, while also maintaining high selectivity for the human and rat muscarinic M1 receptor subtype.
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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.