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Sgc-Gak-1: A Chemical Probe Candidate For The Understudied Kinase Gak

Year: 2017

Type: article

Abstract: SGC-GAK-1 is presented as a chemical probe for the understudied cyclin G associated kinase (GAK). SGC-GAK-1 is potent and shows submicromolar cellular target engagement with GAK. The compound shows > 30-fold selectivity relative to all other kinases profiled with the exception of RIPK2. A closely related molecule that is significantly less potent with GAK, SGC-GAK-1N, is included as a negative control. In addition, a compound having potent activity at RIPK2 but not GAK, HY-19764, is offered to control for the activity of RIPK2.

Source: Zenodo (CERN European Organization for Nuclear Research)

DOI: 10.5281/zenodo.852467

Authors: Asquith, Christopher R. M., Axtman, Alison D., Bennett, James M., Drewry, David H., Elkins, Jonathan M., Godoi, Paulo, Knapp, Stefan, Laitinen, Tuomo, Müller, Susanne, Paso, Antti, Tillman-Berger, Benedict, Wells, Carrow I., Willson, Timothy M., Zuercher, William J.

Institutions: University of North Carolina at Chapel Hill, University of Oxford, Universidade Estadual de Campinas (UNICAMP), Goethe University Frankfurt, University of Eastern Finland

Language: English

Topic: Protein Kinase Regulation and GTPase Signaling

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

OpenAlex ID: W2747926543

FWCI:

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