CK156

CK156 : Inhibitor of STK17A

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe CK156 is in the process of SERP review.

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Information

STK17A

Inhibitor

up to 5 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q9UEE5

Target Class: Kinase

Target SubClass: CAMK

Potency: IC50

Potency Value: 49 nM

Potency Assay: Radiometric assay (33PanQinase)

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

Target aliases:

Serine/threonine-protein kinase 17A, DRAK1, STK17A ...

DOI Reference: 10.1021/acs.jmedchem.2c00173

Uniprot ID: Q9UEE5

Target Class: Kinase

Target SubClass: CAMK

Potency: Kd

Potency Value: 21 nM

Potency Assay: ITC

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

Target aliases:

Serine/threonine-protein kinase 17A, DRAK1, STK17A ...

DOI Reference: 10.1021/acs.jmedchem.2c00173

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

The selectivity profile of CK156 was determined with the scanMAX® assay from DiscoverX at 1000 and 100 nM and on- and off-targets were evaluated with in vitro IC50 with the 33PanQinase activity assay from ProQinase and in cellulo IC50 with NanoBRET assay.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a compound with good in vitro potency Kd = 21 nM (ITC) and IC50 of 49 nM (33PanQuinase), good cellular potency with IC50 of 182 nM and very good selectivity, tested 468 kinases as off-targets. Target engagement has been evaluated with nanoBRET and cytotoxicity window determined. Currently, there are no other inhibitors known against this 'dark-kinome' kinase and no downstream-target known. It is clearly, the best inhibitor so far.

(last updated: 17 Jun 2024 )