GDC-0834

GDC-0834 : Inhibitor, ATP competitive of BTK

Structure

Information

Protein target names: BTK

Mechanism of action: Inhibitor, ATP competitive

Recommended in-cell concentration:
up to 1 uM
Primary References:

In Vitro Validations

Uniprot ID: Q06187
Target Class: Protein kinase
Target SubClass: TK
Potency: IC50
Potency Value: 6 nM
Potency Assay: assayed at Invitrogen using the Z'-LYTE platform, Lanthascreen
PDB ID for probe-target interaction (3D structure): 4OTF
Structure-activity relationship: yes
Target aliases:
Tyrosine-protein kinase BTK, AGMX1, BTK, BTK_HUMAN ...

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

This compound was shown to be a substrate and inhibitor of human aldehyde oxidase. It is a good tool compound to use in cells and small animals, but there are marketed BTK inhibitors that would be more appropriate for routine experiments because they do not interact with AO.

(last updated: 2 Jun 2021 )

SERP Ratings

In Cell Rating

Comments:

At higher concentrations (3-10 uM) this compound has off-target activities in human primary cell assays that may confound interpretation of results in phenotypic assays or animal studies. These activities include inhibition of proliferation of human primary endothelial cells, T cells, coronary artery smooth muscle cells and fibroblasts.

(last updated: 22 Jun 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 13 Jul 2021 )