Evidence map›Paper›PMID 28338621›Full record

ArticleMolecules (Basel, Switzerland)2017

Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK.

Jakob Halekotte, Lydia Witt, Chiara Ianes, Marc Krüger, Mike Bührmann, Daniel Rauh, Christian Pichlo, Elena Brunstein, Andreas Luxenburger, Ulrich Baumann and 3 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
2.2field-weighted citation impact, top 12% 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

19 citing papers in PubMed, 41 citations in OpenAlex.

  1. Inhibition of Casein Kinase 1International journal of molecular sciences · 2025
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  17. Special Issue: Kinase inhibitors.Molecules (Basel, Switzerland) · 2018
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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 5 institutions in 2 countries.

Jakob HalekotteInstitute of Pharmacy, Christian-Albrechts-University of Kiel, Gutenbergstraße 76, D-24118 Kiel, Germany. jhalekotte@pharmazie.uni-kiel.de.
Lydia WittInstitute of Pharmacy, Christian-Albrechts-University of Kiel, Gutenbergstraße 76, D-24118 Kiel, Germany. lwitt@pharmazie.uni-kiel.de.
Chiara IanesDepartment of General and Visceral Surgery, Ulm University Hospital, Albert-Einstein-Allee 23, D-89081 Ulm, Germany. chiara.ianes@uni-ulm.de.
Marc KrügerDepartment of General and Visceral Surgery, Ulm University Hospital, Albert-Einstein-Allee 23, D-89081 Ulm, Germany. marcm3012@googlemail.com.
Mike BührmannInstitute of Chemical Biology, Dortmund University of Technology, Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany. uwe.knippschild@uniklinik-ulm.de.
Daniel RauhInstitute of Chemical Biology, Dortmund University of Technology, Otto-Hahn-Straße 4a, D-44227 Dortmund, Germany. mike.buehrmann@googlemail.com.
Christian PichloDepartment for Chemistry, University of Cologne, Otto-Fischer-Straße 12-14, D-50674 Cologne, Germany. daniel.rauh@tu-dortmund.de.
Elena BrunsteinDepartment for Chemistry, University of Cologne, Otto-Fischer-Straße 12-14, D-50674 Cologne, Germany. pichloc@uni-koeln.de.
Andreas LuxenburgerThe Ferrier Research Institute, Victoria University of Wellington, Gracefield Research Centre, 69 Gracefield Road, Lower Hutt P.O. Box 33-436, New Zealand. Elena.Brunstein@uni-koeln.de.
Ulrich BaumannDepartment for Chemistry, University of Cologne, Otto-Fischer-Straße 12-14, D-50674 Cologne, Germany. ubaumann@uni-koeln.de.
Uwe KnippschildDepartment of General and Visceral Surgery, Ulm University Hospital, Albert-Einstein-Allee 23, D-89081 Ulm, Germany. Andreas.Luxenburger@vuw.ac.nz.
Joachim BischofDepartment of General and Visceral Surgery, Ulm University Hospital, Albert-Einstein-Allee 23, D-89081 Ulm, Germany. joachim.bischof@uniklinik-ulm.de.
Christian PeiferInstitute of Pharmacy, Christian-Albrechts-University of Kiel, Gutenbergstraße 76, D-24118 Kiel, Germany. cpeifer@pharmazie.uni-kiel.de.
University Hospital Ulm · DEChristian-Albrechts-Universität zu Kiel · DEUniversity of Cologne · DETU Dortmund University · DEVictoria University of Wellington · NZ

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The involvement of protein kinase CK1δ in the pathogenesis of severe disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, familial advanced sleep phase syndrome, and cancer has dramatically increased interest in the development of effective small molecule inhibitors for both therapeutic application and basic research. Unfortunately, the design of CK1 isoform-specific compounds has proved to be highly complicated due to the existence of six evolutionarily conserved human CK1 members that possess similar, different, or even opposite physiological and pathophysiological implications. Consequently, only few potent and selective CK1δ inhibitors have been reported so far and structurally divergent approaches are urgently needed in order to establish SAR that might enable complete discrimination of CK1 isoforms and related p38α MAPK. In this study we report on design and characterization of optimized 4,5-diarylimidazoles as highly effective ATP-competitive inhibitors of CK1δ with compounds 11b (IC

Indexed as

Adenosine TriphosphateCasein Kinase IdeltaCell Line, TumorCrystallography, X-RayHumansImidazolesInhibitory Concentration 50Mitogen-Activated Protein Kinase 14Models, MolecularPhylogenyProtein Kinase InhibitorsAdenosine TriphosphateCasein Kinase IdeltaImidazolesMitogen-Activated Protein Kinase 14Protein Kinase Inhibitors4,5-diaryl-imidazolesAlzheimer’s diseaseamyotrophic lateral sclerosiscancerfamilial advanced sleep phase syndromeformerly known as casein kinase 1kinase inhibitorsp38 MAPKprotein kinase CK1

Identifiers

PMID28338621
PMCPMC6154583
OpenAlexW2601416517

What OpenQuestion holds

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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.