Evidence map›Paper›PMID 29072804›Full record

ArticleChemMedChem2018

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Christopher R M Asquith, Tuomo Laitinen, James M Bennett, Paulo H Godoi, Michael P East, Graham J Tizzard, Lee M Graves, Gary L Johnson, Ronna E Dornsife, Carrow I Wells and 3 more

Abstract read
In one paragraph

Article in ChemMedChem, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.

0numbers the graph read from it
0cells of the map it votes in
21citing 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

21 citing papers in PubMed.

  1. Article
  2. Article
  3. Synthesis of a 3,7-Disubstituted Isothiazolo[4,3-Molecules (Basel, Switzerland) · 2024
    Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry · 2022
    Review
  10. Article
  11. Article
  12. Review
  13. Article
  14. SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.ACS medicinal chemistry letters · 2020
    Article
  15. Article
  16. Quinazoline-Based Antivirulence Compounds Selectively TargetAntimicrobial agents and chemotherapy · 2019
    Article
  17. Article
  18. Article
  19. Article
  20. 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

13 authors.

Christopher R M AsquithStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.ORCID 0000-0001-5871-3458
Tuomo LaitinenSchool of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211, Kuopio, Finland.
James M BennettStructural Genomics Consortium and Target Discovery Institute, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford, OX3 7DQ, UK.
Paulo H GodoiStructural Genomics Consortium, Universidade Estadual de Campinas-UNICAMP, Campinas, São Paulo, 13083-886, Brazil.
Michael P EastDepartment of Pharmacology, University of North Carolina at Chapel Hill, NC, 27599, USA.
Graham J TizzardUK National Crystallography Service, School of Chemistry, University of Southampton, Highfield Campus, Southampton, SO17 1BJ, UK.
Lee M GravesDepartment of Pharmacology, University of North Carolina at Chapel Hill, NC, 27599, USA.
Gary L JohnsonDepartment of Pharmacology, University of North Carolina at Chapel Hill, NC, 27599, USA.
Ronna E DornsifeStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.
Carrow I WellsStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.ORCID 0000-0003-4799-6792
Jonathan M ElkinsStructural Genomics Consortium and Target Discovery Institute, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford, OX3 7DQ, UK.ORCID 0000-0003-2858-8929
Timothy M WillsonStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.ORCID 0000-0003-4181-8223
William J ZuercherStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.ORCID 0000-0002-9836-0068

Funding

Illuminating Function of the Understudied Druggable KinomeU24DK116204 · NIDDK · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JOHNSON, GARY L. · 2017 to 2022
$13.6M
Activation and Regulation of the Understudied Kinome Using MIB/MS TechnologyU01MH104999 · NIMH · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JOHNSON, GARY L. · 2014 to 2016
$1.2M
NIDDK NIH HHS U24 DK116204NIMH NIH HHS U01 MH104999Wellcome Trust
6 · The paper itself

Abstract

4-Anilinoquinolines were identified as potent and narrow-spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4-anilino group and the 6,7-quinoline substituents produced GAK inhibitors with nanomolar activity, over 50 000-fold selectivity relative to other members of the numb-associated kinase (NAK) subfamily, and a compound (6,7-dimethoxy-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine; 49) with a narrow-spectrum kinome profile. These compounds may be useful tools to explore the therapeutic potential of GAK in prevention of a broad range of infectious and systemic diseases.

Indexed as

Aniline CompoundsBinding SitesCatalytic DomainDrug DesignEndocytosisHumansIntracellular Signaling Peptides and ProteinsKineticsMolecular Docking SimulationProtein BindingProtein Kinase InhibitorsProtein Serine-Threonine KinasesQuinazolinesStructure-Activity RelationshipVirusesAniline CompoundsanilinoquinazolineGAK protein, humanIntracellular Signaling Peptides and ProteinsProtein Kinase InhibitorsProtein Serine-Threonine KinasesQuinazolinesanilinoquinolinesantibacterial agentschemical probescyclin G associated kinase (GAK)

Identifiers

PMID29072804
PMCPMC5914168

What OpenQuestion holds

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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.