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MK-5108 | MK-5108 : ATP competitive inhibitor of AURKA
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
AURKA
  • IC50:0.064 nM
ATP competitive
1 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - AURKB 14.1 nM, AURKC 12.1 nM, TRKA 2 nM, TRKB 13 nM

Potency Assay Off-Target:
Kinase Profiler Assay
Selectivity Assessment Description:
MK-5108 was tested in the Kinase Profiler Assay against 233 kinases. MK-5108 does not bind to GAB ...

Potency
Cellular
In Vitro

AURKA

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1535-7163.MCT-09-0609

Orthogonal Probes def

AMG900
XMD-12

Chemical Information

Molecular Formula C22H21ClFN3O3S
SMILEs O=C(O)C1(Cc2cccc(Nc3nccs3)n2)CCC(Oc2cccc(Cl)c2F)CC1
InChI InChI=1S/C22H21ClFN3O3S/c23-16-4-2-5-17(19(16)24)30-15-7-9-22(10-8-15,20(28)29)13-14-3-1-6-18(26-14)27-21-25-11-12-31-21/h1-6,11-12,15H,7-10,13H2,(H,28,29)(H,25,26,27)
Molecular weight 461.10 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 52

Vendors

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Expert Reviews

by SERP
(on 3 Jun 2016 )
Cellular Use Rating
In Model Organisms
This is an excellent probe to interrogate Aurora A kinase in vitro and in vivo. It has good selectivity over Aurora B (220-fold) and Aurora C (190-fold). It is known to inhibit only one kinase, TRKA,...
by SERP
(on 12 Sept 2016 )
Cellular Use Rating
In Model Organisms
This compound is reported to have good potency and selectivity for AurA, including over AurB and C. A wide range of cellular work has been published (see for example Chinn et al., J Cancer Res Clin...
by SERP
(on 13 Mar 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria