OTSSP167

Inhibitor, ATP competitive of MELK

Structure

Information

Protein target names: MELK

Mechanism of action: Inhibitor, ATP competitive

In Vitro Validations

Uniprot ID: Q14680
Target Class: Protein kinase
Target SubClass: CAMK
Potency: IC50
Potency Value: 0.41 nM
Potency Assay: In vitro kinase assay using recombinant proteins
PDB ID for probe-target interaction (3D structure): 4CQG
Target aliases:
Maternal embryonic leucine zipper kinase, KIAA0175 ...

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating

Comments:

Broad kinase selectivity data is not available for this compound.

(last updated: 6 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Recently reported selectivity data show that this is not a selective MELK inhibitor (http://www.kinase-screen.mrc.ac.uk/screening-compounds/594372). Based on the selectivity data, I do not recommend this compound as a probe to use in cells or model organisms even though this molecule has entered into Phase 1 clinical trials. OTSSP167 abrogates mitotic checkpoint through inhibiting multiple mitotic kinases (http://dx.doi.org/10.1371/journal.pone.0153518).

(last updated: 16 May 2016 )