Evidence map›Paper›PMID 32677155›Full record

ArticleChemMedChem2020

Discovery of a Lead Brain-Penetrating Gonadotropin-Releasing Hormone Receptor Antagonist with Saturable Binding in Brain.

Roberto B W Bekker, Richard Fjellaksel, Trine Hjornevik, Syed Nuruddin, Waqas Rafique, Jørn H Hansen, Rune Sundset, Ira H Haraldsen, Patrick J Riss

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed, 1 pooled it
1.0field-weighted citation impact, top 23% 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

2 citing papers in PubMed, 1 synthesis or guideline pooled it, 7 citations in OpenAlex.

  1. Pooled it
  2. 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

9 authors at 4 institutions in 1 country.

Roberto B W BekkerDepartment of Chemistry, University of Oslo, Sem Saelands vei, 26, 0371, Oslo, Norway.
Richard FjellakselDepartment of Clinical Medicine, UiT The Arctic University of Norway, Hansine Hansens veg 18, 9019, Tromsø, Norway.
Trine HjornevikDepartment of Diagnostic Physics, Oslo University Hospital, Sognsvannsveien 20, 0372, Oslo, Norway.
Syed NuruddinNorwegian Medical Cyclotron AS, Rikshospitalet, Sognsvannsveien 20, Oslo, Norway.
Waqas RafiqueDepartment of Chemistry, University of Oslo, Sem Saelands vei, 26, 0371, Oslo, Norway.
Jørn H HansenDepartment of Chemistry, UiT - The Arctic University of Norway, Hansine Hansens veg 18, 9019, Tromsø, Norway.
Rune SundsetDepartment of Clinical Medicine, UiT The Arctic University of Norway, Hansine Hansens veg 18, 9019, Tromsø, Norway.
Ira H HaraldsenClinical Neurosciences, Oslo University Hospital-Ulleval, Kirkeveien 166, post code?, Oslo, Norway.
Patrick J RissDepartment of Chemistry, University of Oslo, Sem Saelands vei, 26, 0371, Oslo, Norway.
UiT The Arctic University of Norway · NOUniversity of Oslo · NOOslo University Hospital · NONorwegian Medicines Agency · NO

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

We report the synthesis, radiosynthesis and biological characterisation of two gonadotropin-releasing hormone receptor (GnRH-R) antagonists with nanomolar binding affinity. A small library of GnRH-R antagonists was synthesised in 20-67 % overall yield with the aim of identifying a high-affinity antagonist capable of crossing the blood-brain barrier. Binding affinity to rat GnRH-R was determined by autoradiography in competitive-binding studies against [

Indexed as

Drug DiscoveryAnimalsBinding SitesBrainDose-Response Relationship, DrugFluorine RadioisotopesHydrocarbons, FluorinatedMolecular StructurePositron-Emission TomographyPyrimidinesRadiopharmaceuticalsRatsReceptors, LHRHStructure-Activity RelationshipelagolixFluorine RadioisotopesHydrocarbons, FluorinatedPyrimidinesRadiopharmaceuticalsReceptors, LHRHelagolixfluorine-18GnRHGnRH−RPET

Identifiers

PMID32677155
PMCPMC7540054
OpenAlexW3042869135

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.