BMS-509744

BMS-509744 : Inhibitor of ITK

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe BMS-509744 is in the process of SERP review.

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Information

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q08881

Target Class: Kinase

Target SubClass: Tyr kinase

Potency: IC50

Potency Value: 19 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Tyrosine-protein kinase ITK/TSK, LYK, EMT, ITK, IT ...

DOI Reference: 10.1021/bi049428r

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity studies in vitro revealed that the compound showed >200-fold selectivity versus other Tec family tyrosine kinases and at least a 30-fold potency ratio versus all the other protein kinases tested.

Potency assay, off target (cells): To further analyze compound selectivity in cells, their effects on cellular tyrosine phosphorylation were examined in Jurkat T-cells following stimulation with anti- CD3 antibody. BMS-509744 dose-dependently inhibited tyrosine phosphorylation of PLCγ1. In non-T-cells, BMS-509744, at concentrations up to 10 uM, did not affect EGF-induced cellular tyrosine or PLCγ1 phosphorylation (in A549 lung carcinoma cells).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Since IL-2 secretion is an indirect measurement of in-cell activity, the compound would benefit from a measure of direct target engagement in cells. In addition, IL-2 secretion can be impacted by multiple biological pathways. The 18-member kinase panel is not sufficient to judge selectivity. Additional in vivo doses need to be examined to refine the recommended dose in mice. Considering the insufficient in vitro data is important when deciding whether this is the best in vivo tool for your experiments.

(last updated: 11 Feb 2025 )