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ULK-101 | ULK-101 : Inhibitor of ULK1, ULK2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ULK1
  • IC 50:8.3 nM
  • EC 50:390 nM
ULK2
  • IC 50:30 nM
  • EC50:390 nM
Inhibitor
up to 5 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - DRAK1 14 nM, MNK2 22 mM

Potency Assay Off-Target:
Radiometric Assay
Selectivity Assessment Description:
Tested in vitro in a radiometric assay against 327 recombinant kinases. DRAK1 to be 14 nM and that o ...

Potency
Cellular
In Vitro

ULK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.isci.2018.09.012

ULK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.isci.2018.09.012

Chemical Information

Molecular Formula C22H16F4N4OS
SMILEs O=C(N[C@@H](C1CC1)C(F)(F)F)c1cc(-c2cnn3cc(-c4ccc(F)cc4)cnc23)cs1
InChI InChI=1S/C22H16F4N4OS/c23-16-5-3-12(4-6-16)15-8-27-20-17(9-28-30(20)10-15)14-7-18(32-11-14)21(31)29-19(13-1-2-13)22(24,25)26/h3-11,13,19H,1-2H2,(H,29,31)/t19-/m0/s1
Molecular weight 460.10 Da
AlogP 5.334600000000003
HBond acceptors 5
HBond donors 1
Atoms 48

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Expert Reviews

by SERP
(on 11 Jul 2020 )
Cellular Use Rating
ULK-101 looks to be an appropriate tool for in vitro/in cellulo studies. Kinase selectivity data is included within the supplementary data. Further confidence in use as probe would come from availability...
by SERP
(on 28 Aug 2020 )
Cellular Use Rating
ULK-101 is a potentially valuable probe for studying ULK1 biology in cells, as it is potent against ULK-1 (8.3 nM) and quite selective against the kinome, with only 2 off-target kinases inhibited at...
by SERP
(on 17 Jun 2024 )
Cellular Use Rating
With an in vitro IC50 for ULK1 of 8,3 nM, selectivity screening should ideally be performed at a higher concentration than 40 nM to better evaluate potential off-targets.
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