Evidence map›Paper›PMID 20146481›Full record

ArticleJournal of medicinal chemistry2010

Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.

Sanjeev Kumar V Vernekar, Hasan Y Hallaq, Guy Clarkson, Andrew J Thompson, Linda Silvestri, Sarah C R Lummis, Martin Lochner

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.6field-weighted citation impact, top 18% 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

11 citing papers in PubMed, 53 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Expedient synthesis ofScience advances · 2019
    Article
  6. Article
  7. Article
  8. Article
  9. 4-Methyl-N-(9-methyl-9-aza-bicyclo-[3.3.1]non-3-yl)benzamide.Acta crystallographica. Section E, Structure reports online · 2012
    Article
  10. (1S*,5R*)-9-Phenyl-9-aza-bicyclo-[3.3.1]nonan-3-one.Acta crystallographica. Section E, Structure reports online · 2012
    Article
  11. High-affinity fluorescent ligands for the 5-HT(3) receptor.Bioorganic & medicinal chemistry letters · 2012
    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

7 authors at 2 institutions in 1 country.

Sanjeev Kumar V VernekarDepartment of Chemistry, University of Warwick, Coventry CV4 7AL, UK.
Hasan Y Hallaq
Guy Clarkson
Andrew J Thompson
Linda Silvestri
Sarah C R Lummis
Martin Lochner
University of Warwick · GBUniversity of Cambridge · GB

Funding

Wellcome Trust 081925Wellcome Trust 081925/Z/07/Z
6 · The paper itself

Abstract

This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluorophore was appended to one such position and specifically bound to 5-HT(3)A receptors in mammalian cells.

Indexed as

Binding, CompetitiveBoron CompoundsCell LineGranisetronHumansMagnetic Resonance SpectroscopyRadioligand AssayReceptors, Serotonin, 5-HT3Serotonin 5-HT3 Receptor AntagonistsSerotonin AntagonistsSpectrometry, Mass, Electrospray IonizationStructure-Activity Relationship4,4-difluoro-4-bora-3a,4a-diaza-s-indaceneBoron CompoundsGranisetronReceptors, Serotonin, 5-HT3Serotonin 5-HT3 Receptor AntagonistsSerotonin Antagonists

Identifiers

PMID20146481
PMCPMC4166935
OpenAlexW1974787139

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.