Evidence map›Paper›PMID 29494768›Full record

ArticleJournal of medicinal chemistry2019

Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization.

Maarten L J Doornbos, Xuesong Wang, Sophie C Vermond, Luc Peeters, Laura Pérez-Benito, Andrés A Trabanco, Hilde Lavreysen, José María Cid, Laura H Heitman, Gary Tresadern and 1 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
–field-weighted citation impact
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

9 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Review
  6. Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1ACS medicinal chemistry letters · 2020
    Article
  7. Review
  8. Article
  9. Review
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

11 authors.

Maarten L J DoornbosDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR) , Leiden University , P.O. Box 9502, 2300RA Leiden , The Netherlands.
Xuesong WangDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR) , Leiden University , P.O. Box 9502, 2300RA Leiden , The Netherlands.
Sophie C VermondDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR) , Leiden University , P.O. Box 9502, 2300RA Leiden , The Netherlands.
Luc PeetersJanssen Research and Development , Turnhoutseweg 30 , 2340 Beerse , Belgium.
Laura Pérez-BenitoJanssen Research and Development , Calle Jarama 75A , 45007 Toledo , Spain.
Andrés A TrabancoJanssen Research and Development , Calle Jarama 75A , 45007 Toledo , Spain.ORCID 0000-0002-4225-758X
Hilde LavreysenJanssen Research and Development , Turnhoutseweg 30 , 2340 Beerse , Belgium.
José María CidJanssen Research and Development , Calle Jarama 75A , 45007 Toledo , Spain.
Laura H HeitmanDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR) , Leiden University , P.O. Box 9502, 2300RA Leiden , The Netherlands.
Gary TresadernJanssen Research and Development , Calle Jarama 75A , 45007 Toledo , Spain.ORCID 0000-0002-4801-1644
Adriaan P IJzermanDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research (LACDR) , Leiden University , P.O. Box 9502, 2300RA Leiden , The Netherlands.ORCID 0000-0002-1182-2259

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Covalent labeling of G protein-coupled receptors (GPCRs) by small molecules is a powerful approach to understand binding modes, mechanism of action, pharmacology, and even facilitate structure elucidation. We report the first covalent positive allosteric modulator (PAM) for a class C GPCR, the mGlu

Indexed as

Drug DesignAllosteric RegulationAllosteric SiteHumansKineticsLigandsMolecular Docking SimulationMutagenesisProtein Structure, TertiaryPyridinesReceptors, Metabotropic GlutamateLigandsmetabotropic glutamate receptor 2PyridinesReceptors, Metabotropic Glutamate

Identifiers

PMID29494768
PMCPMC6331142

What OpenQuestion holds

Textmetadata
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.