Evidence map›Paper›PMID 30768268›Full record

ArticleJournal of medicinal chemistry2019

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).

Christopher R M Asquith, Benedict-Tilman Berger, Jing Wan, James M Bennett, Stephen J Capuzzi, Daniel J Crona, David H Drewry, Michael P East, Jonathan M Elkins, Oleg Fedorov and 9 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.

0numbers the graph read from it
0cells of the map it votes in
30citing papers in PubMed
6.5field-weighted citation impact, top 2% 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

30 citing papers in PubMed, 68 citations in OpenAlex.

  1. Article
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  6. Synthesis of a 3,7-Disubstituted Isothiazolo[4,3-Molecules (Basel, Switzerland) · 2024
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  17. Review
  18. Article
  19. Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry · 2022
    Review
  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

19 authors at 4 institutions in 4 countries.

Christopher R M AsquithORCID 0000-0001-5871-3458
Benedict-Tilman BergerStructural Genomics Consortium, Johann Wolfgang Goethe University, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15 , D-60438 Frankfurt am Main , Germany.
Jing Wan
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 , U.K.
Stephen J CapuzziORCID 0000-0003-0001-8211
Daniel J Crona
Michael P East
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 , U.K.
Oleg FedorovStructural Genomics Consortium and Target Discovery Institute, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building , Oxford OX3 7DQ , U.K.
Paulo H GodoiStructural Genomics Consortium , Universidade Estadual de Campinas , Campinas , São Paulo 13083-886 , Brazil.
Debra M Hunter
Stefan KnappStructural Genomics Consortium, Johann Wolfgang Goethe University, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15 , D-60438 Frankfurt am Main , Germany.ORCID 0000-0001-5995-6494
Susanne MüllerStructural Genomics Consortium, Johann Wolfgang Goethe University, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15 , D-60438 Frankfurt am Main , Germany.
Chad D Torrice
Carrow I Wells
H Shelton Earp
Timothy M WillsonORCID 0000-0003-4181-8223
William J ZuercherORCID 0000-0002-9836-0068
University of North Carolina at Chapel Hill · USGoethe University Frankfurt · DEGenomics England · GBUniversidade Estadual de Campinas (UNICAMP) · BR

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

We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK), together with a structurally related negative control SGC-GAK-1N (14). 11 was highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent RIPK2 inhibitor lacking GAK activity. Together, this chemical probe set can be used to interrogate GAK cellular biology.

Indexed as

Cyclin GHEK293 CellsHumansIntracellular Signaling Peptides and ProteinsMaleMolecular ProbesProtein Serine-Threonine KinasesCyclin GGAK protein, humanIntracellular Signaling Peptides and ProteinsMolecular ProbesProtein Serine-Threonine Kinases

Identifiers

PMID30768268
PMCPMC6567991
OpenAlexW2952548225

What OpenQuestion holds

Textmetadata
LicenceTDM
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.