SGC-CLK-1

SGC-CLK-1 : ATP Competitive inhibitor of CLK1, CLK2 and CLK4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe SGC-CLK-1 is in the process of SERP review.

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Information

CLK1
CLK2
CLK4

Inhibitor, ATP Competitive

DOI - 10.3390/ijms21207549

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P49759

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 13 nM

Potency Assay: Luceome Biotechnology Binding assay

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

Structure-activity relationship: yes

Target aliases:

Dual specificity protein kinase CLK1, CLK, CLK1, C ...

DOI Reference: 10.3390/ijms21207549

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

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)

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP 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.

(last updated: 6 May 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 27 May 2021 )