CG211

CG211 : Inhibitor of RIOK2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe CG211 is in the process of SERP review.

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Information

RIOK2

Inhibitor

up to 5 µM

In Vitro Validations

Uniprot ID: Q9BVS4

Target Class: Kinase

Target SubClass: RIO Type

Potency: Kd

Potency Value: 6.1 ± 0.4 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): 7VBT

Target aliases:

Serine/threonine-protein kinase RIO2, RIO2, RIOK2, ...

DOI Reference: 10.1021/acs.jmedchem.2c00271

Uniprot ID: Q9BVS4

Target Class: Kinase

Target SubClass: RIO Type

Potency: IC50

Potency Value: 139 ± 46 nM

Potency Assay: ADP-GloTM kinase assay

PDB ID for probe-target interaction (3D structure): 7VBT

Target aliases:

Serine/threonine-protein kinase RIO2, RIO2, RIOK2, ...

DOI Reference: 10.1021/acs.jmedchem.2c00271

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KINOMEscan approach was used to test the specificity of the binding of compound CQ211 to RIOK2 by screening it in a panel of 468 kinases, including 412 wild-type kinases (403 wild-type human kinases) and 56 disease-related mutants. Surprisingly, CQ211 exhibited excellent selectivity to RIOK2, with no interaction being observed between CQ211 and any of the other wild-type kinases (S (35) = 0.002 at 1 μM). CQ211 showed binding interactions only with three FLT3 mutants, FLT3-ITD-D835V, FLT3-ITD-F691L, and FLT3-D835V with percentage of control (%Ctr) of 4, 3.6, and 28, respectively, at 1 μM concentration.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

CQ211 shows adequate potency and selectivity and can be used as a probe in cells, with several reservations. 1) No cytotoxicity data is available in non-malignant cells, and 2) "CQ211 showed poor solubility in H2O and organic solvents. This may lead to poor membrane permeability and a loss of potency when moving into cells." Limited dosage and PK data do not allow for a recommended dose in model organisms to be provided.

(last updated: 3 Apr 2025 )