SGC-CDKL2/AAK1/BMP2K-1

SGC-CDKL2/AAK1/BMP2K-1 : Inhibitor of CDK2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe SGC-CDKL2/AAK1/BMP2K-1 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

CDK2

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P24941

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 230 nM

Potency Assay: In Vitro kinase assay

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

Target aliases:

Cyclin-dependent kinase 2, CDKN2, CDK2, CDK2_HUMAN ...

DOI Reference: 10.1021/acsmedchemlett.4c00219

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Off Target: AAK1

Potency end-point : IC50 160 nM

Potency assay (off target): SGC-CDKL2/AAK1/BMP2K-1 was profiled in the DiscoverX MAX assay against 403 wild-type kinases at 1 μM. Only 2 kinases showed PoC <10 giving an S10(1 μM) = 0.002. When the PoC <40 fraction was examined, 10 kinases were included (S35(1 μM) = 0.022).

Potency assay, off target (cells): Potential off-targets within the S40(1 μM) fraction were tested via biochemical enzymatic and/or NanoBRET target engagement assays. AAK1: IC50 of 2300 nM; BMP2K: IC50 of 5700 nM in NAnoBRET

Off Target: BMP2K

Potency end-point : IC50 320 nM

I have extra information to add

SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Good in vitro binding affinity & in cells. Comprehensive data in cells with multiple cancer cell lines. Recommended 1 uM for use in cells due to toxicity approaching 10 uM. The compound also shows binding to 2 other related targets AAK1, BMP2K.

(last updated: 23 Sept 2024 )