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OTSSP167 | OTSSP167: ATP competitive inhibitor of MELK
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
MELK
  • IC50:0.41 nM
  • IC50:2.3 - 97 nM
up to 100 nM

Selectivity

Potency
Cellular
In Vitro

MELK

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.18632/oncotarget.790

In Vivo Validations

Mouse
Dose: 1-20 mg/Kg
Route of delivery: Intravenous, Oral

Reference: --

Orthogonal Probes def

NVS-MELK8a
JNJ-47117096

Chemical Information

Molecular Formula C25H28Cl2N4O2
SMILEs CC(=O)c1cnc2ccc(-c3cc(Cl)c(O)c(Cl)c3)nc2c1N[C@H]1CC[C@H](CN(C)C)CC1
InChI InChI=1S/C25H28Cl2N4O2/c1-14(32)18-12-28-22-9-8-21(16-10-19(26)25(33)20(27)11-16)30-24(22)23(18)29-17-6-4-15(5-7-17)13-31(2)3/h8-12,15,17,33H,4-7,13H2,1-3H3,(H,28,29)/t15-,17-
Molecular weight 486.16 Da
AlogP 6.044100000000006
HBond acceptors 6
HBond donors 2
Atoms 61

Vendors

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Expert Reviews

by SERP
(on 6 May 2016)
Cellular Use Rating
Broad kinase selectivity data is not available for this compound.
by SERP
(on 16 May 2016)
Cellular Use Rating
In Model Organisms
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...
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