Evidence map›Paper›PMID 30696302›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2019

Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.

Giulio Poli, Margherita Lapillo, Vibhu Jha, Nayla Mouawad, Isabella Caligiuri, Marco Macchia, Filippo Minutolo, Flavio Rizzolio, Tiziano Tuccinardi, Carlotta Granchi

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
5.4field-weighted citation impact, top 4% of its field
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

17 citing papers in PubMed, 35 citations in OpenAlex.

  1. The biological functions of monoacylglycerol lipase (MAGL) in cancer.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2026
    Review
  2. Article
  3. Review
  4. Frontiers in pharmacology · 2024
    Article
  5. Machine Learning and Computational Chemistry for the Endocannabinoid System.Methods in molecular biology (Clifton, N.J.) · 2023
    Review
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  15. Article
  16. Key Topics in Molecular Docking for Drug Design.International journal of molecular sciences · 2019
    Review
  17. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 2 institutions in 2 countries.

Giulio Polia Department of Pharmacy , University of Pisa , Pisa , Italy.
Margherita Lapilloa Department of Pharmacy , University of Pisa , Pisa , Italy.
Vibhu Jhaa Department of Pharmacy , University of Pisa , Pisa , Italy.
Nayla Mouawada Department of Pharmacy , University of Pisa , Pisa , Italy.
Isabella Caligiurib Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano , Italy.
Marco Macchiaa Department of Pharmacy , University of Pisa , Pisa , Italy.
Filippo Minutoloa Department of Pharmacy , University of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-3312-104X
Flavio Rizzoliob Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano , Italy.ORCID http://orcid.org/0000-0002-3400-4363
Tiziano Tuccinardia Department of Pharmacy , University of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-6205-4069
Carlotta Granchia Department of Pharmacy , University of Pisa , Pisa , Italy.ORCID http://orcid.org/0000-0002-5849-0722
University of Pisa · ITCa' Foscari University of Venice · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Monoacylglycerol lipase (MAGL) is an attractive therapeutic target for many pathologies, including neurodegenerative diseases, cancer as well as chronic pain and inflammatory pathologies. The identification of reversible MAGL inhibitors, devoid of the side effects associated to prolonged MAGL inactivation, is a hot topic in medicinal chemistry. In this study, a novel phenyl(piperazin-1-yl)methanone inhibitor of MAGL was identified through a virtual screening protocol based on a fingerprint-driven consensus docking (CD) approach. Molecular modeling and preliminary structure-based hit optimization studies allowed the discovery of derivative 4, which showed an efficient reversible MAGL inhibition (IC

Indexed as

Computer SimulationCell Line, TumorCell ProliferationCell SurvivalDrug DiscoveryEnzyme InhibitorsHigh-Throughput Screening AssaysHumansInhibitory Concentration 50Molecular Dynamics SimulationMonoacylglycerol LipasesPiperazinesStructure-Activity RelationshipSubstrate SpecificityEnzyme InhibitorsMonoacylglycerol LipasesPiperazinesdrug designMAGL inhibitorsmolecular modellingvirtual screening

Identifiers

PMID30696302
PMCPMC6352951
OpenAlexW2913644870

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.