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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

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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 public 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