Evidence map›Paper›PMID 34342227›Full record

ArticleJournal of medicinal chemistry2021

Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.

Scott H Henderson, Fiona Sorrell, James Bennett, Oleg Fedorov, Marcus T Hanley, Paulo H Godoi, Roberta Ruela de Sousa, Sean Robinson, Alexander Ashall-Kelly, Iva Hopkins Navratilova and 3 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
7.6field-weighted citation impact, top 3% 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

5 citing papers in PubMed, 20 citations in OpenAlex.

  1. Article
  2. Article
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  5. 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

13 authors at 8 institutions in 3 countries.

Scott H HendersonSussex Drug Discovery Centre, University of Sussex, Brighton BN1 9RH, U.K.ORCID 0000-0002-9504-5943
Fiona SorrellStructural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Oxford OX3 7DQ, U.K.
James BennettTarget Discovery Institute, University of Oxford, Oxford OX3 7FZ, U.K.
Oleg FedorovTarget Discovery Institute, University of Oxford, Oxford OX3 7FZ, U.K.
Marcus T HanleyMedicines Discovery Institute, Cardiff University, Cardiff CF10 3AT, U.K.
Paulo H GodoiStructural Genomics Consortium, Universidade Estadual de Campinas, Cidade Universitária Zeferino Vaz, Av. Dr. André Tosello, 550, Barão Geraldo, Campinas, SP 13083-886, Brazil.
Roberta Ruela de SousaStructural Genomics Consortium, Universidade Estadual de Campinas, Cidade Universitária Zeferino Vaz, Av. Dr. André Tosello, 550, Barão Geraldo, Campinas, SP 13083-886, Brazil.
Sean RobinsonExscientia, The Schrödinger Building, Oxford Science Park, Oxford OX4 4GE, U.K.ORCID 0000-0001-9312-7411
Alexander Ashall-KellyMedicines Discovery Institute, Cardiff University, Cardiff CF10 3AT, U.K.
Iva Hopkins NavratilovaExscientia, The Schrödinger Building, Oxford Science Park, Oxford OX4 4GE, U.K.
Daryl S WalterEvotec (UK) Ltd., 112-114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, U.K.
Jonathan M ElkinsStructural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Oxford OX3 7DQ, U.K.ORCID 0000-0003-2858-8929
Simon E WardMedicines Discovery Institute, Cardiff University, Cardiff CF10 3AT, U.K.ORCID 0000-0002-8745-8377
Universidade Estadual de Campinas (UNICAMP) · BRUniversity of Wales Institute Cardiff · SGScience Oxford · GBEvotec (United Kingdom) · GBGenomics England · GBUniversity of Dundee · GBUniversity of Oxford · GBUniversity of Sussex · GB

Funding

Biotechnology and Biological Sciences Research Council BB/L017105/1Wellcome TrustWellcome Trust 106169/ZZ14/Z
6 · The paper itself

Abstract

Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer's disease (AD) and Down's syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A's role as a mediator in the cell cycle has garnered interest in oncologic indications. Structure-activity relationship (SAR) analysis in combination with high-resolution X-ray crystallography leads to a series of pyrazolo[1,5-

Indexed as

Drug DiscoveryDose-Response Relationship, DrugDyrk KinasesHEK293 CellsHumansLigandsMolecular StructureProtein Kinase InhibitorsProtein Serine-Threonine KinasesProtein-Tyrosine KinasesSolubilityStructure-Activity RelationshipDyrk KinasesLigandsProtein Kinase InhibitorsProtein Serine-Threonine KinasesProtein-Tyrosine Kinases

Identifiers

PMID34342227
PMCPMC8482766
OpenAlexW3190706740

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.