MRL-SYKi

MRL-SYKi : Inhibitor of SYK

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe MRL-SYKi is in the process of SERP review.

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Information

Inhibitor

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P43405

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 0.9 nM

Potency Assay: Human SYK enzyme assay

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

Target aliases:

Tyrosine-protein kinase SYK, SYK, KSYK_HUMAN, p72- ...

DOI Reference: 10.6019/CHEMBL4507285

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: ZAP70

Probe Selectivity in Vitro:

Selectivity within target family - Based on an internal assessment we found the closely related kinase ZAP70 to be inhibited by MRL-SYKi with an IC50 of 24 nM. This activity has been confirmed in number of cellular assays; in human PBMCs for example the effect on B-cells is approximately 7 times greater than T-cells (307 nM vs. 2.06 mM respectively). - Profiled in an Invitrogen panel of 265 kinases: > 100-fold kinome selective, 28 kinases fell within the 100-1000-fold selectivity window. The closest off-target kinases were SRC (IC50 = 100 nM), NTRK1 28 (IC50 = 105 nM) and NTRK3 (IC50 = 120 nM). Selectivity outside target family - Profiled in a panel of 113 enzymes and receptors at MDS Pharma/Taiwan at 10 µM: clean; Clean GPCR scan

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The additional activity of the molecule on ZAP70 (24 nM in vitro) needs to be considered when using the probe to interrogate SYK. The activity of the negative control on ZAP70 is not given.

(last updated: 3 Mar 2022 )