Target intelligence / Profile preview

Kinome panel

Molecular classification
Enzyme, Kinase
01

Overview

A kinome panel refers to a comprehensive set of kinases—enzymes that catalyze the transfer of phosphate groups from ATP to specific substrates—used primarily in drug discovery to evaluate the selectivity and potency of inhibitors (Manning et al., 2002). The human kinome comprises approximately 518 protein kinases that play pivotal roles in regulating complex cellular processes, including signal transduction, cell growth, and metabolism (NCBI, 2023). Because aberrant kinase activity is a primary driver in various pathologies, particularly oncology and inflammatory disorders, kinome-wide screening is essential for identifying lead compounds and assessing potential off-target liabilities (PubMed, 2021). These panels allow researchers to map the fingerprint of a drug across the entire kinase family, facilitating the development of highly selective therapies or multi-target inhibitors designed to overcome resistance (Nature Reviews Drug Discovery, 2018). Consequently, while not a single target itself, the kinome panel is a fundamental tool for characterizing the pharmacological profile of modern kinase-targeted therapeutics.

Other names
Kinase panelHuman kinomeKinome screening libraryKinase profiling panel
02

Mechanism of action

Kinase inhibitors typically act by competing with ATP for the binding site (Type I/II inhibitors) or through allosteric modulation to prevent the phosphorylation of substrate proteins (StatPearls, 2023).

03

Biological functions

Signal transductionProtein phosphorylationCell cycle regulationApoptosisMetabolic regulation
04

Disease associations

CancerInflammationAutoimmune diseaseNeurodegenerative disease
05

Safety considerations

Off-target toxicityCardiotoxicityHepatotoxicityPolypharmacology-related adverse effects
06

Interacting drugs

6 more in the full profile.

07

Biomarkers

Kinase mutation statusPhospho-protein levelsGene amplificationProtein expression levels

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