JNJ-6204

JNJ-6204 : Inhibitor of CSNK1D, CSNK1E

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe JNJ-6204 is in the process of SERP review.

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Information

CSNK1D
CSNK1E

Inhibitor

up to 1 uM
Reviewer recommended concentration: up to 10µM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P48730

Target Class: Kinase

Target SubClass: CK1

Potency: Kd

Potency Value: 2.3 nM

Potency Assay: ADP-Glo assay using recombinant proteins

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

Target aliases:

Casein kinase I isoform delta, HCKID, CSNK1D, KC1D ...

DOI Reference: 10.1021/acsmedchemlett.3c00523

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Closely related kinases: CSNK1A1 (IC50 = 419 nM) Panel of 370 kinases at 1 μM: clean; Closest hit: TNIK (IC50 = 1.6 μM).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Selective CK1 delta inhibitor with a 542 nM IC50 for PER2 functional activity in cells. Good bioavailability in mice, but the dosing regimen should be carefully designed to achieve desired coverage over the target.

(last updated: 30 May 2023 )