GDC-0834

GDC-0834 : ATP competitive inhibitor of BTK

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(2 ratings)

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Information

ATP competitive

up to 1 uM

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Probe Availability:

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 ...

DOI Reference: 10.1124/jpet.111.181545

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

excellent biochemical selectivity against a panel of 331 kinases, except for TEC-family kinase Bmx where a 3-fold difference was observed.

Probe Selectivity in Cell:

Minimal to no off-target receptor activity when screened against a panel of 30 targets (all <35% at 10 μM), minimal inhibition of the hERG channel (27% at 10 μM), and was negative in a gene-tox profile Ames (TA98/100 strains; +/− S9) and micronucleus tests (+/− S9). Known to bind six AO substrates with IC50 values ranging from 0.86 to 1.87 μM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP 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

SERP 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 )