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NR162 | NR162 : Inhibitor of CASK
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
CASK
  • Kd:22 nM
  • IC50:80 nM
Inhibitor
up to 3 uM
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
NR162 has been shown to be selective in a DiscoverX KINOMEScan at 1 µM. The closest off-target was T ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
In the NCI-60 screen, which is a human tumor cell line screen, NR162 showed no significant cell toxi ...

Potency
Cellular
In Vitro

CASK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.1c00845

Negative Control Compounds

CANSAR3550554
Notes: The negative control NR187 with its blocked hinge-binding amine showed no activity in NanoBRET and KINOMEScan was also clean.

Chemical Information

Molecular Formula C24H30Br2N6O3
SMILEs Cc1cc(Br)c(CNc2ncc(C(=O)NCCCN3CCOC3=O)c(NC3CCCC3)n2)cc1Br
InChI InChI=1S/C24H30Br2N6O3/c1-15-11-20(26)16(12-19(15)25)13-28-23-29-14-18(21(31-23)30-17-5-2-3-6-17)22(33)27-7-4-8-32-9-10-35-24(32)34/h11-12,14,17H,2-10,13H2,1H3,(H,27,33)(H2,28,29,30,31)
Molecular weight 608.07 Da
AlogP 0.0
HBond acceptors 9
HBond donors 3
Atoms 65

Vendors

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Expert Reviews

by SERP
(on 22 Apr 2022 )
Cellular Use Rating
The chemical probe has been well designed and its in vitro and in vivo profile has been thoroughly investigated. The inclusion of a negative control is highly commended, and overall, the probe is fit for...
by SERP
(on 30 Apr 2022 )
Cellular Use Rating
NR162 is a good cellular chemical probe for CASK. The reported binding as well as consistent nanoBRET data with additional characterization in JMC provides a full, but not a complete data set. In particular...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
NR162 shows good potency for its target kinase CASK with good kinome-wide selectivity. It shows 48-fold selectivity over its closest off-target TYRO3. To avoid potential phenotypic effects by inhibiting...
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