T3-CLK

Inhibitor of CLK1, CLK2, CLK3, CLK4

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe T3-CLK is in the process of SERP review.

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Information

CLK1
CLK2
CLK3
CLK4

Inhibitor

< 100 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P49759

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 0.67 nM

Potency Assay: In vitro kinase assay

PDB ID for probe-target interaction (3D structure): 6RAA

Target aliases:

Dual specificity protein kinase CLK1, CLK, CLK1, C ...

DOI Reference: 10.1038/s41467-016-0008-7

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

200 to 300 times selective against dual specificity kinases such as DYRK1A (IC50 = 260 nM) and DYRK1B (IC50 = 230 nM) in vitro; NanoBRET assay results: IC50 DYRK1A 32 nM and DYRK1B 67 nM. Outside target family: Clean GPCR scan except for weak activity on HRH1 (Ki = 2154.79 nM)

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

T3-CLK is a pan-CLK inhibitor with high in vitro and cellular potency and with a proven on-target engagement and good negative control compound. There is only little activity on off-targets. The compound is non-toxic in cell assays up to 10 micromolar and stable in tissue culture medium.

(last updated: 17 Jun 2024 )