SGC-CLK-1

Protein target name:

CLK1, CLK2, CLK4

Mechanism of action:

Inhibitor, ATP Competitive

Recommended Concentration for use in cells:

up to 1 uM

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

CMGC

HUGO ID:

HGNC:2068 HGNC:2069 HGNC:13659

Entrez gene ID:

1195 1196 57396

UNIPROT ID:

P49759 P49760 Q9HAZ1

Target alias:

CLK; STY; CLK/STY; CDC-like kinase 2; CDC-like kinase 4

Probe Details

Chemical Probes Portal ID:

CPP2205

Probe alias:

cpd 47

PubChem CID:

146681133

ChEMBL ID:

CHEMBL187139

SMILES string:

COC1=NN2N=CC(C3=NC(NC4=CC(C(F)(F)F)=CC(OC)=C4)=NC=C3)=C2C=C1

InChi Key:

GJYVLTPTDBQQCY-UHFFFAOYSA-N

Control compound:

SGC-CKL-1N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

13 nM CLK1, 4 nM CLK2, 46 nM CLK4

Potency assay:

Luceome Biotechnology Binding assay

Structure-activity relationship:

yes

Off target activity

Potency assay (off target):

KINOMEscan

Probe Selectivity in Vitro:

Only 6/403 kinases with PoC<35 when screened at 1 µM in KINOMEscan. (ERK8, NEK7, PIP5K2B, HIPK1 50 nM, HIPK2 42 nM, STK16 49 nM, also 167 nM in NanoBRET)

In cell validation

On target activity in cells

Potency in cells:

IC50

165 nM CLK1, 100 nM CLK2, 70 nM CLK4

Potency assay (cells):

NanoBRET

Primary Reference

Reference (doi):

10.3390/ijms21207549

Reference (PMID):

33066143

External Resources

Available data:

SGC Chemical Probes

Under Review

This probe is in the process of SAB review. Please continue to check back for new reviews and commentary.

Part of SGC Chemical Probe Collection

SAB Rating

Rating for use in Cells

2 review(s)

Rating for use in Model Organisms

2 review(s)

SAB Members

SAB Comments

This probe has potent activity against the CLK family of CMGC kinases (1,2,4). It seems to be a good probe for these targets in cells. However, there is no data provided for the most related kinases, DYRK1A/B and DYRK2. Lack of activity against these kinases would make this probe even more valuable, as there are many probes against this family generally, but it has been difficult to separate CLK activity from DYRK activity.

May 6 2021 - 10:38am

SGC-CLK-1

Probe Information

Target Details

CLK; STY; CLK/STY; CDC-like kinase 2; CDC-like kinase 4

Probe Details

In vitro validation

In cell validation

Primary Reference

External Resources

Supporting Organizations

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SGC-CLK-1

Probe Information

Target Details

CLK; STY; CLK/STY; CDC-like kinase 2; CDC-like kinase 4

Probe Details

In vitro validation

In cell validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?