Chemical Probes logo
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
Download

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

NR187
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

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

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